СПОСОБ ПОЛУЧЕНИЯ СМЕСЕЙ КРЕМНИЙОРГАНИЧЕСКИХ ОЛИГОСУЛЬФАНОВ С ВЫСОКИМ СОДЕРЖАНИЕМ КРЕМНИЙОРГАНИЧЕСКИХ ДИСУЛЬФАНОВ

Описывается способ получения смесей кремнийорганических олигосульфанов с высоким содержанием дисульфанов общей формулы Z-Alk-Sx-Alk-Z, в которой Z представляет собой группировки в которых R1 представляет собой линейную либо разветвленную алкильную группу с 1-6 С-атомами, циклоалкильный остаток с 5-8 С-атомами, бензильный остаток или не обязательно замещенный метилом, этилом либо хлором фенильный остаток; R2 представляет собой алкоксигруппу с линейной либо разветвленной углеродной цепью с 1-6 С-атомами или циклоалкоксигруппу с 5-8 С-атомами, феноксигруппу или бензилоксигруппу, причем R1 и R2 могут иметь соответственно идентичные или разные значения; Alk представляет собой предпочтительно двухвалентный насыщенный линейный либо разветвленный углеводородный остаток с 1-10 С-атомами, предпочтительно метилен, а также предпочтительно этилен, изопропилен, н-пропилен, изобутилен или н-бутилен, в равной степени предпочтительны и такие значения, как н-пентилен, 2-метилбутилен, 3-метилбутилен, н-пентилен ...

Смеси силанов и способ приготовления таких смесей силанов

КАРБАМИДСОДЕРЖАЩИЕ СИЛАНЫ, СПОСОБ ИХ ПОЛУЧЕНИЯ И ИХ ПРИМЕНЕНИЕ

РЕГИОСЕЛЕКТИВНЫЙ СИНТЕЗ CCI-779

... 1. Способ получения сложного 42-эфира рапамицина, который включает(а) ацилирование 31-силилового эфира рапамицина соединением формулыНООС.CRRRили его смешанным ангидридом,где Rпредставляет собой водород, алкил с 1-6 атомами углерода, алкенил с 2-7 атомами углерода, алкинил с 2-7 атомами углерода, -(CRR)OR, -CF, -F или -COR;Rпредставляет собой водород, алкил с 1-6 атомами углерода, алкенил с 2-7 атомами углерода, алкинил с 2-7 атомами углерода, трифенилметил, бензил, алкоксиметил с 2-7 атомами углерода, хлорэтил или тетрагидропиранил;Rи R, взятые вместе, образуют Х;Х представляет собой 2-фенил-1,3,2-диоксаборинан-5-ил или 2-фенил-1,3,2-диоксаборинан-4-ил, где фенил может быть необязательно замещенным;Rи Rкаждый, независимо, представляет собой водород, алкил с 1-6 атомами углерода, алкенил с 2-7 атомами углерода, алкинил с 2-7 атомами углерода, трифторметил или -F; и f = 0-6;для образования 42-эфирбороната 31-силилового эфира рапамицина;(b) селективный гидролиз 42-эфирбороната 31-силилового ...

СПОСОБЫ ПОЛНОГО СИНТЕЗА РЕЗОЛВИНА E1

СПОСОБ ПОЛУЧЕНИЯ НЕНАСЫЩЕННЫХ ИМИДОАЛКОКСИСИЛАНОВ

... 1. Способ получения ненасыщенного циклического имидоалкоксисилана, который включает ! i) трансимидацию по существу безводного защищенного по методу Дильса-Альдера ненасыщенного ароматического N-замещенного циклического имида с по крайней мере одним аминоалкоксисиланом с целью получения по крайней мере одного защищенного по методу Дильса-Альдера ненасыщенного циклического имидоалкоксисилана. ! 2. Способ по п.1, кроме того, включающий ! i) снятие защиты защищенного циклического имидоалкоксисилана с целью получения α,β-ненасыщенного циклического имидоалкоксисилана. ! 3. Способ по п.1, в котором защищенный по методу Дильса-Альдера ненасыщенный ароматический N-замещенный циклический имид получают методом, включающим имидацию циклического ненасыщенного ангидрида с по крайней мере одним первичным ароматическим амином с целью получения по крайней мере одного ненасыщенного ароматического N-замещенного циклического имида и защиту двойной связи ненасыщенного N-замещенного циклического имида с по крайней ...

СПОСОБ ПОЛУЧЕНИЯ ОРГАНОСИЛАНОВ

... 1. Способ получения органосиланов общей формулы Iв которойR являются одинаковыми или разными и обозначают С-С-алкильную, C-C-алкенильную, C-C-арильную, C-C-арилалкильную группу или группу OR', R' являются одинаковыми или разными и обозначают С-Сразветвленную или неразветвленную одновалентную алкильную или алкенильную группу, арильную группу, арилалкильную группу, водород (-Н), простую алкилэфирную группу O-(CR )-O-Alk или O-(CR )-O-Alk или простую алкилполиэфирную группу O-(CR -O)-Alk или O-(CR -CR -O)-Alk, где y=2-20, Rнезависимо обозначает Н или алкильную группу и Alk представляет собой разветвленную или неразветвленную, насыщенную или ненасыщенную алифатическую, ароматическую или смешанную алифатическую/ароматическую одновалентную С-С-углеводородную группу,R'' обозначает разветвленную или неразветвленную, насыщенную или ненасыщенную алифатическую, ароматическую или смешанную алифатическую/ароматическую одновалентную С-С-углеводородную группу, которая необязательно замещена с помощью ...

CПOCOБ ПOЛУЧEHИЯ CИЛAHOBOГO COEДИHEHИЯ

Verfahren zur Herstellung von Zwischenverbindungen für Vitamin-D-Derivate sowie Verbindungen

Verfahren zur Herstellung von Organosilylalkylpolysulfanen

Verfahren zur Herstellung von Arylaminoalkylpolysiloxanen

Verfahren zur Herstellung von Alkylaminen

Gegenstand der Erfindung ist ein kontinuierliches Verfahren zur Herstellung von Alkylaminen, bei dem kontinuierliche Ströme von Ammoniak und Alkylhalogenid mit einem molaren Verhältnis von mindestens 10 : 1 in einem Druckreaktor zur Reaktion gebracht werden. Die Endreaktionsmischung besteht bei einer Temperatur > 80 DEG C, einem Druck > 40 bar und einem Ammoniumhalogenid-Gehalt von > 1 Gew.-% aus zwei Phasen DOLLAR A A welche mindestens 75 Gew.-% der gebildeten Gesamtmenge an Ammoniumhalogenid enthält und DOLLAR A B welche mindestens 80 Gew.-% der Gesamtmenge an Alkylamin enthält, DOLLAR A die aufgetrennt werden.

Verfahren zur Herstellung fluorierter cyclischer aliphatischer Verbindungen

Die vorliegende Erfindung betrifft ein neuartiges Verfahren zur Herstellung fluorierter cyclischer aliphatischer Verbindungen aus den analogen aromatischen Verbindungen durch Hydrierung mit einem Rh-Katalysatorsystem.

Verfahren zur Herstellung von sekundären und tertiären Amino-funktionellen Silanen

VERFAHREN ZUR HERSTELLUNG VON 1-HYDROXY-2-SUBSTITUIERTEN CYCLOHEXYLAZETIDIN-2-ON-VERBINDUNGEN

CHEMICAL PROCESS

PROCESS FOR PREPARING SULPHOXIDE CONTAINING COMPOUNDS

PROCESS FOR THE PRODUCTION OF SULPHUR-CONTAINING ORGANO SILICON COMPOUNDS

Substituted beta-lactam compounds useful as hypocholesterolemic agents and processes for the preparation thereof

PROCEDURE FOR THE PRODUCTION OF N-2AMINOETHYLAMINOALKYLALKOXYSILANEN WITH ETHYL DIAMINE SALT RECUPERATION

PROCEDURE FOR THE PREVENTION OF THE POLYMERIZATION OF INSATIATED ORGANOSILICIUMVERBINDUNGEN

PROCEDURE FOR THE PRODUCTION OF MERCAPTOALKYLALKOXYSILANEN

SUBSTITUTED BETA LACTAM CONNECTIONS AS HYPOCHOLESTEROLEMI MEANS AND PROCEDURE FOR THEIR PRODUCTION

PROCEDURE FOR THE PRODUCTION OF AMINOALKYLSILANEN

PROCEDURE FOR THE PRODUCTION OF ORGANOSILYLALKYLPOLYSULFANEN

PROCEDURE FOR THE PRODUCTION OF PRIMARY AMINOORGANOSILANEN

PROCEDURE FOR THE PRODUCTION OF METHACRYLOXY OR ACRYLOXYGRUPPEN ABSTENTION ORGANOSILANEN

(1S, 2S, 3R, 5R) - 2 ((3S) - 2-HALOGEN-3-HYDROXY-1ALKEN (INYL) >3-TRIALKYL-SILYLOXY-7,7 (2,2-DIMETH L-TRIMETHYL-ENOXY) - BICYCLO (3.3.0>OCTAN-VERBINDU GENE AND PROCEDURE FOR THEIR PRODUCTION.

PROCEDURE FOR THE PRODUCTION OF MIXTURES OF ORGANOSILICIUMOLIGOSULFANEN WITH A HIGH PORTION OF ORGANOSILICIUMDISULFANEN

POLYSULFIDE SILANES WITH LOW SULPHUR CONTENT AND A PROCEDURE FOR THEIR PRODUCTION

PROCEDURE FOR THE PRODUCTION OF TO (SILYLORGANYL) - POLYSULFANEN

PROCEDURE FOR THE PRODUCTION OF ORGANOSILYLALKYLPOLYSULFANEN

Stereoselective ring opening reactions

Process for the preparation of thiocarboxylate silane

Intermediary compounds for the hemisynthesis of taxanes and preparation processes therefor

Processes for production of phenolic 4-biphenylylazetidin-2-ones

A facile method for synthesizing baccatin III compounds

INTERMEDIATES FOR THE SYNTHESIS OF DISCODERMOLIDE AND RELATED ANALOGUES AND METHODS FOR THEIR PREPARATION

Process for synthesizing aspartic and glutamic acid derivatives and diazoketone intermediates thereof

METHOD OF PREPARING ORGANO DIALKYLALKOXYSILANE

Process for selective derivatization of taxanes

Synthesis of epothilones, intermediates thereto and analogues therof

PROCESS FOR SYNTHESIS OF ACYLAMINO ORGANOSILICON COMPOUNDS

ROSUVASTATIN AND SALTS THEREOF FREE OF ROSUVASTATIN ALKYLETHER AND A PROCESS FOR THE PREPARATION THEREOF

LIGANDS FOR METALS AND METAL-CATALYZED PROCESSES

One aspect of the present invention relates to novel ligands for transition metals. A second aspect of the present invention relates to the use of catalysts comprising these ligands in transition metal-catalyzed carbon- heteroatom and carbon-carbon bond-forming reactions. The subject processes provide improvements in many features of the transition metal-catalyzed reactions, including the range of suitable substrates, reaction conditions, and efficiency.

PROCESSES FOR PREPARING CLARITHROMYCIN AND CLARITHROMYCIN INTERMEDIATE, ESSENTIALLY OXIME-FREE CLARITHROMYCIN, AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME

PROCESS FOR MANUFACTURING ACRYLAMIDOALKYLALKOXYSILANES

A method for preparing acrylamidoalkylalkoxysilanes from aminoalkylalkoxysilanes and acrylate esters is described wherein at least two inhibitors and an amidation catalyst are used in an elevated temperature reaction.

PROCESS FOR PREPARING ENTECAVIR AND ITS INTERMEDIATES

A process of making entecavir comprising converting a compound of formula (M5) to entecavir, wherein the two PGs on the formula (M5) are taken together to form an optionally substituted six- or seven-member cyclic ring.

VITAMIN D PRECURSORS, METHOD AND INTERMEDIATES

The invention relates to precursors of the A-ring of vitamin D, of formula (I): in which A, R, R1 and R2 are as defined in the specification. The invention also relates to a method of preparing compounds (I) comprising the enzymatic asymmetrisation of 3,5-dihydroxybenzoic acid derivatives, as well as intermediates of preparation of said compounds.

METHOD OF PREPARING MERCAPTANS

SYNTHESIS OF EPOTHILONES, INTERMEDIATES THERETO AND ANALOGUES THEROF

The present invention provides convergent processes for preparing epothilone A and B, desoxyepothilones A and B, and analogues thereof, useful in the treatment of cancer and cancer which has developed a multidrug-resistant phenotype. Also provided are intermediates useful for preparing said epothilones.

PROCESS FOR PRODUCING SULPHUR-CONTAINING ORGANOSILICON COMPOUNDS

METHOD FOR SILYLATING UNSATURATED NATURALLY OCCURRING OILS OR TRANSESTERIFICATION PRODUCTS THEREOF

TWO-STAGE PREPARATION OF GAMMA-MERCAPTOPROPYL TRIALKOXYSILANE

METHOD FOR PREPARING SILICON-CONTAINING HETEROCYCLES

The present invention relates to a method for preparing silicon-containing heterocycles of the general formula (I), wherein R1 is hydrogen; R2 and R3 are same or different and are, independently from one another, selected from a linear or branched, substituted or unsubstituted C1-C20 alkyl or C6-C18 aryl residue which may be interrupted by at least one heteroatom; R4 is selected from a linear or branched C1-C20 alkylene residue which may be interrupted by at least one heteroatom; R5 and R6 are same or different and are, independently from one another, selected from the group consisting of hydrogen, a linear or branched, substituted or unsubstituted C1-C20 alkyl or C6- C18 aryl which may be interrupted by at least one heteroatom, and a C4-C8 cycloalkyl, or R5 and R6 may form a ring, preferably a 4- to 8-membered alkyl ring; and n is 0, 1 or 2, preferably 2, said method comprising a one-step reaction of at least one epoxide compound of the general formula (II) and at least one aminoalkoxysilane ...

HETEROBIFUNCTIONAL POLY(ETHYLENE GLYCOL) AND USES THEREOF

... ²²²The present invention provides bifunctional polymers, methods of preparing the ²same, and intermediates thereto. These compounds are useful in a variety of ²applications including the PEGylation of biologically active molecules. The ²invention also provides methods of using said compounds and compositions ²thereof.² ...

ISOMERISATION OF PHARMACEUTICAL INTERMEDIATES

The present invention relates to an isomerisation method of vitamin D analogues, such as compounds useful for the synthesis of calcipotriol, and to and to the use of a flow- through photoreactor or continuous flow photoreactor reactor for making said vitamin D analogues. The present invention relates further to the use of intermediates produced with said method for making calcipotriol or calcipotriol monohydrate, or pharmaceutical formulations thereof.

PROCESS FOR THE PRODUCTION OF EZETIMIBE AND INTERMEDIATES USED IN THIS PROCESS

This invention provides a novel, industrially easily realizable and economical process comprising only few steps, and built on new intermediates for the production of 1-(4-3(R)- [3(S)-(4-fluorophenyl)-3-hydroxypropyl]-4(S)-(4- hydroxyphenyl)-2-azetidinone (ezetimibe) according to the following reaction scheme: (I), (II), (III), (IV), (V), (VI), (VII), (VIII), (IX), (X), (XI) wherein, the substances of the general Formulas II, IV, VI, VIII, IX, X and XI are new, Formula III is a non-isolated intermediate, Rl, R2 and R3 are represented by the compounds of Formulas Va-Vd, (Va), (Vb), (Vc), (Vd) and R4 is a silil, e.g. tert.buthyl-dimethyl-silil, tert-buthyl-diphenyl-silil group.

METAL-CATALYZED ASYMMETRIC 1,4-CONJUGATE ADDITION OF VINYLBORON COMPOUNDS TO 2-SUBSTITUTED-4-OXY- CYCLOPENT-2-EN-1-ONES YIELDING PROSTAGLANDINS AND PROSTAGLANDIN ANALOGS

This invention provides a novel method for the preparation of 2,3- disubstituted-4-oxy-cyclopentan-l-one compounds that are useful for the synthesis of prostaglandins and prostaglandin analogs of industrial relevance. The method comprises the metal -catalyzed asymmetric 1,4-conjugate addition of vinylboron compounds to 2- substituted-4-oxy-cyclopent-2-en-l-ones. This method relies on the use of less toxic, easily- handled reagents, and can be performed under milder conditions than offered by some conventional methods, affording 2,3-disubstituted-4-oxy-cyclopentan-l-one compounds enantio- and diastereoselectively, which are precursors to the said prostaglandin and prostaglandin analogs, in high yield.

MACROLIDES AND METHODS OF THEIR PREPARATION AND USE

Provided herein are methods of preparing macrolides by the coupling of an eastern and western half, followed by macrocyclization, to provide macrolides, including both known and novel macrolides. Intermediates in the synthesis of macrolides including the eastern and western halves are also provided. Pharmaceutical compositions and methods of treating infectious diseases and inflammatory conditions using the inventive macrolides are also provided. A general diastereoselective aldol methodology used in the synthesis of the western half is further provided.

PROCESS FOR PRODUCING SULPHUR-CONTAINING ORGANOSILICON COMPOUNDS

METHOD FOR FORMING REACTIVE SILANE ESTERS

Methods are provided for preparing reactive silane ester compounds, such as aromatic reactive silane ester compounds. The methods include providing a carboxylic, acid-containing starting material, reacting the carboxylic acid-containing starting material with a base to form a salt, and reacting the salt with a halo-alkylene-silane to form a reactive silane ester compound. Compositions prepared by these methods, protective layers that include hydrolysis and condensation products of such compositions, electrophotographic photoreceptors that include such protective layers, and image forming apparatuses that include such electrophotographic photoreceptors are also provided.

MIXTURES, PARTICULARLY LOW IN VOLATILE ORGANIC COMPOUNDS (VOC), OF OLEFINICALLY FUNCTIONALISED SILOXANE OLIGOMERS BASED ON ALKOXY SILANES

The invention relates to a composition containing olefinically functionalized siloxane oligomers which are derived from olefinically functionalized alkoxy silanes and optionally alkoxy silanes functionalized with saturated hydrocarbons and optionally a tetraalkoxysilane, at most comprising an olefinic group on the silicon atom having a reduced chloride content and the VOC content being lower with respect to the hydrolysable alkoxy-groups. The invention also relates to methods for the production thereof and to the use thereof.

PYRANONES

... 2118796 9306235 PCTABS00021 A process for the separation of at least one isomer from a mixture of isomers of a tetrahydropyran-2-one, having at least two chiral centres, which comprises selective reaction of at least one isomer with a reagent catalysed by a hydrolase enzyme whereby at least one isomer is preferentially converted into a distinct chemical species from the other isomers so that it is susceptible of separation by an appropriate chemical or physical separation process in which the tetrahydrapyranone is of formula (1), wherein Z is -H or a protecting group susceptible of reaction with the reagent under the influence of the enzyme; and Y is optionally substituted hydrocarbyl.

ANTIFUNGAL AGENTS, PROCESSES FOR THE PREPARATION THEREOF, AND INTERMEDIATES

A compound represented by the general formula: (see formula 1) wherein R1 and R2 denote a halogen atom or hydrogen atom; R3 means a hydrogen atom or lower alkyl group; ~ , r and m stand for 0 or 1; A is N or CH; W denotes an aromatic ring or a condensed ring thereof; X means another aromatic ring, an alkanediyl group, an alkenediyl group, or an alkynediyl group; Y stand for -S-, etc.; Z denotes a hydrogen atom, etc., or a salt thereof, and intermediates thereof or a salt thereof as well as processes for the preparation thereof, and pharmacetical composition suitable for use as an antifungal agent.

PROCESS FOR THE PREPARATION OF HETEROSUBSTITUTED ACETALS

Heterosubstituted acetals of the formula (I), can be obtained by reacting vinyl compounds of the formula CH2=CH-A1 (II) with alkyl nitrites of the formula R1-ONO (III). The reaction is performed in the presence of palladium in metallic or bonded form and in alcohols or ethers as reaction medium at from 0 to 120.degree.C.

PROCESS FOR REDUCING THE SULFANE CHAIN LENGTH OF BIS(SILYLORGANYL)POLYSULFANES

This invention relates to a process for reducing the sulfane chain length of bis(silylorganyl)polysulfanes, in which these compounds are reacted with an anhydrous sulfide and a haloalkylsilane compound.

AN ASYMMETRIC CONJUGATE ADDITION REACTION

This invention relates to a key intermediate in the synthesis of an endothel in antagonist and the synthesis of this key intermediate using an asymmetric conjugate addition reaction.

PROCESS FOR SELECTIVE REDUCTION

Process for the stereoselective reduction of chiral .alpha.- or .beta.-keto esters which have a chiral centre in the .gamma. position in an inert solvent at temperatures from -80 to +50.degree.C using a reductant obtained by reaction of NaBH4 and (D)- or (L)-tartaric acid, to give the corresponding diastereomeric hydroxy compounds in each case.

PROCESS FOR PREPARING ANTIOSTEOPOROTIC AGENTS

A process for the preparation of a novel triethylsilyl ether analogue of the CD ring fragment of formula (see formula A) wherein R2 is a silyl protecting group; and new intermediates for the preparation of such analogues are disclosed.

VERFAHREN ZUR HERSTELLUNG VON MERCAPTOSILANEN.

PROCEDURE FOR THE PRODUCTION OF SCHWEFELHALTIGEN ORGANOSILICIUMVERBINDUNGEN.

СПОСОБЫ ПОЛУЧЕНИЯ 4-(БИФЕНИЛИЛ)АЗЕТИДИН-2-ОНАЛКИЛФОСФИНОВЫХ КИСЛОТ

Настоящее изобретение относится к способам получения производных 4-(бифенилил)азетидин-2-оналкилфосфиновой кислоты формулы ...

СПОСОБЫ ПОЛУЧЕНИЯ 4-БИФЕНИЛИЛАЗЕТИДИН-2-ОНОВ

Настоящее изобретение относится к способам получения производных 4-бифенилилазетидин-2-она формулы (I).

PROCESS FOR THE PRODUCTION OF YELLOW BIS(3-[TRIETHOXYSILYL]PROPYL)POLYSULFANE

СПОСОБ СИНТЕЗА ИНГИБИТОРОВ HMG-CoA РЕДУКТАЗЫ

В изобретении описан новый синтез статинов с использованием реакции Виттига между гетероциклическим ядром статина и лактонизованной боковой цепью, уже обладающей необходимой стереохимической конфигурацией. Разделение диастереоизомеров проводят в начале синтеза.

ПРОСТОЙ СПОСОБ СИНТЕЗА СОЕДИНЕНИЙ БАККАТИНА III

Способ синтеза соединения баккатина III с защитой по позиции С-7, представленного формулой (А), который включает реакцию соединения 10-деацетилбаккатина III, представленного формулой (Б), с агентом, вводящим защитную группу, и ацилирующим агентом в присутствии вторичного амина и азот-содержащего соединения. А также, способ синтеза соединения 10-деацетилбаккатина III с защитой по позиции С-7, представленного формулой (В), который включает реакцию соединения 10-деацетилбаккатина III, представленного формулой (Б), с агентом, вводящим защитную группу, в присутствии вторичного амина и азотсодержащего соединения. В обоих процессах азотсодержащее соединение выбирают из азотсодержащего гетероцикла или триалкиламина. Когда выбран азотсодержащий гетероцикл, он может быть незамещенным или замещенным пиридином или незамещенным или замещенным пиразином. Когда выбирают триалкиламин, он может быть, например, триэтиламином или диизопропилэтиламином (А, Б, В), где PG1 представляет органический остаток агента ...

METHODS AND SYSTEMS FOR SYNTHESIS OF CAMPTOTHECIN ANALOGS

СПОСОБ ПОЛУЧЕНИЯ МЕРКАПТООРГАНИЛ(АЛКОКСИСИЛАНОВ)

В заявке описан способ получения меркаптоорганил(алкоксисиланов), который состоит в том, что бис(алкоксисилилорганил)полисульфиды гидрируют под действием водорода в присутствии, по крайней мере, одного спирта и одного легированного металлического катализатора, который содержит, по крайней мере, одно вещество из группы, которая включает железо, железосодержащее соединение, никель, никельсодержащее соединение, палладий, палладийсодержащее соединение, осмий, осмийсодержащее соединение, рутений, рутенийсодержащее соединение, родий, родийсодержащее соединение, иридий и иридийсодержащее соединение, и, по крайней мере, одну легирующую примесь.

СПОСОБ ПОЛУЧЕНИЯ ЭЗЕТИМИБА И ПРОМЕЖУТОЧНЫХ ПРОДУКТОВ, ИСПОЛЬЗУЕМЫХ В ЭТОМ СПОСОБЕ

Настоящее изобретение обеспечивает новый, легко реализуемый в промышленности и рентабельный способ, содержащий только небольшое число стадий и основанный на использовании новых промежуточных продуктов, для получения 1-(4-3(R)-[3(S)-(4-фторфенил)-3-гидрокспропил]-4(S)-(4-гидроксифенил)-2-азетидинона (эзетимиба) согласно следующей реакционной схеме: (I), (II), (III), (IV), (V), (VI), (VII), (VIII), (IX), (X), (XI), где соединения общих формул II, IV, VI, VIII, IX, Х и XI являются новыми веществами, формула III обозначает невыделенный промежуточный продукт, R1, R2 и R3 представлены соединениями формул Va-Vd, (Va), (Vb), (Vc), (Vd) и R4 представляет собой силильную, например, трет-бутилдиметилсилильную, трет-бутилдифенилсилильную группу.

METHOD OF OBTAINING THE DERIVATIVES OF THE ACID

РЕГІОСЕЛЕКТИВНИЙ СИНТЕЗ ССІ-779

Пропонується спосіб регіоселективного синтезу ССІ-779, оснований на хімії боронатів. Також запропоновані нові проміжні продукти, що застосовуються в даному способі.

METHOD FOR SYNTHESIS OF ORGANOSILYLALKYLPOLYSULFANES

Networked organosilicon polysulphides

ЧЕТЫРЕХЦИКЛИЧЕСКИЕ КОНДЕНСИРОВАННЫЕ СОЕДИНЕНИЯ С ГЕТЕРОАТОМАМИ, ЗАМЕЩЕННЫЕ АРИЛОМ, ПРОМЕЖУТОЧНЫЕ СОЕДИНЕНИЯ, СПОСОБЫ ПОЛУЧЕНИЯ, КОМПОЗИЦИИ И МЕТОДЫ ЛЕЧЕНИЯ

Данное изобретение относится к соединениям формулы (I) и (II), где Х обозначает -О-; Y обозначает -О-, -S-, -CH2-, -CH2CH2-, -СН=СН- или -NR4-; В обозначает -CH2- или -СО-; R1, R2 обозначают каждый независимо -Н, -ОН, -O(С1-С4алкил), -OCOC6H5, -OCO(С1-С6алкил), -OSO2(С4-С6алкил), ОSО2СF3, Сl или F; n равно 1 или 2; W обозначает СН2 или С=O; R3 обозначает 1-пиперидинил, 2-оксо-1-пиперидинил, 1-пирролидинил, метил-1-пирролидинил, диметил-1-пирролидинил, 2-оксо-1-пирролидинил, 4-морфолино, диметиламино, диэтиламино или 1-гексаметиленимино; R4 oбозначает С1-С3алкил, -COC6H5, -CO(С1-С6алкил), -С(O)ОС6Н5, -C(O)O(С1-С6алкил), -SO2(С1-С6алкил), -SO2C6H5 или -SО2СF3; или их фармацевтически приемлемые соли. Данное изобретение также представляет промежуточные соединения, способы получения соединений формулы (I) и (II) и фармацевтические способы и лекарственные формы с использованием соединений формулы (I) и (II).

METHOD OF THE SYNTHESIS OF THE INHIBITORS Of hMG-CoA OF THE REDUCTASE

PROCESSES FOR PREPARING JAK INHIBITORS AND RELATED INTERMEDIATE COMPOUNDS

A method for preparing the vinyl-terminated siloxane

Guanidine official functionalized particle and its preparation and methods of use

Process for the preparation of (mercaptoorganyl)-alkoxysilanen

Process for the preparation of organic compounds of silicon

Synthesis of enone intermediate

The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides a more efficient route for preparing the enone intermediate.

Methods of making lubiprostone and intermediates thereof

There is provided processes for preparing Lubiprostone and intermediates thereof. Also provided are compounds, including intermediates for preparing Lubiprostone as well compositions comprising Lubiprostone and other compounds, including intermediates for preparing Lubiprostone and other compounds. (I)

Method for producing alkoxy-substituted 1,2-bissilylethanes

The invention relates to a method for producing alkoxy-substituted 1,2-bissilylethanes of the general formula 1 (R 1 O) n R 2 (3-n) Si—CH 2 —CH 2 —SiR 2 (3-n) (OR 1 ) n   (1), which comprises reacting, in a first step, a mixture containing compounds of the general formulae 2 and 3 Cl n R 2 (3-n) Si—CH 2 —CH 2 —SiR 2 (3-n) Cl n   (2) Cl n R 2 (3-n) Si—CH═CH—SiR 2 (3-n) Cl n   (3) with an alcohol of the general formula 4 R 1 OH  (4) and, in a second step, subjecting the resultant mixture which contains compounds of the general formula 1 and compounds of the general formula 5 (R 1 O) n R 2 (3-n) Si—CH═CH—SiR 2 (3-n) (OR 1 ) n   (5) to reductive conditions such that the compound of the general formula 5 is converted into a compound of the general formula 1, wherein R 1 and R 2 are monovalent, unsubstituted or halogen-substituted hydrocarbon radicals having 1 to 16 carbon atoms and n is the value 1, 2 or 3.

Trihydroxy polyunsaturated eicosanoid derivatives

The invention features methods for the preparation of naturally occurring trihydroxy polyunsaturated eicosanoids and their structural analogs. The invention further provides new derivatives and analogs of trihydroxy polyunsaturated eicosanoids that can be prepared according to these methods. The invention also provides compositions and methods using trihydroxy polyunsaturated eicosanoid derivatives for the prevention, amelioration and treatment of a variety of diseases or conditions associated with inflammation or inflammatory response, autoimmune diseases, rheumatoid arthritis, cardiovascular diseases, or abnormal cell proliferation or cancer.

Method of producing beraprost

An improved method is described for making single isomers of synthetic benzoprostacyclin analogue compounds, in particular the pharmacologically active 314-d isomer of beraprost. In contrast to the prior art, the method is stereoselective and requires fewer steps than the known methods for making these compounds.

ALKOXYSILANE FUNCTIONALIZED ISOCYANATE BASED MATERIALS

Alkoxysilane functionalized isocyanate based materials of low viscosity prepared by reacting in any possible order of addition an organic polyisocyanate with an isocyanate-reactive compound and an amino-functional alkoxysilane of formula I 2. The process according to wherein the organic polyisocyanate is pre-reacted with the compound containing isocyanate-reactive hydrogen atoms to form a so-called isocyanate functional prepolymer.3. The process according to wherein the compound containing isocyanate-reactive hydrogen atoms has a functionality of at least 2 and a molecular weight of at least 400.4. The according to wherein the polyisocyanate is reacted with the isocyanate-reactive compound in a molar ratio NCO/OH of at least 2.5. The process according to wherein the molar ratio amine/NCO is from 1 to 100.6. The process according to wherein said polyisocyanate is a difunctional aromatic isocyanate.7. The process according to wherein said polyisocyanate is based on diphenylmethane diisocyanate.8. The process according to wherein R represents an aryl claim 1 , vinyl or carbamate group.9. The process according to wherein R is a phenyl group.10. The process according to wherein Rrepresents a linear alkylene group containing 1 to 4 carbon atoms.11. The process according to wherein both Rand Rrepresent an alkylene group having 1 to 4 carbon atoms.12. The process according to wherein x is 0 or 1.13. The process according to wherein the amino-functional alkoxysilane is gamma-N-phenylaminopropyl trimethoxysilane.14. An alkoxysilane functionalized isocyanate based material obtainable by the process of .15. An alkoxysilane functionalized isocyanate based material according to having a biuret-urea ratio of less than 0.5.16. An alkoxysilane functionalized isocyanate based material according to having a viscosity of at most 200 Pa.s.17. An alkoxysilane functionalized isocyanate based material according to wherein the alkoxysilane functionalized isocyanate based material comprises ...

Functionalized Particles and Use Thereof

A method of making a powder coating composition includes obtaining functionalized particles by reacting inorganic particles with alkoxysilanes having the general structural formula (I) RSi(OR), silane oligomers having the general structural formula (II) (R)(OR)Si-O-[-Si(R)(OR)-O-]-Si(R)(OR)or mixtures thereof. 2. The powder coating composition as claimed in claim 1 , which comprises functionalized particles obtainable by a method which comprises subjecting the reaction mixture obtained after the reaction to drying.3. The powder coating composition as claimed in claim 1 , wherein titanium dioxide particles or barium sulfate particles are used as inorganic particles.4. The powder coating composition as claimed in claim 1 , comprising:a. 20% to 80% by weight of binder,b. 5% to 60% by weight of inorganic pigment or mineral filler,c. 5% to 60% by weight of functionalized inorganic particles,d. 0.1% to 10.0% by weight of additive, selected from flow, leveling, and deaerating additives or mixtures thereof, with all of the ingredients together making 100% by weight.5. The powder coating composition according to claim 4 , where the functionalized pigment and/or the filler is present in an amount of 10% to 50% by weight claim 4 , preferably 30% to 40% by weight.6. (canceled)7. An article powder coated with the coating composition according to .89-. (canceled)11. A method as claimed in claim 10 , wherein Ris a nonhydrolyzable claim 10 , aliphatic claim 10 , straight-chain or branched-chain hydrocarbon radical having 1 to 10 carbon atoms.12. A method as claimed in claim 10 , wherein Ris a nonhydrolyzable claim 10 , aliphatic claim 10 , straight-chain or branched-chain hydrocarbon radical having at least one terminal claim 10 , functional group which is able to enter into an addition reaction or condensation reaction.13. A method as claimed in claim 10 , wherein Ris a nonhydrolyzable claim 10 , aliphatic claim 10 , straight-chain or branched-chain hydrocarbon radical having at ...

RUTHENIUM COMPLEXES FOR USE IN OLEFIN METATHESIS

Cls ruthenium complexes that can be used as catalysts are described. The complexes are generally square pyramidal in nature, having two anionic ligands X adjacent to each other. The complexes can be used as catalysts, for example in olefin metathesis reactions. Corresponding trans ruthenium complexes are also described, together with cationic complexes where one or both of the anionic ligands X are replaced by a non-co-ordinating anionic ligand. 2. The cis ruthenium complex according to wherein the anionic ligands X are independently selected from the group consisting of halogen claim 1 , benzoate claim 1 , C-Ccarboxylates claim 1 , C-Calkoxy claim 1 , phenoxy claim 1 , C-Calkyl thio groups claim 1 , tosylate claim 1 , mesylate claim 1 , brosylate claim 1 , trifluoromethane sulfonate claim 1 , and pseudo-halogens.3. The cis ruthenium complex according to wherein the groups Rand Rare H and aryl.4. The cis ruthenium complex according to wherein the groups Rand Rare fused to form a substituted or unsubstituted indenylidene moiety.6. The cis ruthenium complex according to wherein the phosphite group is selected from the group consisting of P(OMe)P(OEt) claim 5 , P(OiPr)and P(OPh).7. The cis ruthenium complex according to wherein the group A is a nucleophilic carbene having a four claim 1 , five claim 1 , six or seven membered ring containing the carbene carbon.8. The cis ruthenium complex according to wherein the group A is an N-heterocyclic carbene.9. The cis ruthenium complex according to wherein the N-heterocyclic carbene ligand contains more than one nitrogen atom in the ring and/or contains at least one of O or S in the ring.11. The cis ruthenium complex according to wherein the N-heterocyclic carbene ligand contains two nitrogen atoms in the ring claim 9 , each adjacent the carbene carbon.18. The method of wherein the leaving group L is selected from the group cnsisting of; substituted or unsubstituted pyridine claim 17 , phosphine claim 17 , phosphite claim 17 , ...

CYCLIZATION METHODS

The invention provides methods for cyclizing poly-yne compounds under mild conditions to provide cyclic compounds. 1. A method comprising cyclizing a tri-yne compound at a temperature below about 300° C. to provide a polycyclic compound.2. A method comprising cyclizing a nonaromatic compound comprising at least three alkyne groups at a temperature below about 300° C. to provide a polycyclic compound.3. A method comprising cyclizing a first compound that comprises two or more alkyne groups with a second compound that comprises at least one alkyne group at a temperature below about 300° C. to provide a cyclic compound.5. The method of wherein W comprises 2 claim 4 , 3 claim 4 , 4 claim 4 , or 5 alkyne groups.6. The method of wherein W comprises 2 or 3 alkyne groups.7. The method of wherein X is a linking group that comprises 2-20 carbon atoms and at least one severable group.8. The method of wherein X is a linking group that comprises 2-10 carbon atoms and at least one severable group.9. The method of wherein the severable group is selected from an ester claim 4 , an amide claim 4 , a carbonate claim 4 , a carbamate claim 4 , an ether claim 4 , a silylether claim 4 , an alkene claim 4 , a urea claim 4 , a sulfide claim 4 , a disulfide claim 4 , a borate ester claim 4 , a borinate ester claim 4 , an aluminate ester claim 4 , a silicate ester claim 4 , a hydrazine claim 4 , an azo moiety claim 4 , a sulfone claim 4 , a phosphate ester claim 4 , and a phosphonate ester.10. The method of wherein X is a non-aromatic linking group that comprises 2-20 carbon atoms.11. The method of wherein X is a non-aromatic linking group that comprises 2-10 carbon atoms.12. The method of wherein Y comprises 1 claim 4 , 2 claim 4 , 3 claim 4 , or 4 alkyne groups.13. The method of wherein Y comprises 1 or 2 alkyne groups.14. The method of wherein Y has only 1 or 2 alkyne group.15. The method of further comprising contacting the polycyclic compound or the cyclic compound with a benzyne ...

Entecavir synthesis method and intermediate compound thereof

The present invention relates to a preparation method for a medicine and an intermediate compound thereof, specifically, relates to a preparation method for entecavir, an intermediate compound thereof, and a synthesis method for the intermediate compound.

Synthesis Of Treprostinil And Intermediates Useful Therein

Treprostinil is prepared by a process which involves Pauson-Khan cyclization of an an alkene-substituted, alkyne-substituted benzene corresponding to formula: (I) where PMB represents para-methoxy benzyl protecting group and Rand Rare alcohol protecting groups. Following cyclization, the resulting compound can be subjected to several chemical trans-formations followed by alkylation, hydrolysis and salt formation to yield treprostinil sodium. The use of para-methoxybenzyl group as the phenolic protecting group confers several process advantages that result in simplified purification of the final product and improved yields. 2. The process of wherein the carbon monoxide for intramolecular cyclization is used in the form of a Group VIII transition metal-carbon monoxide complex3. The process of wherein the carbon monoxide for intramolecular cyclization is used in the form of a cobalt-carbon monoxide complex.6. The process of any preceding claim including the additional claim 1 , subsequent step of removing the p-methoxy benzyl protecting group and the group R.8. The process of including the additional claim 7 , final step of converting the treprostinil so formed to its sodium salt.9. The process of or wherein the alkylation step (j) is conducted using an alkyl bromoalkanoate. This invention relates to a novel synthesis of the prostacyclin derivative treprostinil and intermediates useful in such syntheses.Prostacyclin derivatives are naturally occurring pharmaceutically active compounds, with a variety of pharmacological properties and utilities. A specific example of such prostacyclin derivative is treprostinil, which has the structural formula depicted below:Treprostinil sodium, under the trade name Remodulin is indicated for oral use in management of pulmonary arterial hypertension in human patients. Other salt forms are proposed for administration by inhalation.Treprostinil synthesis has previously been described in U.S. Pat. Nos. 6,700,025; 6,765,117; and 6,809,223; ...

SYNTHESIS OF THIOETHER CONTAINING TRIALKOXYSILANES

The invention relates to a radical-initiated thiol-ene or thiol-yne “click” reaction that provides a simple and efficient route to diverse trialkoxysilanes. Trialkoxysilanes made in this way are obtained in quantitative to near-quantitative yields with high purity without any or minimal purification. A wide range of functional groups is tolerated in this approach, and even complex alkenes click with the silane precursors. The modular nature of these radical-based thiol-ene or thiol-yne “click” reactions allows a wide variety of pendant groups to be coupled to silane compounds that can then be coupled to a wide variety surfaces in order to modify their material properties. Consequently, such radical initiated thiol-ene and thiol-yne reactions provide facile and efficient methods for preparing an enormous number of surface-active functional trialkoxysilanes. 1. A method for making a trialkoxysilane compound comprising a thioether , the method comprising the steps of: a trialkoxysilane compound;', 'a compound comprising a sulfhydryl moiety;', 'an alkene compound or an alkyne compound; and', 'a radical initiator agent;, '(a) forming a mixture comprising the radical initiator agent reacts with a hydrogen atom in a first sulfhydryl moiety so as to form a thiyl radical;', 'the thiyl radical reacts with the alkene or the alkyne so as to form a radical intermediate;', 'the radical intermediate reacts with a hydrogen atom in a second thiol moiety so as to form a thioether;, '(b) initiating a chemical reaction in the mixture so thatso that the trialkoxysilane compound comprising the thioether is made; andthe chemical reaction in (b) produces a composition of matter wherein the trialkoxysilane compound comprising the thioether has a purity of at least 90%.2. The method of claim 1 , wherein:the trialkoxysilane compound comprises the sulfhydryl moiety; orthe trialkoxysilane compound is the alkene compound.3. The method of claim 1 , further comprising placing the composition of ...

ORGANOZINC COMPLEXES AND PROCESSES FOR MAKING AND USING THE SAME

Processes for making an organozinc reagents are disclosed comprising reacting (A) organomagnesium or organozinc complexes with (B) at least one coordination compound comprising one or more carboxylate groups and/or alcoholate groups and/or tertiary amine groups, optionally in combination with zinc ions and/or lithium ions and/or halide ions, wherein the halide ions are selected from chloride, bromide and iodide, the organozinc complex comprises an aryl group, a heteroaryl group or a benzyl group when the coordinating compound is a chelating polyamine, and the reaction is conducted in the presence of zinc complexed with at least one coordinating compound when reactant (A) comprises at least one organomagnesium complex. The resulting organozinc reagents may optionally be isolated from solvents to obtain a solid reagent. The reagents may be used for making organic compounds via Negishi cross-coupling reactions or via aldehyde and/or ketone oxidative addition reactions. The organozinc reagents are stable and, due to their high selectivity, permit maintenance of sensitive functional groups such as aldehydes during cross-coupling. 1. A process for making organozinc reagents comprising:(1) reacting (A) at least one organomagnesium complex or organozinc complex with (B) at least one coordinating compound comprising one or more carboxylate groups and/or alcoholate groups and/or tertiary amine groups, optionally in combination with zinc ions and/or lithium ions and/or halide ions, wherein the halide ions are selected from chloride, bromide and iodide, the organozinc complex comprises an aryl group, a heteroaryl group or a benzyl group when the coordinating compound is a chelating polyamine, and the reaction is conducted in the presence of zinc complexed with at least one coordinating compound when reactant (A) comprises at least one organomagnesium complex,(2) contacting an organic compound having at least one leaving group with magnesium metal and a zinc coordination complex ...

PRODUCTION METHOD FOR ALKOXYSILANES

Provided is a method for efficiently producing alkoxysilanes that are useful as various functional chemicals. In order to produce alkoxysilanes efficiently, an ethoxy- or methoxysilane and an alcohol are caused to react using, as a catalyst, for instance an inorganic solid acid having a regular-pore and/or layered structure. Zeolites, montmorillonites or the like can be used as the inorganic solid acid. When a zeolite is used as the catalyst, the silica/alumina ratio of the zeolite ranges preferably from 5 to 1000. The reaction can be promoted through irradiation of microwaves. 1. A method for producing alkoxysilanes , comprising a reaction step of reacting an alkoxysilane having an ethoxy group or a methoxy group , and an alcohol , in the presence of a catalyst , whereinthe alkoxysilane having an ethoxy group or methoxy group is an alkoxysilane represented by Formula (I);the alcohol is an alcohol represented by Formula (II);the catalyst is a solid acid catalyst; and {'br': None, 'sup': 1', '2', '3', '4, 'sub': p', 'q', 'r', '4−(p+q+r), 'RRRSi(OR)\u2003\u2003(I)'}, 'an alkoxysilane obtained in the reaction step is an alkoxysilane represented by Formula (III){'sup': 1', '2', '3', '4', '1', '2', '3, 'claim-text': {'br': None, 'ROH\u2003\u2003(II)'}, '(In Formula (I), p, q, r and p+q+r are integers ranging from 0 to 3; R, Rand Rare each independently a hydrocarbon group having 1 to 23 carbon atoms, or a hydrogen atom; Ris independently an ethyl group or a methyl group; and in a case where R, Rand Rare hydrocarbon groups, some of the hydrogen atoms of the hydrocarbon groups may be substituted by groups that do not participate in the reaction);'} {'br': None, 'sup': 1', '2', '3', '4, 'sub': p', 'q', 'r', '4−(p+q+r)−m', 'm, 'RRRSi(OR)(OR)\u2003\u2003(III)'}, '(In Formula (II), R is a hydrocarbon group having 1 to 23 carbon atoms, and some of the hydrogen atoms in the hydrocarbon group may be substituted by groups that do not participate in the reaction);'}{'sup': 1', '2', ...

PROCESSES FOR PREPARING JAK INHIBITORS AND RELATED INTERMEDIATE COMPOUNDS

The present invention is related to processes for preparing chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines of Formula III, and related synthetic intermediate compounds. The chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines are useful as inhibitors of the Janus Kinase family of protein tyrosine kinases (JAKs) for treatment of inflammatory diseases, myeloproliferative disorders, and other diseases. 192-. (canceled)97. The process of claim 93 , wherein claim 93 , in step (e):the solvent is 2,2,2-trifluoroethanol (TFE).98105-. (canceled)106. The process of claim 93 , wherein claim 93 , in step (e) claim 93 , the hydrogenation catalyst loading is about 0.005 to about 0.01 mol %.107. The process of claim 93 , wherein claim 93 , in step (e) claim 93 , the ratio of said compound of Formula II to said hydrogenation catalyst is from about 20000/1 to about 10000/1.108. The process of claim 93 , wherein claim 93 , in step (e) claim 93 , the hydrogen pressure is from about 7 to about 60 bar.109. The process of claim 93 , wherein claim 93 , in step (e) claim 93 , the reaction is run at a temperature from about room temperature to about 75° C.110. The process of claim 93 , wherein claim 93 , in step (e) claim 93 , the reaction is run until the conversion of said compound of Formula II′ to said compound of Formula I′ is about equal to or greater than 99.5%.111. The process of claim 93 , wherein claim 93 , in step (e) claim 93 , the reaction is run from about 10 to about 25 hours. This application claims the benefit of U.S. Ser. No. 61/144,991, filed Jan. 15, 2009, the disclosure of which is incorporated herein by reference in its entirety.The present invention is related to processes for preparing chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines and related synthetic intermediate compounds. The chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines are useful as inhibitors of the Janus Kinase family of protein tyrosine kinases (JAKs) for treatment of inflammatory ...

Silanes and Curable Compositions Containing Said Silanes as Crosslinkers

The invention relates to a silane of the formula (1), 2. The silane according to claim 1 , wherein each Rindependently of one another stands for an alkyl group having 1 to 10 carbon atoms claim 1 , or for an alkenyl group having 2 to 10 carbon atoms.3. The silane according to claim 1 , wherein each Rindependently of one another stands for a group of the formula (2) claim 1 , one of the Rgroups stands for hydrogen and the second Rgroup stands for hydrogen or a substituted or unsubstituted alkyl group having 1 to 10 carbon atoms claim 1 , and/or Rstands for a substituted or unsubstituted alkyl group having 1 to 10 carbon atoms.4. The silane according to claim 1 , wherein each Rindependently of one another stands for a group of the formula (2-2) claim 1 , where Rstands for a substituted or unsubstituted alkyl group having 1 to 10 carbon atoms.5. The silane according to claim 1 , wherein each Rindependently of one another stands for a group of the formula (3) claim 1 , one of the Rgroups stands for hydrogen and the second Rgroup stands for hydrogen or a substituted or unsubstituted alkyl group having 1 to 10 carbon atoms.6. The silane according to claim 1 , wherein each Rindependently of one another stands for a group of the formula (3) claim 1 , and Rstands for hydrogen claim 1 , a substituted or unsubstituted alkyl group having 1 to 10 carbon atoms or R.7. The silane according to claim 1 , wherein each Rindependently of one another stands for a group of the formula (3) claim 1 , Rstands for a group of the formula (4) claim 1 , Rstands for an alkylene group of the formula —(CH)— claim 1 , and p is an integer from 1 to 6.8. The silane according to claim 1 , wherein each Rindependently of one another stands for a group of the formula (3) claim 1 , where Rstands for a group of the formula (4) claim 1 , each Rindependently of one another stands for a substituted or unsubstituted alkyl group having 1 to 10 carbon atoms claim 1 , and/or each Rindependently of one another ...

Polysiloxanes comprising methylene-bonded polar groups

Organopolysiloxanes containing a large proportion of methylene-bonded polar groups have high relative permittivities, and are especially useful as thermally stable dielectrics. A methoxymethyl alkoxysilane starting material is easily synthesized, and can be incorporated into the polymers by conventional methods known in organosilicon chemistry.

METAL-CATALYZED ASYMMETRIC 1,4-CONJUGATE ADDITION OF VINYLBORON COMPOUNDS TO 2-SUBSTITUTED-4-OXY-CYCLOPENT-2-EN-1-ONES YIELDING PROSTAGLANDINS AND PROSTAGLANDIN ANALOGS

This invention provides a novel method for the preparation of 2,3-disubstituted-4-oxy-cyclopentan-1-one compounds that are useful for the synthesis of prostaglandins and prostaglandin analogs of industrial relevance. The method comprises the metal-catalyzed asymmetric 1,4-conjugate addition of vinylboron compounds to 2-substituted-4-oxy-cyclopent-2-en-1-ones. This method relies on the use of less toxic, easily-handled reagents, and can be performed under milder conditions than offered by some conventional methods, affording 2,3-disubstituted-4-oxy-cyclopentan-1-one compounds enantio- and diastereoselectively, which are precursors to the said prostaglandin and prostaglandin analogs, in high yield. 3. The process of claim 1 , wherein Ris alkyl claim 1 , aryl claim 1 , arylalkyl or aryloxyalkyl claim 1 , each of which is optionally substituted with from one to three members selected from the group consisting of Calkyl claim 1 , Calkoxy claim 1 , silyloxy claim 1 , aryloxy claim 1 , acyloxy claim 1 , tetrahydropyranyl (THP) claim 1 , trifluoromethyl and fluoro.4. The process of claim 1 , wherein the solvent is selected from the group consisting of water claim 1 , methanol claim 1 , ethanol claim 1 , isopropyl alcohol claim 1 , isobutyl alcohol claim 1 , 1 claim 1 ,4-dioxane claim 1 , toluene claim 1 , tetrahydrofuran (THF) claim 1 , 2-methyl-tetrahydrofuran (2-Me-THF) claim 1 , diglyme claim 1 , acetonitrile claim 1 , N-methylpyrrolidone claim 1 , N claim 1 ,N-dimethylformamide (DMF) claim 1 , N claim 1 ,N-dimethylacetamide (DMAC) claim 1 , ethylene glycol and combinations thereof.5. The process of claim 4 , wherein the solvent is methanol.6. The process of claim 1 , wherein the metal additive is selected from the group consisting of rhodium compounds claim 1 , cobalt compounds claim 1 , nickel compounds and combinations thereof.7. The process of claim 6 , wherein the rhodium compound is a rhodium(I) compound selected from the group consisting of [RhCl(1 claim 6 ,5- ...

BENZYL COMPOUND

The purpose of the present invention is to provide a protecting group which improves the solubility of a compound having a functional group protected with the protecting group in an organic solvent and which is easily separated and purified after a reaction with avoiding solidification or insolubilization. Provided is a benzyl compound represented by Formula (1) where Xrepresents —CHOR(where Rrepresents a hydrogen atom, a halogenocarbonyl group, or an active ester-type protecting group), —CHNHR(where Rrepresents a hydrogen atom, a linear or branched alkyl group having 1 to 6 carbon atoms, or an aralkyl group), a halogenomethyl group, a methyl azide group, a formyl group, or an oxime; and at least one of R, R, R, R, and Ris a group represented by Formula (2), and the remainders each represent a hydrogen atom, a halogen atom, an alkyl group having 1 to 4 carbon atoms, or an alkoxy group having 1 to 4 carbon atoms, where Rrepresents a linear or branched alkylene group having 1 to 16 carbon atoms; Xrepresents O or CONR(where Rrepresents a hydrogen atom or an alkyl group having 1 to 4 carbon atoms); and A represents a group represented by Formula (3), (4), (5), (6), (7), (8), (9), (10), (11), (12), or (13). 2: The method according to claim 1 , wherein the compound having the functional group is amino acid or peptide.3: The method according to claim 1 , wherein Xis —CHOR(where Rrepresents a hydrogen atom claim 1 , a halogenocarbonyl group claim 1 , or an active ester-type protecting group) claim 1 , —CHNHR(where Rrepresents a hydrogen atom claim 1 , a liner or branched alkyl group having 1 to 6 carbon atoms claim 1 , or an aralkyl group) claim 1 , or a halogenomethyl group.4: The method according to claim 1 , wherein R represents a linear or branched alkylene group having 2 to 16 carbon atoms.5: The method according to claim 1 , wherein Ris a single bond or a methylene group; and R claim 1 , R claim 1 , and Rare methylene groups.7: The peptide producing method according ...

Polymer Materials With Silane-Based Transfer Reagents

Radically polymerizable silane according to the general formula I 2. Radically polymerizable silane according to claim 1 , wherein{'sup': '1', 'sub': 3', '2', '5, 'Ris —CH, —CH, phenyl or tolyl,'}{'sup': 2', '3, 'sub': 1', '10, 'R, Rindependently of each other in each case are absent or are a linear aliphatic C-C-alkylene radical, which can be interrupted by O atoms,'}{'sup': 4', '5', '6, 'sub': 3', '2', '5, 'R, R, Rindependently of each other in each case are —O—CHor —O—CH,'}{'sub': '2', 'X is CHor O,'}Y is absent or is O, andZ is absent, or is O, —CO—O—, —CO—NH—, —O—CO—O— or —O— CO—NH—.3. Radically polymerizable silane according to claim 1 , wherein{'sup': '1', 'sub': 3', '2', '5, 'Ris —CH, —CH, phenyl or tolyl,'}{'sup': '2', 'sub': 2', '8, 'Ris a linear aliphatic C-C-alkylene radical, which can be interrupted by O atoms,'}{'sup': '3', 'sub': 1', '6, 'Ris absent or is a linear aliphatic C-C-alkylene radical,'}{'sup': 4', '5', '6, 'sub': 3', '2', '5, 'R, R, Rindependently of each other in each case are —O—CHor —O—CH,'}{'sub': '2', 'X is CHor O,'}Y is O, andZ is absent, or is —CO—NH— or —O—CO—NH—.4. Process for the production of polysiloxane condensates claim 1 , in which at least one silane according to is mixed with a stoichiometric amount or an excess of water and the mixture is then allowed to react.5. Process according to claim 4 , in which the silane is dissolved in an organic solvent claim 4 , the solution is then mixed with water or a mixture of water and an organic solvent claim 4 , the mixture is then allowed to react at a temperature in the range of from 0° C. to 140° C. and the solvent and volatile components are subsequently removed.6. Process according to claim 4 , in which the mixture is additionally mixed with a catalyst.7. Process according to claim 6 , in which the catalyst comprises an acid selected from acetic acid or hydrochloric acid or a base selected from ammonia claim 6 , amine claim 6 , NaOH claim 6 , methylimidazole claim 6 , or ammonium ...

TETRACARBOXYLIC ACID DIESTER COMPOUND, POLYMER OF POLYIMIDE PRECURSOR AND METHOD FOR PRODUCING SAME, NEGATIVE PHOTOSENSITIVE RESIN COMPOSITION, PATTERNING PROCESS, AND METHOD FOR FORMING CURED FILM

A polymer of a polyimide precursor which includes a structural unit represented by the following general formula (7), 5. A negative photosensitive resin composition which comprises{'claim-ref': {'@idref': 'CLM-00002', 'claim 2'}, '(A) the polymer of a polyimide precursor according to ,'}(B) a photo-radical initiator, and(D) a solvent.6. A negative photosensitive resin composition which comprises{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '(A′) the polymer of a polyimide precursor according to ,'}(B) a photo-radical initiator,(C) a crosslinking agent having two or more photopolymerizable unsaturated bonding group in one molecule, and(D) a solvent.7. A negative photosensitive resin composition which comprises{'claim-ref': {'@idref': 'CLM-00002', 'claim 2'}, '(A′) the polymer of a polyimide precursor according to ,'}(B) a photo-radical initiator,(C) a crosslinking agent having two or more photopolymerizable unsaturated bonding group in one molecule, and(D) a solvent.10. A patterning process which comprises{'claim-ref': {'@idref': 'CLM-00005', 'claim 5'}, '(1) coating the negative photosensitive resin composition according to onto a substrate to form a film of a photosensitive material, then,'}(2) after heat treatment, exposing the film of a photosensitive material by a high energy beam having a wavelength of 190 to 500 nm or an electron beam through a photomask, and(3) developing the film by using a developer of an organic solvent.11. The patterning process according to claim 10 , further comprising a post-exposure bake step between the exposing step and the developing step.12. A method for forming a cured film which comprises heating and post-curing a pattern-formed film obtained by the patterning process according to at a temperature of 100 to 300° C. This is a Divisional of application Ser. No. 15/705,842 filed Sep. 15, 2017. The entire disclosure of the prior application is hereby incorporated by reference herein its entirety.The present invention relates to ...

A VOC-free, aqueous and storage-stable N-vinylbenzylaminoalkyl-functional siloxanol and process for the production thereof

An aqueous, storage-stable and preferably colorless composition containing N-vinylbenzylaminoalkyl-functional siloxanols is derived from a reaction of hydrolysis products and optionally, condensation products of hydrolysis products, of at least one aminoalkyl-functional alkoxysilane or a mixture of aminoalkyl-functional alkoxysilanes with vinylbenzyl halide. The composition contains not less than 1% by weight of N-vinylbenzylaminoalkyl-functional siloxanols and/or salts of the protonated N-vinylbenzylaminoalkyl-functional siloxanols and water, based on the weight of the composition. The composition has a pH of 2 to 3.5. A process can be used for producing this composition. 1: An aqueous composition comprising N-vinylbenzylaminoalkyl-functional siloxanols and , optionally , salts of the protonated N-vinylbenzylaminoalkyl-functional siloxanols which are derived from a reactionof hydrolysis products and, optionally, condensation products of hydrolysis products, of at least one aminoalkyl-functional alkoxysilane or a mixture of aminoalkyl-functional alkoxysilanes with vinylbenzyl halide,wherein the composition comprises1% to 70% by weight of the N-vinylbenzylaminoalkyl-functional siloxanols and/or the salts of the protonated N-vinylbenzylaminoalkyl-functional siloxanols, and30% to 99% by weight of water, based on a total weight of the composition; andwherein the composition has an acidic pH.2: The composition according to claim 1 , wherein the compositionhas a pH of less than 7.0, and/orcontains not less than 0.1% by weight of acid selected from the group consisting of inorganic acid, organic acid, and a mixture thereof.3: The composition according to claim 2 , wherein the acid is selected from the group consisting of hydrochloric acid claim 2 , formic acid claim 2 , acetic acid claim 2 , oxalic acid claim 2 , and fumaric acid.4: The composition according to claim 1 , wherein a weight average molecular weight (Mw) of the N-vinylbenzylaminoalkyl-functional siloxanols and ...

Preparation of a cured polymer comprising urethane groups and silicon atoms

A process prepares a cross-linked polymer containing urethane groups and silicon atoms. Starting materials of the process include a compound A) with a five-membered cyclic monothiocarbonate group, a compound B) with an amino group, selected from primary or secondary amino groups or blocked amino groups, and optionally, a compound C) with at least one functional group that reacts with a group —SH. One of the compounds contains a silicon-functional group. In one example of the process, compounds A) and B), and optionally C), are then reacted under exclusion of water to obtain a polymer with curable silicon-functional groups. The polymer is applied to a surface, gap, or a three-dimensional template. The silicon-functional groups are cured with ambient water. The polymer contains 0.001 to 0.3 mol of silicon per 100 g of the polymer.

One-component sealant or adhesive composition

A process prepares a prepolymer containing a urethane group and a curable silicon-functional group, or a prepolymer of formula (IV), 1: A process for preparing a prepolymer comprising a urethane group and a curable silicon-functional group , the process comprising:reacting a compound A) with a compound B), and optionally a compound C), under exclusion of water, to obtain the prepolymer comprising the urethane group and the curable silicon-functional group,wherein the compound A) comprises at least one five-membered cyclic monothiocarbonate group, andwherein the compound B) comprises at least one amino group, selected from the group consisting of primary amino groups, secondary amino groups, blocked primary amino groups, and blocked secondary amino groups, andwherein the compound C), if present, comprises at least one functional group that reacts with a group —SH,wherein at least one of the compounds A), B), and optionally C) comprises a silicon-functional group.3: The process according to claim 1 , wherein the compound B) comprises one to five amino groups.4: The process according to claim 1 , wherein the at least one functional group of compound C) that reacts with —SH is a non-aromatic claim 1 , ethylenically unsaturated group.5: The process according to claim 1 , wherein the compound B) or compound C) claim 1 , if present claim 1 , comprises the silicon-functional group.6: The process according to claim 1 , wherein the silicon-functional group is an alkoxysilane group of formula (III) claim 1 ,{'br': None, 'sup': 1s', '2s', '3s, '—SiRRR'}{'sup': 1s', '3s', '1s', '3s, 'wherein two or three of the groups Rto Rare an alkoxy group, and the remaining group Rto Ris an alkyl or alkylene-vinyl group.'}7: The process according to claim 1 , wherein at least one of the compounds A) claim 1 , B) claim 1 , or optionally C) comprises a segment selected from the group consisting of a polyether group and an organic polysulfide group.8: The process according to claim 1 , wherein ...

MODIFIER, METHOD OF PREPARING THE SAME, AND MODIFIED CONJUGATED DIENE-BASED POLYMER INCLUDING THE SAME

The present invention relates to a modifier, and more particularly, to a modifier including a compound represented by Formula 1, a method of preparing the same, and a modified conjugated diene-based polymer including the same. 2. The modifier of claim 1 , wherein claim 1 , in Formula 1 claim 1 , Ris a substituted or unsubstituted C-Calkyl group claim 1 , a substituted or unsubstituted C-Calkenyl group claim 1 , a substituted or unsubstituted C-Calkynyl group claim 1 , a substituted or unsubstituted C-Cheteroalkyl group claim 1 , a substituted or unsubstituted C-Ccycloalkyl group claim 1 , a substituted or unsubstituted C-Caryl group claim 1 , or a substituted or unsubstituted C-Cheterocyclic group claim 1 ,{'sup': '2', 'Ris the functional group of Formula 1a,'}{'sup': '3', 'Ris the functional group of Formula 1b,'}{'sup': '1', 'sub': 1', '30', '1', '30', '2', '30', '2', '30', '1', '30', '1', '30', '5', '30', '6', '30', '3', '30, 'wherein, when Ris the substituted alkyl group, the substituted alkenyl group, the substituted alkynyl group, the substituted heteroalkyl group, the substituted cycloalkyl group, the substituted aryl group, or the substituted heterocyclic group, a substituent of the substituted alkyl group, the substituted alkenyl group, the substituted alkynyl group, the substituted heteroalkyl group, the substituted cycloalkyl group, the substituted aryl group, or the substituted heterocyclic group comprises one or more selected from the group consisting of deuterium, a halogen, a hydroxyl group, a nitro group, a cyano group, a C-Calkyl group, a C-Calkylsilyl group, a C-Calkenyl group, a C-Calkynyl group, a C-Calkoxy group, a substituted or unsubstituted C-Cheteroalkyl group, a C-Ccycloalkyl group, a C-Caryl group, and a C-Cheterocyclic group, and'}X is one heteroatom selected from the group consisting of N, O, and S,{'sup': 2', '3, 'wherein, when X is O or S, only one of the Rand Rfunctional groups is present, and, in Formulae 1a and 1b,'}{'sup': 4', '7, ...

BENZYL COMPOUND

The purpose of the present invention is to provide a protecting group which improves the solubility of a compound having a functional group protected with the protecting group in an organic solvent and which is easily separated and purified after a reaction with avoiding solidification or insolubilization. Provided is a benzyl compound represented by Formula (1) where Xrepresents —CHOR(where Rrepresents a hydrogen atom, a halogenocarbonyl group, or an active ester-type protecting group), —CHNHR(where Rrepresents a hydrogen atom, a linear or branched alkyl group having 1 to 6 carbon atoms, or an aralkyl group), a halogenomethyl group, a methyl azide group, a formyl group, or an oxime; and at least one of R, R, R, R, and Ris a group represented by Formula (2), and the remainders each represent a hydrogen atom, a halogen atom, an alkyl group having 1 to 4 carbon atoms, or an alkoxy group having 1 to 4 carbon atoms, where Rrepresents a linear or branched alkylene group having 1 to 16 carbon atoms; Xrepresents O or CONR(where Rrepresents a hydrogen atom or an alkyl group having 1 to 4 carbon atoms); and A represents a group represented by Formula (3), (4), (5), (6), (7), (8), (9), (10), (11), (12), or (13). 2: The benzyl compound according to claim 1 , wherein Xis —CHORwhere Rrepresents a hydrogen atom claim 1 , a halogenocarbonyl group claim 1 , or an active ester-type protecting group claim 1 , —CHNHRwhere Rrepresents a hydrogen atom claim 1 , a linear or branched alkyl group having 1 to 6 carbon atoms claim 1 , or an aralkyl group claim 1 , or a halogenomethyl group.3: The benzyl compound according to claim 1 , wherein Ris a linear or branched alkylene group having 2 to 16 carbon atoms.4: The benzyl compound according to claim 1 , wherein Ris a linear or branched alkylene group having 6 to 16 carbon atoms.5: The benzyl compound according to claim 1 , wherein Ris a single bond or a methylene group; and R claim 1 , R claim 1 , and Rare methylene groups.6: A method claim ...

METHOD FOR PREPARING 3-((2S, 5S)-4-METHYLENE-5-(3-OXOPROPYL)TETRAHYDROFURANE-2-YL) PROPANOL DERIVATIVE, AND INTERMEDIATE THEREFOR

A method for preparing a 3-((2S,5S)-4-methylene-5-(3-oxopropyl)tetrahydrofuran-2-yl)propanol derivative by a simple process with high yields, and an intermediate useful for the method. 2. The process according to claim 1 , whereinR is p-toluenesulfonyl, andPG is t-butyldiphenylsilyl.3. The process according to claim 1 , whereinthe reaction of step (i) is performed in the presence of sodium bis(trimethylsilyl)amide and n-tetrabutylammonium iodide.4. The process according to claim 1 , whereinthe reaction of step (ii) is performed in the presence of n-butyl lithium.5. The process according to claim 1 , whereinthe denitrification and rearrangement of step (iii) are performed in the presence of a rhodium catalyst.6. The process according to claim 1 , wherein{'sub': 2', '3, 'the hydrolysis of step (iii) is performed in the presence of alumina (AlO).'}8. The compound according to claim 7 , whereinR is p-toluenesulfonyl, andPG is t-butyldiphenylsilyl.10. The process according to claim 9 , whereinR is p-toluenesulfonyl, andPG is t-butyldiphenylsilyl.12. The process according to claim 11 , whereinR is p-toluenesulfonyl, andPG is t-butyldiphenylsilyl. The present invention relates to a process for preparing a 3-((2S,5S)-4-methylene-5-(3-oxopropyl)tetrahydrofuran-2-yl)propanol derivative and an intermediate therefor. More particularly, the present invention relates to a process for preparing a 3-((2S,5S)-4-methylene-5-(3-oxopropyl)tetrahydrofuran-2-yl)propanol derivative by a simple process with high yields, and an intermediate therefor.3-((2S,5S)-4-methylene-5-(3-oxopropyl)tetrahydrofuran-2-yl)propanol derivatives have the structure of the following formula (1), and have been effectively used as intermediates for C14-C23 moiety in the preparation of Halichondrin B of the following formula (2) and Eribulin mesylate of the following formula (3) having anti-cancer activity[see U.S. Pat. No. 5,436,238 and Korean Patent No. 10-1434673].For the preparation of the 3-((2S,5S)-4- ...

Synthesis of Thapsigargin, Nortrilobolide, and Analogs Thereof

The present invention relates to the preparation of compounds of Formula I, including thapsigargin, nortrilobolide and 8-O-debutanoyl-thapsigargin from commercially available (R)-(−)-carvone via synthetic intermediate compound of formula 12 by pinacol coupling and in situ lactonization. 6. The method of claim 1 , wherein the reactant is (R)-(−)-carvone (10).23. The method of claim 1 , further comprising attaching a polypeptide or a linker suitable for attachment of an antibody. This application claims the benefit of the filing date of U.S. Provisional Patent Application No. 62/477,118, filed on Mar. 27, 2017, the contents of which are incorporated herein by reference in their entirety.The field pertains to synthesis of natural products. Specifically, the field is the synthesis of a particular family of terpenes, known as the thapsigargins, which are sesquiterpene lactonesTerpenes are a large and diverse class of natural products, which are produced by a variety of plants (e.g., conifers), and by some insects (e.g., termites, swallowtail butterflies). Their diversity stems from structural and stereochemical diversity. Of these, a particular terpene compound, thapsigargin (1), was first isolated from Mediterranean plant L. in 1978 (Rasmussen U. at al. 1978, 15:133-140). This compound, together with structurally-related guaianolides, are collectively known as a family of compounds termed “thapsigargins”. For example, nortrilobolide (3), which only differs from thapsigargin (1) at C-2 position, was isolated from the plant L by Christensen in 1991 (U. W. Smitt, at al., 1991, 57: 196-197). Terpenes have played significant roles as pesticides in agriculture, as fragrances in cosmetics, and as chemotherapeutic agents in human disease therapy and prevention. Their use has been restricted by limited natural sources, low natural abundance, and difficulties associated with their chemical syntheses on a preparative scale.In one aspect, the invention provides a method for ...

TRIAZOLE SILANE COMPOUND, METHOD FOR SYNTHESIZING SAID COMPOUND AND USE THEREOF

The abstract of the international application is being replace by the following abstract: The purpose of the present invention is to provide: a novel triazole silane compound and a method for synthesizing the same, and a silane coupling agent containing the triazole silane compound as a component; and a surface treatment solution, a surface treatment method, and a method for bonding two different materials, which use said triazole silane compound. 5. The surface treatment solution according to claim 4 , which is used for treating a surface of at least one material selected from the group consisting of a metal claim 4 , an inorganic material and a resin material.6. The surface treatment solution according to claim 4 , which is used for bonding two materials selected from the group consisting of a metal claim 4 , an inorganic material and a resin material.711-. (canceled)12. A surface treatment method of metal claim 4 , comprising bringing the surface treatment solution described in into contact with a surface of a metal.1314-. (canceled)15. The surface treatment method of metal according to claim 12 ,wherein the metal is copper or a copper alloy, andthe method comprises, before bringing the surface treatment solution into contact with a surface of copper or a copper alloy, bringing an aqueous solution containing a copper ion into contact with the surface of the copper or the copper alloy.16. The surface treatment method of metal according to claim 12 ,wherein the metal is copper or a copper alloy, andthe method comprises, after bringing the surface treatment solution into contact with a surface of copper or a copper alloy, bringing an aqueous acidic solution or an aqueous alkaline solution into contact with the surface of the copper or the copper alloy.17. A surface treatment method of an inorganic material claim 4 , comprising bringing the surface treatment solution described in into contact with a surface of an inorganic material.1819-. (canceled)20. A surface ...

SILICON COMPOUND AND METHOD FOR PRODUCING SAME, AND USE THEREOF

A novel silicon compound capable of initiating radical polymerization is provided. The silicon compound is represented by the following general formula (1) 6. The method according to claim 4 , wherein the compound represented by the general formula (6) and the compound represented by the general formula (7) are reacted with each other by using a radical generating agent as a reaction catalyst.7. A radical polymerization initiator that comprises the silicon compound of .8. A method for producing a polymer claim 7 , the method comprising subjecting a monomer to radical polymerization or living radical polymerization with the radical polymerization initiator of .9. A polymer having a terminal alkoxysilyl group and obtained by using the method of .11. A rubber composition comprising the polymer of in 0.1 to 100 parts by mass with respect to 100 parts by mass of a rubber component.12. A method for producing a complex claim 1 , the method comprising fixing the silicon compound of to a surface of a solid substance claim 1 , and polymerizing a monomer from the fixed silicon compound through living radical polymerization to form a polymer graft chain.13. The method for producing a complex according to claim 12 , wherein the solid substance is at least one selected from the group consisting of a silica fine particle claim 12 , a zinc oxide fine particle claim 12 , a titanium oxide fine particle claim 12 , and a barium titanate fine particle.14. The method for producing a complex according to claim 12 , wherein the monomer is at least one selected from the group consisting of a vinyl monomer and a diene monomer.15. The method for producing a complex according to claim 12 , wherein the amount of the polymer graft chain formed by living radical polymerization of the monomer is 5 to 1 claim 12 ,000 parts by mass with respect to 100 parts by mass of the solid substance.16. A complex obtained by using the method of .17. A molded article that comprises the complex of .18. A method ...

COMPOUNDS, DEVICES, AND USES THEREOF

The present invention provides compounds, e.g., compounds of Formula (I) and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are implantable elements (e.g., devices and materials) comprising the same, as well as methods of use thereof, e.g., for treating or preventing a disease, disorder, or condition. 2. The compound of claim 1 , wherein Mis aryl (e.g. claim 1 , phenyl).4. The compound of any one of the preceding claims claim 1 , wherein each of R claim 1 , R claim 1 , R claim 1 , and Ris independently hydrogen or alkyl or one of Rand Ror Rand Rare taken together to form an oxo group.5. The compound of claim 4 , wherein each of R claim 4 , R claim 4 , R claim 4 , and Ris independently hydrogen.6. The compound of any one of the preceding claims claim 4 , wherein each of m and n is 1.7. The compound of any one of the preceding claims claim 4 , wherein X is absent or O.8. The compound of any one of the preceding claims claim 4 , wherein Z is heterocyclyl (e.g. claim 4 , 6-membered heterocyclyl).9. The compound of claim 8 , wherein Z is a nitrogen-containing heterocyclyl claim 8 , an oxygen-containing heterocyclyl claim 8 , or a sulfur-containing heterocyclyl (e.g. claim 8 , oxetanyl claim 8 , tetrahydrofuranyl claim 8 , tetrahydropyranyl claim 8 , thiomorpholinyl-1 claim 8 ,1-dioxide claim 8 , piperidinyl claim 8 , piperazinyl claim 8 , or pyrrolidinyl).10. The compound of any one of - claim 8 , wherein Z is aryl (e.g. claim 8 , phenyl).11. The compound of claim 10 , wherein Z is monosubstituted phenyl (e.g. claim 10 , with 1 R).12. The compound of claim 10 , wherein Z is monosubstituted phenyl claim 10 , wherein the 1 Ran amine-containing group (e.g. claim 10 , NH) or an oxygen-containing group (e.g. claim 10 , OCH).13. The compound of any one of - claim 10 , wherein the 1 Ris in the ortho position or the para position.16. The compound of any one of - claim 10 , ...

PROCESSES FOR PREPARING TUBULYSIN DERIVATIVES AND CONJUGATES THEREOF

The invention described herein pertains to processes for preparing tubulysin derivatives, conjugates of tubulysins, and intermediates therefore. In one illustrative embodiment of the invention, processes for derivatives or analogs of natural tubulysins including compounds of formula (T). In another embodiment, vitamin receptor binding conjugates of tubulysins are described. The processes include one or more steps described herein. In another embodiment, a process is described for preparing a compound of formula B, wherein R5 and R6 are as described in the various embodiments herein, such as each being independently selected from optionally substituted alkyl or optionally substituted cycloalkyl; and R8 is C1-C6 n-alkyl; wherein the process comprises the step of treating a compound of formula A with a silylating agent, such as triethylsilyl chloride, and a base, such as imidazole in an aprotic solvent. 811-. (canceled)12. The process of wherein Y is RC(O)O claim 1 , where Ris selected from the group consisting of optionally substituted alkyl and optionally substituted cycloalkyl.13. (canceled)14. The process of wherein Ris n-butyl.15. (canceled)16. The process of wherein Ris methyl.17. (canceled)18. (canceled)19. The process of wherein Aris 4-hydroxyphenyl.20. (canceled)21. The process of wherein Ris methyl.22. (canceled)23. The process of wherein Ris iso-propyl.2426-. (canceled)27. The process of wherein Ris methyl.2830-. (canceled)31. The process of wherein Aris 3-nitro-2-pyridyl.3236-. (canceled)37. The process of wherein L is —(CR)CRR—.38. The process of wherein p is 1.3941-. (canceled)4346-. (canceled)47. The compound of wherein Aris 3-nitro-2-pyridyl.48. The compound of wherein Aris 4-substituted phenyl. The present application claims the benefit under 35 U.S.C. §119(e) of U.S. Provisional Application No. 61/617,386, filed Mar. 29, 2012, U.S. Provisional Application No. 61/684,450, filed Aug. 17, 2012, U.S. Provisional Application No. 61/771,451, filed Mar. 1, ...

MACROLIDES AND METHODS OF THEIR PREPARATION AND USE

Provided herein are methods of preparing macrolides by the coupling of an eastern and western half, followed by macrocyclization, to provide macrolides, including both known and novel macrolides. Intermediates in the synthesis of macrolides including the eastern and western halves are also provided. Pharmaceutical compositions and methods of treating infectious diseases and inflammatory conditions using the inventive macrolides are also provided. A general diastereoselective aldol methodology used in the synthesis of the western half is further provided. 922-. (canceled)23. The compound of claim 1 , wherein each instance of Rand Ris independently hydrogen claim 1 , optionally substituted alkyl claim 1 , or halogen.2425-. (canceled)26. The compound of claim 1 , wherein Ris optionally substituted alkyl claim 1 , optionally substituted alkenyl claim 1 , optionally substituted aralkyl claim 1 , or optionally substituted heteroaralkyl.2732-. (canceled)33. The compound of claim 1 , wherein Ris optionally substituted alkyl.34. (canceled)35. The compound of claim 1 , wherein Ris optionally substituted alkyl.3637-. (canceled)3955-. (canceled)57. (canceled)58. The compound of claim 1 , wherein the compound is selected from any one of the compounds listed in Tables A claim 1 , B claim 1 , C claim 1 , D claim 1 , E claim 1 , F claim 1 , G claim 1 , H claim 1 , I claim 1 , J claim 1 , K claim 1 , L or salt thereof.59. A pharmaceutical composition comprising a macrolide of claim 1 , or pharmaceutically acceptable salt thereof claim 1 , and a pharmaceutically acceptable excipient.60. A method of treating an infectious disease comprising administering an effective amount of a macrolide of claim 1 , or pharmaceutically acceptable salt thereof claim 1 , to a subject in need thereof.61. The method of claim 60 , wherein the infectious disease is a bacterial infection.6267-. (canceled)7075-. (canceled)7779-. (canceled) The present application claims priority under 35 U.S.C. §119(e) to U ...

ORGANOSILANE TEMPLATES AND METHODS FOR THE SYNTHESIS OF MESOPOROUS ZEOLITES

Methods of forming mesoporous zeolites with tunable pore widths are provided. In some embodiments, the method includes mixing a silicon-containing material, an aluminum-containing material, and at least a quaternary amine to produce a zeolite precursor solution. The zeolite precursor solution is pre-crystallized at a pre-crystallization temperature of greater than 125° C. and autogenous pressure to form a pre-crystallized zeolite precursor solution and combined with an organosilane mesopore template to produce a zeolite precursor gel. The zeolite precursor gel is crystallized without a previous discrete functionalization step to produce a crystalline zeolite intermediate and the crystalline zeolite intermediate is calcined to produce the mesoporous zeolite. An organosilane mesopore template in accordance with 1. A method of forming mesoporous zeolites with tunable physical properties , the method comprising:mixing a silicon-containing material, an aluminum-containing material, and at least a quaternary amine to produce a zeolite precursor solution;pre-crystallizing the zeolite precursor solution at a pre-crystallization temperature of greater than 125° C. and autogenous pressure to form a pre-crystallized zeolite precursor solution represented by the formation of an amorphous phase in pseudo-steady-state where solid and solution phases approach equilibrium and silicate and aluminosilicate anion distributions are established;combining an organosilane mesopore template with the pre-crystallized zeolite precursor solution to produce a zeolite precursor gel;crystallizing the zeolite precursor gel to produce a crystalline zeolite intermediate; andcalcining the crystalline zeolite intermediate to produce the mesoporous zeolite,wherein the method does not comprise a discrete functionalization step of the zeolite precursor gel before crystallizing the zeolite precursor gel.2. The method of claim 1 , wherein the crystalline zeolite intermediate is calcined by exposure to a ...

SILICON COMPOUNDS AND METHODS FOR DEPOSITING FILMS USING SAME

A composition, and chemical vapor deposition method, is provided for producing a dielectric film. A gaseous reagent including the composition is introduced into the reaction chamber in which a substrate is provided. The gaseous reagent includes a silicon precursor that includes a silicon compound according to Formula I as defined herein. Energy is applied to the gaseous reagents in the reaction chamber to induce reaction of the gaseous reagents and to thereby deposit a film on the substrate. The film as deposited is suitable for its intended use without an optional additional cure step applied to the as-deposited film. A method for making the composition is also disclosed. 2. The method of wherein the silicon precursor further comprises a hardening additive.3. The method of wherein the silicon compound comprises at least one selected from the group consisting of 2 claim 1 ,2 claim 1 ,5 claim 1 ,5-tetramethyl-1-oxa-2-silacyclopentane claim 1 , 2 claim 1 ,5 claim 1 ,5-trimethyl-2-ethoxy-1-oxa-2-silacyclopentane claim 1 , 2 claim 1 ,5 claim 1 ,5-trimethyl-2-methoxy-1-oxa-2-silacyclopentane claim 1 , 2 claim 1 ,5 claim 1 ,5-trimethyl-2-iso-propoxy-1-oxa-2-silacyclopentane claim 1 , 2 claim 1 ,2-dimethyl-1-oxa-2-silacyclohexane claim 1 , 2 claim 1 ,2 claim 1 ,6 claim 1 ,6-tetramethyl-1-oxa-2-silacyclohexane claim 1 , 2-methyl-2-ethoxy-1-oxa-2-silacyclohexane claim 1 , 2 claim 1 ,6 claim 1 ,6-trimethyl-2-ethoxy-1-oxa-2-silacyclohexane claim 1 , 2-methyl-2-methoxy-1-oxa-2-silacyclohexane claim 1 , 2 claim 1 ,6 claim 1 ,6-trimethyl-2-methoxy-1-oxa-2-silacyclohexane claim 1 , 2-methyl-2-n-propoxy-1-oxa-2-silacyclohexane claim 1 , 2 claim 1 ,6 claim 1 ,6-trimethyl-2-n-propoxy-1-oxa-2-silacyclohexane claim 1 , 2-methyl-2-iso-propoxy-1-oxa-2-silacyclohexane claim 1 , 2 claim 1 ,6 claim 1 ,6-trimethyl-2-iso-propoxy-1-oxa-2-silacyclohexane claim 1 , 2 claim 1 ,5 claim 1 ,5-trimethyl-2-iso-propyl-1-oxa-2-silacyclopentane claim 1 , 2-methyl-2-iso-propyl-1-oxa-2-silacyclopentane ...

SILANE-MODIFIED DIALLYL BISPHENOL COMPOUND AND PREPARATION METHOD THEREOF

A silane-modified diallyl bisphenol compound and a preparation method thereof are provided. A diallyl bisphenol compound with hydroxyl groups at both ends and a silane with at least one alkoxy group and at least one functional group having a crosslinkable double bond at the ends are reacted, so as to obtain a silane-modified diallyl bisphenol compound with a functional group having a crosslinkable double bond at the end. 2. The silane-modified diallyl bisphenol compound of claim 1 , wherein the functional group having the crosslinkable double bond comprises an allyl group claim 1 , a vinyl group claim 1 , an acrylate claim 1 , or a methacrylate.3. The silane-modified diallyl bisphenol compound of claim 1 , wherein n+m is 2 or 3.5. The silane-modified diallyl bisphenol compound of claim 4 , wherein the functional group having the crosslinkable double bond comprises an allyl group claim 4 , a vinyl group claim 4 , an acrylate claim 4 , or a methacrylate.7. The preparation method of the silane-modified diallyl bisphenol compound of claim 6 , wherein the functional group having the crosslinkable double bond comprises an allyl group claim 6 , a vinyl group claim 6 , an acrylate claim 6 , or a methacrylate.8. The preparation method of the silane-modified diallyl bisphenol compound of claim 6 , wherein n+m is 2 or 3.9. The preparation method of the silane-modified diallyl bisphenol compound of claim 6 , wherein a reaction temperature of reaction formula (1) is 100° C. to 180° C.10. The preparation method of the silane-modified diallyl bisphenol compound of claim 6 , wherein calculated based on a mole ratio of a hydroxyl group of a diallyl bisphenol compound to an alkoxy group containing a dialkoxysilane with a functional group having a crosslinkable double bond claim 6 , a ratio of the diallyl bisphenol compound to the dialkoxysilane with the functional group having the crosslinkable double bond is 1:0.5 to 1:4.0.11. The preparation method of the silane-modified diallyl ...

Surfactant-Enabled Transition Metal-Catalyzed Chemistry

In one embodiment, the present application discloses mixtures comprising (a) water in an amount of at least 1% wt/wt of the mixture; (b) a transition metal catalyst; and (c) one or more solubilizing agents; and methods for using such mixtures for performing transition metal mediated bond formation reactions. 114.-. (canceled)16. The method of claim 15 , wherein the transition metal mediated bond formation is performed in an aqueous solvent.17. The method of claim 15 , wherein the transition metal catalyst is selected from an organo-palladium or -nickel reagent claim 15 , organo-copper or -gold reagent claim 15 , organo-rhodium or -iridium complex claim 15 , or an organo-ruthenium claim 15 , -iron claim 15 , or -osmium reagent claim 15 , wherein the catalyst is capable of promoting cross-coupling reactions claim 15 , or other reactions characteristic of catalysis by these metals claim 15 , that form a carbon-carbon claim 15 , carbon-heteroatom or carbon-hydrogen bond.18. The method of claim 15 , wherein Yis methyl.19. The method of claim 15 , wherein the solubilizing agent is selected from the group consisting of Poloxamer 188 claim 15 , Polysorbate 80 claim 15 , Polysorbate 20 claim 15 , Vit E-TPGS claim 15 , Solutol HS 15 claim 15 , PEG-40 Hydrogenated castor oil (Cremophor RH40) claim 15 , PEG-35 Castor oil (Cremophor EL) claim 15 , PEG-8-glyceryl capylate/caprate (Labrasol) claim 15 , PEG-32-glyceryl laurate (Gelucire 44/14) claim 15 , PEG-32-glyceryl palmitostearate (Gelucire 50/13); Polysorbate 85 claim 15 , polyglyceryl-6-dioleate (Caprol MPGO) claim 15 , mixtures of high and low HLB emulsifiers; sorbitan monooleate (Span 80) claim 15 , Capmul MCM claim 15 , Maisine 35-1 claim 15 , glyceryl monooleate claim 15 , glyceryl monolinoleate claim 15 , PEG-6-glyceryl oleate (Labrafil M 1944 CS) claim 15 , PEG-6-glyceryl linoleate (Labrafil M 2125 CS) claim 15 , oleic acid claim 15 , linoleic acid claim 15 , propylene glycol monocaprylate (e.g. Capmul PG-8 or Capryol ...

MIXTURES, PARTICULARLY LOW IN VOLATILE ORGANIC COMPOUNDS (VOC), OF OLEFINICALLY FUNCTIONALISED SILOXANE OLIGOMERS BASED O ALKOXY SILANES

The invention relates to a composition containing olefinically functionalized siloxane oligomers which are derived from olefinically functionalized alkoxy silanes and optionally alkoxy silanes functionalized with saturated hydrocarbons and optionally a tetraalkoxysilane, at most comprising an olefinic group on the silicon atom having a reduced chloride content and the VOC content being lower with respect to the hydrolysable alkoxy-groups. The invention also relates to methods for the production thereof and to the use thereof. 1. A composition comprising an olefinically functionalized siloxane oligomer having not more than one olefinic radical on a silicon atom , [ {'br': None, 'sup': 1', '1', '2', '4', '3', '3, 'sub': 1-x', 'x', 'a', '2', 'c', 'y', '1-y', 'b, '(RO)[(RO)(R)Si(A)O][Si(Y)O][Si(B)(R)(OR)O]R\u2003\u2003(I),'}, 'the olefinically functionalized siloxane oligomer comprises Si—O-crosslinked structural elements that form a catenary, cyclic, crosslinked or optionally three-dimensionally crosslinked structure corresponding to a formula I,'}, 'the structural elements are derived from one or more alkoxysilanes,', 'A corresponds to an olefinic radical and is a linear, branched or cyclic alkenyl- or cycloalkenyl-alkylene-functional group having in each case 2 to 16 C atoms,', 'B corresponds to a saturated hydrocarbon radical and is a linear, branched or cyclic alkyl radical having 1 to 16 C atoms,', {'sup': 3', '3, 'sub': '1/2', 'Y corresponds to ORor, in a crosslinked and optionally three-dimensionally crosslinked structure, independently of one another, to ORor O,'}, {'sup': '1', 'Rindependently at each occurrence corresponds to a linear, branched or cyclic alkyl radical having 1 to 4 C atoms or H,'}, {'sup': '3', 'Rindependently at each occurrence corresponds to a linear, branched or cyclic alkyl radical having 1 to 4 C atoms or to H,'}], 'wherein{'sup': '2', 'Rcorresponds independently at each occurrence to a linear, branched or cyclic alkyl radical having 1 to ...

Continuous process for the preparation of thiocarboxylate silane

The invention is directed to a process for the preparation of thiocarboxylate silane comprising reacting an aqueous solution of a salt of a thiocarboxylic acid with a haloalkylalkoxysilane in the presence of a solid supported catalyst. The invention is also directed to a process for the preparation of an aqueous solution of a salt of a thiocarboxylic acid which comprises reacting an aqueous solution of a sulfide and/or hydrosulfide with a carboxylic acid halide and/or acid anhydride.

SILANES COMPRISING OXAMIDO ESTER GROUPS

,Oxamidoester-functional alkylalkoxysilanes are prepared in high yield by the reaction of an alkylalkoxysilane with an oxalic diester. 18.-. (canceled)10. The silanes of claim 9 , wherein radical Ris a hydrogen atom.12. The method of claim 11 , wherein the molar ratio of compound(s) of the formula (III) to aminosilanes of the formula (II) is greater than 1:1.13. The method of claim 11 , wherein the reaction is carried out at 0° C. to 150° C.14. The method of claim 11 , wherein the reaction is carried out at a pressure of 400 to 1100 hPa. This application is the U.S. National Phase of PCT Appln. No. PCT/EP2017/083534 filed Dec. 19, 2017, the disclosure of which is incorporated in its entirety by reference herein.The invention relates to silanes having oxamidoester groups, to a method for the preparation thereof, and to the use thereof.The chemical groupis often referred to as a 2-amino-2-oxoacetate or oxamide group or as an oxamidoester group, with the term oxamidoester being used to refer to this group hereinbelow. The combination of the half-ester structure with an oxo group means that oxamidoesters have the advantage of being more reactive than amides or carbamates, especially when reacting with amines or alcohols. They are, however, appreciably more stable than isocyanate structures—for example they do not dimerize or trimerize and are appreciably less reactive, which makes reaction control with these groups much more straightforward.Trialkoxysilanes containing oxamidoester groups are mentioned in DE 23 15 242 C2 in the reaction with polyazamide solutions. A method for preparing such products is not however described therein. Moreover, these trialkoxy-functional silanes have the disadvantage that their trifunctionality makes them of only very limited utility as a structural unit for preparing correspondingly functionalized siloxanes, as described inter alia in US-A 2007/149745.Means have accordingly been sought for preparing, in high purity, silanes containing ...

Sacubitril intermediate and preparation method thereof

The present invention relates to a sacubitril intermediate and a preparation method thereof. The sacubitril intermediate disclosed herein can be prepared by a deprotection reaction of a compound. In addition, the intermediate can be used as a raw material to synthesize sacubitril.

CATIONIC LIPIDS CONTAINING SILICON

Certain embodiments of the invention provide a cationic lipid of formula (I): wherein R, R, Rand Rare defined as described herein, as well as methods of making these lipids. Certain embodiments of the invention also provide nucleic acid-lipid particles comprising a cationic lipid of formula (I), methods of making the lipid particles, and methods of delivering and/or administering the lipid particles.

SILANE, RUBBER MIXTURE CONTAINING THE SILANE, VEHICLE TIRE COMPRISING THE RUBBER MIXTURE IN AT LEAST ONE COMPONENT, AND PROCESS FOR PRODUCING THE SILANE

The invention relates to a silane, to a rubber mixture comprising the silane and to a vehicle tire which comprises the rubber mixture in at least one component, and to a process for producing the silane. 110.-. (canceled)11. A silane of formula I):{'br': None, 'sup': 1', '2', '3', '3, 'sub': 'o', '(R)Si—R—S—R—S—R—S—X\u2003\u2003I)'}{'sup': 1', '6', '5', '6', '5, 'sub': r', '1', '30', '2', '2', '13', '27, 'wherein o may be 1, 2 or 3 and the Rradicals may be identical or different and are selected from alkoxy groups having 1 to 10 carbon atoms, cycloalkoxy groups having 4 to 10 carbon atoms, phenoxy groups having 6 to 20 carbon atoms, aryl groups having 6 to 20 carbon atoms, alkyl groups having 1 to 10 carbon atoms, alkenyl groups having 2 to 20 carbon atoms, alkynyl groups having 2 to 20 carbon atoms, aralkyl groups having 7 to 20 carbon atoms, halides, or alkyl polyether groups —O—(R—O)—Rwherein Rare identical or different and are branched or unbranched, saturated or unsaturated, aliphatic, aromatic or mixed aliphatic/aromatic bridging C-Chydrocarbon groups, preferably —CH—CH—, r is an integer from 1 to 30, preferably 3 to 10, and Rare unsubstituted or substituted, branched or unbranched, terminal alkyl, alkenyl, aryl or aralkyl groups, preferably —CHalkyl group;'}or{'sup': '1', 'two Rform a cyclic dialkoxy group having 2 to 10 carbon atoms, in which case o is <3;'}or{'sup': '1', 'two or more silanes of formula I) may be bridged via Rradicals;'}{'sup': 2', '3, 'wherein Rand Rmay be identical or different and are selected from the group consisting of linear or branched alkylene groups having 1 to 20 carbon atoms or cycloalkyl groups having 4 to 12 carbon atoms or aryl groups having 6 to 20 carbon atoms or alkenyl groups having 2 to 20 carbon atoms, alkynyl groups having 2 to 20 carbon atoms or aralkyl groups having 7 to 20 carbon atoms;'}{'sup': 4', '7', '4', '7', '7, 'sub': 3', '1', '20', '4', '10', '6', '20', '2', '20', '7', '20, 'wherein the X group is a hydrogen ...

CYCLIC AMINOORGANOXYSILANE COMPOUND AND ITS PRODUCTION METHOD

A method for producing a cyclic aminoorganoxysilane compound is provided. The method comprises the step of conducting dehydrochlorination coupling of a chloroalkylalkoxysilane compound represented by the formula: 2. The method for producing the cyclic aminoorganoxysilane compound represented by the general formula (3) of comprising the steps of conducting dehydrochlorination coupling of the chloroalkylalkoxysilane compound represented by the general formula (1) and the aminoalcohol represented by the general formula (2) claim 1 , separating and removing hydrochloric salt of the aminoalcohol represented by the general formula (2) by a separation procedure claim 1 , and promoting intramolecular transesterification. This non-provisional application claims priority under 35 U.S.C. §119(a) on Patent Application No. 2014-209951 filed in Japan on Oct. 14, 2014, the entire contents of which are hereby incorporated by reference.The present invention relates to a cyclic aminoorganoxysilane compound which is useful as a silane coupling agent, surface treating agent, resin additive, coating additive, adhesive, and the like. This invention also relates to its production method.Aminoorganoxysilane compounds are useful as a silane coupling agent, surface treating agent, resin additive, coating additive, and adhesive, and in particular, the use of a cyclic aminoorganoxysilane compound for such application is quite useful in view of reducing environmental burden since the amount of a low-boiling alcohol component generated is smaller than the conventional aminoorganoxysilane compound. A cyclic aminoorganoxysilane compound is generally produced at a high yield from an epoxy compound and a primary or secondary aminosilane compound by coupling the epoxy compound and the primary or secondary aminosilane compound and thereafter conducting intramolecular transesterification (Patent Document 1: JP-A 2014-1152).Patent Document 1: JP-A 2014-1152However, the epoxy compound used for the ...

PRODUCTION METHOD FOR COMPOUND COMPRISING AMINO GROUP AND/OR HYDROXYL GROUP

Disclosed is a method for producing a compound having an amino group and/or a hydroxyl group from a substrate compound having an atomic group containing CO or CS by eliminating such atomic group. The substrate compound, having an atomic group containing CO or CS (for example, an amide, a carbamate, or the like), is allowed to react with a compound expressed by formula (I) below, at a temperature of 120° C. or lower, preferably in the presence of an ammonium salt, to eliminate such atomic group containing CO or CS. In formula (I) A may not be present, and in a case where A is present, A represents an alkyl group having 1 to 6 carbon atoms. HN-A—NH(I) - - -. 2. (canceled)3. The method as claimed in claim 1 , wherein the ammonium salt is an ammonium halide.4. The method as claimed in claim 3 , wherein the substrate compound is an amide claim 3 , the atomic group containing CX is an N-acyl group claim 3 , and the reaction is carried out by eliminating the acyl group to produce a compound having an amino group from said substrate compound.5. The method as claimed in claim 4 , wherein the compound expressed by the formula (I) for the reaction is hydrazine.6. The method as claimed in claim 4 , wherein the compound expressed by the formula (I) for the reaction is the alkylamine.7. The method as claimed in claim 6 , wherein the compound expressed by the formula (I) for the reaction is ethylenediamine.8. The method as claimed in claim 1 , wherein the substrate compound is a cyclic carbamate claim 1 , a chain carbamate claim 1 , a cyclic carbonate claim 1 , a chain carbonate claim 1 , a cyclic urea or a chain urea claim 1 , the atomic group containing CX is carbonyl group claim 1 , and the reaction is carried out by allowing the substrate compound with the alkylamine as the compound expressed by the formula (I) to eliminate the carbonyl group to produce a compound having an amino group and/or a hydroxyl group.9. The method as claimed in claim 1 , wherein the substrate compound ...

Intermediate of eribulin and preparation method therefor

Disclosed are an intermediate of Eribulin and a preparation method therefor. In particular, disclosed are compounds as represented by formula II, formula III and formula V and a preparation method therefor. Ar is C 1-10 alkyl substituted, alkyloxy substituted or unsubstituted aryl; R 1 and R 2 is an acetal protecting group or a thioacetal protecting group; R 3 is hydrogen or a hydroxyl protecting group; and X is halogen or a leaving group. The preparation method therefor has the advantages of mild reaction conditions, high selectivity, easy purification, low synthesis cost and the like, being suitable for large scale production.

Methods of carbon-carbon bond fragmentation

The present disclosure relates to methods of carbon-carbon bond fragmentation.

METHOD FOR PRODUCING NITROGEN-CONTAINING ORGANOXYSILANE COMPOUND

A method for producing a compound (3), 2. The method for producing a nitrogen-containing organoxysilane compound according to claim 1 , wherein the solvent is a protic polar solvent.3. The method for producing a nitrogen-containing organoxysilane compound according to claim 2 , wherein the protic polar solvent is an alcohol compound.4. The method for producing a nitrogen-containing organoxysilane compound according to claim 1 , wherein 1.4 mol or more of the amine compound having the general formula (1) is used per 1 mol of the halogen atom in the haloalkyl organoxysilane compound having the general formula (2).5. The method for producing a nitrogen-containing organoxysilane compound according to claim 1 , wherein 0.6 mol or more and less than 1 mol of the nitrogen-containing compound having the general formula (4) is used per 1 mol of the halogen atom in the haloalkyl organoxysilane compound having the general formula (2).6. The method for producing a nitrogen-containing organoxysilane compound according to claim 1 , wherein the nitrogen-containing compound having the general formula (4) is 1 claim 1 ,8-diazabicyclo[5.4.0]undeca-7-ene or 1 claim 1 ,5-diazabicyclo[4.3.0]nona-5-ene. This non-provisional application claims priority under 35 U.S.C. § 119(a) on Patent Application No. 2020-197919 filed in Japan on Nov. 30, 2020, the entire contents of which are hereby incorporated by reference.The present invention relates to a method for producing a nitrogen-containing organoxysilane compound.Nitrogen-containing organoxysilane compounds are useful as an agent such as a silane coupling agent, a surface treatment agent, a resin additive agent, a paint additive agent, or an adhesive agent.Examples of the compound known as such a nitrogen-containing organoxysilane compound include organoxysilane compounds, such as aminopropyltrimethoxysilane, having a primary amino group, organoxysilane compounds, such as N-phenylaminopropyltrimethoxysilane, having a secondary amino group, ...

SILANE COUPLING COMPOUNDS AND MEDICAL AND/OR DENTAL CURABLE COMPOSITIONS COMPRISING THE SAME

The present invention relate to a novel silane coupling agent and a medical and/or dental curable composition comprising the same. It is an object of the present invention to provide a novel silane coupling agent that imparts high affinity to a radical polymerizable monomer, thereby imparting high mechanical strength, flexibility and durability when used for a medical and/or dental curable composition, and an inorganic filler surface-treated with the novel silane coupling agent and a novel medical and/or dental curable composition. A silane coupling agent including repeating units such as a urethane bond and polyethylene glycol (ether bond) at a specific position is used. 17-. (canceled)8. A silane coupling agent having:a polymerizable group,a reactive silyl group, anda spacer group connecting the polymerizable group and the reactive silyl group, [ {'br': None, 'sup': 1', '3, '—Z—NH—C(O)OR—\u2003\u2003Formula (I)'}, 'Spacer group I, {'sup': 1', '3', 'n', 'n, 'sub': 2', '2', '3', '2', '2', '3', '2', '6', '6', '4', '2', '2', '3', '2', '2', '3, 'wherein, Zis a C2-C30 linear or branched saturated aliphatic hydrocarbon group, and has at least one or more of —CH—CH—O—, —O—CH(CH)—CH— and —O—CH—CH(CH)— groups, and Ris a C7-C30 linear or branched alkylene group, and may have one or more of —S—, —NH—, —NR— wherein Rrepresents an alkylene group, —CH—CH— wherein CHrepresents a phenylene group, —C(O)—O—, —O—, —CH—CH—O—, —O—CH(CH)—CH— and —O—CH—CH(CH)— groups.'}], 'wherein the spacer group is the following spacer group I10. The silane coupling agent according to claim 8 , which is synthesized using a compound having any one of the following structures (2-(2-isocyanatoethoxy)ethyl methacrylate or 2-(2-isocyanatoethoxy)ethyl acrylate):{'br': None, 'sub': 2', '3', '2', '2', '2', '2, 'CH═C(CH)—C(O)—O—CH—CH—O—CH—CH—NCO'}{'br': None, 'sub': 2', '2', '2', '2', '2, 'CH═CH—C(O)—O—CH—CH—O—CH—CH—NCO.'}11. An inorganic filler which is surface-treated with the silane coupling agent according ...

METHOD FOR PRODUCING AN IONIC LIQUID

The present invention is directed to a method of preparing an alkoxy silane functional ionic liquid comprising reacting a halogenated compound comprising a halogen and an active hydrogen functional group, an isocyanato functional alkoxy silane, and an ionizable compound capable forming an ionic bond with the halogen to form the alkoxy silane functional ionic liquid. The present invention is also directed to alkoxy silane functional ionic liquids. 1. A method of preparing an alkoxy silane functional ionic liquid comprising:reacting a halogenated compound comprising a halogen and an active hydrogen functional group, an isocyanato functional alkoxy silane, and an ionizable compound capable of forming an ionic bond with the halogen to form the alkoxy silane functional ionic liquid; wherein the ionizable compound comprises a heteroatom.2. The method of claim 1 , wherein the method comprises:a first step comprising reacting the halogenated compound and the isocyanato functional alkoxy silane to form a halogenated alkoxy silane, anda second step comprising reacting the halogenated alkoxy silane with the ionizable compound to form the alkoxy silane functional ionic liquid.3. The method of claim 1 , wherein the method comprises:a first step comprising reacting the halogenated compound and the ionizable compound to form an ionic liquid comprising an active hydrogen functional group, anda second step comprising reacting the ionic liquid comprising an active hydrogen functional group with the isocyanato functional alkoxy silane to form the alkoxy silane functional ionic liquid.4. The method of claim 1 , wherein the halogenated compound comprises a halogenated alcohol.5. The method of claim 4 , wherein the halogenated alcohol comprises 3-chloro-propanol.7. The method of claim 6 , wherein the isocyanato functional trialkoxy silane comprises isocyanatopropyl trimethoxy silane.8. The method of claim 1 , wherein the ionizable compound comprises an imidazole.9. The method of claim 8 ...

METHODS AND SYSTEMS FOR CAMPTOTHECIN ANALOG SYNTHESIS

Methods and systems for making camptothecin analogs and intermediates are provided. Aspects include safer and lower cost methodologies for making camptothecin analogs and intermediates from synthetic materials. In another aspect, the methods and systems can achieve a yield of the camptothecin analogs greater than about 0.4%. 1forming AP4622-1 from propane-1,3-dithiol and 3-hydroxybenzaldehyde;adding a solution of TBSC1 to a solution of AP4622-1 and imidazole to form AP4622-2;adding n-BuLi to a solution of AP4622-2 to form a first mixture and adding TBSC1 to the mixture to form AP4622-3;adding a solution of AP4622-3 to a solution of NBS to form AP4622-4;adding tetrabutylammonium fluoride trihydrate to a solution of AP4622-4 to form AP4622-5;{'sub': '3', 'adding HNOto a solution of AP4622-5 to form AP4622-6;'}adding tin powder to a mixture of AP4622-6 to form AP4622; andcombining AP4622, s-Trione, in the presence of TsOH to form AR67.. A method of making the compound of Formula II comprising: This application claims priority to U.S. Provisional Patent Application Ser. No. 62/067,065, filed Oct. 22, 2014. The above referenced application is incorporated herein by reference as if restated in full.All references cited herein, including but not limited to patents and patent applications, are incorporated by reference in their entirety.Camptothecin is a topoisomerase I inhibitor originally isolated from the bark and stem of Camptothecaacuminata (Camptotheca, Happy tree), a tree native to China.Camptothecin analogs having anti-cancer and anti-tumor properties are described in U.S. Pat. No. 6,136,978, hereby incorporated by reference in its entirety. In one aspect, these camptothecin analogs have the following general structure (Formula I) described in U.S. Pat. No. 6,136,978 (“'978 patent”):where R-Rare defined as in the '978 (e.g., col. 3, line 35—col. 4, line 65).Of particular interest is a camptothecin analog known as AR-67 or DB-67 ((20S)-10-hydroxy-7- ...

Process for preparing a colourless solution of 3-(N-benzyl-2-aminoethyl)aminopropyltrimethoxy-silane hydrochloride in methanol

A process can prepare a colourless, methanolic solution of 3-(N-benzyl-2-aminoethyl)aminopropyltrimethoxysilane hydrochloride. The process includes, in step 1 fractionally distilling the vinylbenzyl chloride reactant component with addition of at least one stabilizer, and in step 2, metering and mixing the distillate (vinylbenzyl chloride) from step 1 into an initial charge of N-(2-aminoethyl)-3-aminopropyltrimethoxysilane and methanol in a molar ratio of the N-(2-aminoethyl)-3-aminopropyltrimethoxysilane to vinylbenzyl chloride of 1.0:0.80 to 1.0:1.15 and at a temperature in the range from 40 to 60° C. and leaving them to react further. The colourless, methanolic solution has an APHA colour number of <200 mg Pt—Co/I. 1. A process for preparing a colourless solution of 3-(N-benzyl-2-aminoethyl)aminopropyltrimethoxysilane hydrochloride in methanol , wherein the colourless solution has an APHA colour number of ≤200 mg Pt—Co/I , the process comprising:fractionally distilling a vinylbenzyl chloride reactant component with addition of at least one stabilizer, to obtain a distillate containing vinylbenzyl chloride, andmetering and mixing the distillate from said fractionally distilling into an initial charge of N-(2-aminoethyl)-3-aminopropyltrimethoxysilane and methanol in a molar ratio of the N-(2-aminoethyl)-3-aminopropyltrimethoxysilane to vinylbenzyl chloride of 1.0:0,80 to 1.0:1.15 and at a temperature in the range from 40 to 60° C. and leaving them to react further.2. The process according to claim 1 , wherein at least one stabilizer selected from the group consisting of nitromethane claim 1 , 4-tert-butylpyrocatechol claim 1 , and 2 claim 1 ,4-dinitrophenol is used during said fractionally distilling.3. The process according to claim 1 , wherein a vinylbenzyl chloride with APHA colour number ≤5 mg Pt—Co/I is used during said metering and mixing.4. The process according to claim 1 , wherein N-(2-aminoethyl)-3-aminopropyltrimethoxysilane is metered into vinylbenzyl ...

Ester-Functional Silanes And The Preparation And Use Thereof; And Use Of Iminium Compounds As Phase Transfer Catalysts

A method for producing a reaction product comprising an ester-functional silane, the method comprising: i) reacting a composition comprising: a) a haloorganosilane, b) a metal salt of a carboxy-functional compound, c) a phase transfer catalyst comprising a bicyclic amidine, an iminium compound, or a mixture thereof, provided that the iminium compound is not an acyclic guanidinium compound or pyridinium compound, and d) a co-catalyst, provided that the co-catalyst is optional when the phase transfer catalyst comprises the iminium compound. 1. A method for producing a reaction product comprising an ester-functional silane , the method comprising: i) reacting a composition comprising:a) a haloorganosilane,b) a metal salt of a carboxy-functional compound,c) a phase transfer catalyst comprising a bicyclic amidine, an iminium compound, or a mixture thereof, provided that the iminium compound is not an acyclic guanidinium compound or pyridinium compound, andd) a co-catalyst, provided that the co-catalyst is optional when the phase transfer catalyst comprises the iminium compound.2. The method of claim 1 , the method being characterizable by one or more of limitations (g) claim 1 , (h) claim 1 , (j) claim 1 , (k) claim 1 , (l) claim 1 , and (m):(g) step i) is performed under substantially anhydrous conditions by heating at a reaction temperature up to 180° C. for a reaction time up to 18 h;(h) the method further comprises step ii) removing at least a portion of a metal halide formed as a by-product in step i);(j) the method further comprises step iii) recovering an ester-functional silane formed in step i);(k) the method further comprises drying one or more of a), b), and c) before step i);(l) ingredient c) comprises a 8-octyl-1,8-diazabicyclo[5.4.0]-undec-7-enium bromide; a 8-2-ethylhexyl-1,8-diazabicyclo[5.4.0]-undec-7-enium bromide; a 8-octyl-1,8-diaza-bicyclo[5.4.0]-undec-7-enium chloride; a 7-2-ethylhexyl-7-methyl-1,5,7-triazabicyclo[4.4.0]dec-5-enium bromide; 5-butyl- ...

Metal Complexes, Their Application and Methods of Carrying out of Metathesis Reaction

This disclosure relates to new metal complexes, such as compounds of Formula 1, and their application in olefin or alkyne metathesis and to methods of carrying out olefin metathesis reactions. 2. A compound according to claim 1 , wherein R claim 1 , R claim 1 , and Rare independently hydrogen or methyl.3. A compound of claim 1 , whereinM is ruthenium;{'sup': 1', '9', '9', '9', '9', '9, 'sub': 2', '1', '12', '3', '12', '5', '14', '1', '6', '1', '6', '1', '6, 'X and Xare independently halide, —OR, —O(C═O)R, or —O(SO)R, wherein Ris C-Calkyl, C-Ccycloalkyl, or C-Caryl, wherein Rmay be optionally substituted with C-Calkyl, C-Cperhaloalkyl, C-Calkoxy, or halide;'}L is N-heterocyclic carbene ligand (NHC);{'sup': '1', 'sub': '1-20', 'Ris hydrogen or Calkyl;'}{'sup': 2', '3', '4', '5, 'sub': 1-20', '2-20', '2-20', '5-10', '1-20', '2-20', '2-20', '5-10', '1-20', '1-20', '1-20', '1-20', '1-20', '1-20', '1-20', '5-10', '4-10, 'R, R, R, and Rare independently hydrogen, halide, Calkyl, Calkenyl, Calkynyl, Caryl, Calkoxy, Calkenyloxy, Calkynyloxy, Caryloxy, Calkoxycarbonyl, Calkylamino, Cprotonated alkylamino, amino, protonated amino, Calkylammonium, nitro, carboxy, amido, sulfonamido, or Cperhaloalkyl; those groups can be optionally substituted with Calkyl, Cperhaloalkyl, Caryl, or Cquaternized heterocyclic;'}{'sup': 2', '3', '4', '5, 'sub': 4-8', '5-14, 'wherein 2 or more of R, R, R, and Rmay be linked together to form a substituted or unsubstituted fused Ccarbocyclic ring, or a substituted or unsubstituted fused aromatic Cring;'}{'sup': 6', '7', '8', '7', '8, 'sub': 1-6', '4-10', '4-10', '5-14', '4-8, 'R, R, and Rare independently hydrogen, Calkyl, Ccycloalkyl, Cheterocyclic, or Caryl; wherein Rand Rmay be linked together to form a substituted or unsubstituted cyclic system C.'}4. A compound according to claim 3 , wherein R claim 3 , R claim 3 , and Rare independently hydrogen or methyl.5. A compound of claim 1 , whereinM is ruthenium;{'sup': 1', '9', '9', '9', '9', '9, 'sub': ...

IMPROVED PROCESS FOR THE PREPARATION OF TREPROSTINIL AND DERIVATIVES THEREOF

A method for the preparation of treprostinil and its derivatives is described. In contrast to prior art, this method utilizes an easily scalable enzymatic resolution of a key intermediate for making these compounds. Another significant improvement of the described method over prior methods is the regioselective Claisen rearrangement of a 5-allyloxy-benzaldehyde precursor, which is facilitated by a bromo substituent in 2-position. 2. A compound according to claim 1 , wherein X and Y are independently of one another selected from the group consisting of H claim 1 , Br and Cl claim 1 , and wherein at least one of X or Y is not H.3. A compound according to claim 2 , wherein:X is Br or Cl; andY is H.4. A compound according to claim 1 , wherein X is Br.5. (canceled)7. The process according to claim 6 , wherein PGis TBDMS.8. The process according to claim 6 , wherein Ris hydroxy.9. The process according to claim 6 , wherein:X is Br;Y is hydrogen;{'sub': '1', 'PGis benzyl;'}{'sub': '2', 'PGis TBDMS; and'}{'sup': 'a', 'Ris hydroxy.'}11. The process according to claim 10 , wherein the solvent is selected from the group consisting of vinyl acetate claim 10 , hexane(s) claim 10 , heptane(s) claim 10 , and chloroform.12. The process according to claim 10 , wherein the hydrogenation is performed at a pH of between about 8 and 12.14. (canceled)15. The process according to claim 12 , wherein the hydrogenation is performed at a pH of between about 9 and 10. The present invention relates to a shortened and more convenient process for producing treprostinil as well as novel intermediates useful in the process. Key features of the described process include a regioselective Claisen rearrangement of an allyloxy benzaldehyde precursor; tert-butyl-dimethylsilyl (TBDMS) protection of the alcohol moiety in the alkyne-bearing side chain during the non-stereoselective, intramolecular Pauson-Khand cyclization; and enzymatic kinetic resolution and subsequent chromatographic separation of two ...

PRODUCTION METHOD FOR OPTICALLY ACTIVE ALCOHOL COMPOUND

A method for stereoselectively producing an optically active alcohol compound. The optically active alcohol compound of Formula (8) can be produced in high yield and high selectivity from the compound of Formula (3), and the production method that is useful industrially and the intermediates therefor can be provided. In formulae, Ris a hydrogen atom, Calkyl, Calkyl optionally substituted with R, or the like, Ris cyano or —CHN(R)R, and Ris Ccycloalkyl. 2. The method for producing the optically active alcohol compound according to claim 1 , wherein Ris a hydrogen atom claim 1 , (C) alkyl optionally substituted with R claim 1 , —C(O)R— claim 1 , or —Si(R)(R)R.3. The method for producing the optically active alcohol compound according to claim 2 , wherein the reaction is carried out in the presence of the optically active ruthenium catalyst of Formula (4).4. The method for producing the optically active alcohol compound according to claim 3 , wherein{'sup': 2', '5', '4, 'sub': '2', 'Ris —CHN(R)R;'}{'sup': 4', '6', '7, 'Ris —C(O)Ror —C(O)OR;'}{'sup': '6', 'sub': 1-6', '1-6, 'Ris Calkyl or (C) alkyl optionally substituted with a halogen atom; and'}{'sup': '8', 'sub': 1-6', '1-6, 'Ris a hydrogen atom, Calkyl, or (C) alkyl optionally substituted with a halogen atom.'}5. The method for producing the optically active alcohol compound according to claim 4 , wherein{'sup': 1', '3', '12a', '12b', '12, 'sub': '1-6', 'Ris (C) alkyl optionally substituted with R, or —Si(R)(R)R;'}{'sup': '3', 'sub': '3-8', 'Ris phenyl, or Ccycloalkyl;'}{'sup': 5', '5', '4', '5', '4, 'sub': '4', 'Ris a hydrogen atom, or Roptionally forms a 5-membered ring together with a nitrogen atom to which Rand Rare bonded by forming a Calkylene chain together with R, and in this case the alkylene chain is optionally substituted with an oxo group, or the alkylene chain optionally forms phenyl together with carbon atoms to which two substituents each bond when the two substituents exist at adjacent positions on ...

Method for producing aqueous hydrolysates from aminoalkyltrialkoxysilanes

The present invention relates to a process for preparing aqueous hydrolysates of aminoalkyltrialkoxysilanes by (a) initially charging water, optionally heating, (b) adding hydrolysable silanes consisting of at least one aminoalkyltrialkoxysilane in an amount which provides a molar ratio of water to total amount of aminoalkyltrialkoxysilane of 10.5 to 20, and (c) distilling off the alkyl alcohol formed in the reaction, wherein the solids content in an aqueous composition thus prepared is 30% to 55% by weight, based on the composition, and the aqueous solution has a total content of free and bound alkyl alcohol of not more than 1% by weight, based on the composition.

Intermediates useful in the preparation of halichondrin compounds and methods for preparing the same

The invention relates to intermediates useful in the preparation of halichondrin compounds, methods for preparing the same and use thereof, such as halichondrins, eribulin, or their analogs. The intermediates, the methods and use thereof are used for the synthesis of the C20-C26 fragment of halichondrin compounds. The raw materials in the synthetic route of the invention are cheap and easily obtained, the sources and the qualities of the raw materials are reliable. The choice of the methods useful in the synthesis of chiral central structures are based on the structural characteristics of the reactants, thus effectively improving the synthesis efficiency, reducing the difficulties and risks of product quality control, and avoiding the use of highly toxic and expensive organotin catalysts to significantly decrease costs and improve environmental friendliness. 110-. (canceled)21. The method for preparing the compound of Formula (8) of claim 16 ,the method for preparing said aldehyde comprises the following steps:{'sub': n', '4-n, '(I) reacting butanediol and RSiXin the presence of coupling agents to obtain a monohydroxy protected product;'}{'sub': '1-10', 'wherein X is halogen selected from the group consisting of chlorine, bromine and iodine, R is selected from the group consisting of Calkyl or fluorinated alkyl, and n is an integer of 1-3. Examples of said halogenated silane are TMSCl, TMSI, TBDPSCl, or TBDPSI, etc.'}(II) Oxidizing said product obtained in step (I).25. A method for preparing halichondrins claim 11 , eribulin claim 11 , their pharmaceutically acceptable salts claim 11 , their analogs or C20-C26 fragment claim 11 , comprising the reaction step in .26. A method for preparing halichondrins claim 24 , eribulin claim 24 , their pharmaceutically acceptable salts claim 24 , their analogs or C20-C26 fragment claim 24 , comprising the reaction step in .27. A method for preparing halichondrins claim 22 , eribulin claim 22 , their pharmaceutically acceptable ...

ALKOXY-SILANES COMPOUNDS AND RELATED CONDENSATION PRODUCTS AS COSMETIC RAW MATERIALS AND FOR COATING COSMETIC POWDERS

There are described alkoxy-silanes compounds and related condensation products as cosmetic raw materials and for coating cosmetic powders; synthesis processes of such compounds and condensation products and production of coated cosmetic powders. Said cosmetic powders can be used for preparing cosmetic products such as anhydrous products for face/eyes/lips, cosmetic pencils and face/eyes emulsions. 115-. (canceled)17. A coating compound for cosmetic powders according to claim 16 , whereinA is a hydrocarbon radical having from 15 to 25 carbon atoms,B is a urethane group,{'sub': 2', '3', 'x', '3-x', '2', '3', '3, 'sup': 1', '2', '1', '2, 'C is a propyl trialkoxyl silane group —(CH)Si(OR)(OR)where 0≤x≤3 where Rcorresponds to an ethyl radical —CHCHand Rto the methyl radical —CH.'}20. Coating compound according to claim 19 , wherein the grinding is adapted to obtain a powdery solid having a particle size of <250 μm.21. Coating compound according to claim 19 , wherein the grinding is adapted to obtain a powdery solid having a particle size of <100 μm.22. Coating compound according to claim 19 , wherein the powdery solid is adapted to be added to a cosmetic formulation in a percentage from 80% to 1%.23. Coating compound according to claim 22 , wherein the powdery solid is adapted to be added to a cosmetic formulation in a percentage from 50% to 5%.24. Coating compound according to claim 22 , wherein the powdery solid is adapted to be added to a cosmetic formulation in a percentage from 30% to 10%.25. Coating compound according to claim 19 , wherein the condensation reaction occurs in the presence of a suitable cosmetic substrate comprising surface silanols adapted to be functionalized through the formation of stable covalent bonds with the organic compound.26. Coating compound according to claim 16 , wherein it comprises the docosanil carbamoyl propyl triethoxysilane compound from 1 to 10% by weight with respect to a cosmetic substrate claim 16 , conveying the compound by ...

HYDROLYSABLE AND POLYMERIZABLE SILANES WITH ADJUSTABLE SPATIAL DISTRIBUTION OF THE FUNCTIONAL GROUPS, AND USE THEREOF

The present invention relates to a process for a chain extension of radicals bonded to silicon via carbon in silanes or siloxanes while maintaining or increasing the number of functional groups on the respective Si—C-bonded radicals, wherein a silane or siloxane with a radical bonded to a silicon atom by a carbon atom, which bears at least two functional groups, wherein a first group of the functional groups is an unsaturated, organically polymerizable group and a second group of the functional groups is selected from among 1. A process for a chain extension of Si—C bonded radicals of silanes or siloxanes having at least two functional groups , wherein the number of functional groups on the respective Si—C bonded groups is maintained or increased ,whereina silane or siloxane with a radical bonded to a silicon atom by a carbon atom, the radical bearing at least two functional groups,wherein a first group of the functional groups is an unsaturated, organically polymerizable group and a second group of said functional groups is selected among(a) additional unsaturated, organically polymerizable groups,{'sup': 8', '5, 'sub': b', '2, '(b) COORor —(O)P(O)(R)and'}(c) —OH,{'sup': 8', '4', 'x+', 'x+, 'sub': '1/x', 'with Requal to Ror M, M being hydrogen or an x-fold positively charged metal cation,'}and b=0 or 1,is converted in an initial reaction {'br': None, 'sub': 'a', 'X—W—(Z)\u2003\u2003(I)'}, 'with a compound of a formula (I)'}wherein{'sub': '2', 'sup': '4', 'X is SH, NHor NHR,'}Z is OH, a carboxylic acid group —COOH or a salt or an ester of said group or a silyl group,W is a substituted or non-substituted hydrocarbon group, a chain of which can be interrupted by{'sup': '4', '—S—, —O—, —NH—, —NR—, —C(O)O—, —NHC(O)—, —C(O)NH—, —NHC(O)O—, —C(O)NHC(O)—, —NHC(O)NH—, —S(O)—, —C(S)O—, —C(S)NH—, —NHC(S)—, —NHC(S)O—, and'}a represents 1, 2, 3, 4 or a greater whole number, andwherein{'sup': '4', 'Ris a non-substituted or substituted hydrocarbon group,'}{'sup': 5', '6, 'Ris a ...

Preparation method of epoxy compound having alkoxysilyl group, epoxy compound having alkoxysilyl group, composition comprising the same, and use thereof

Provided are a preparation method of an epoxy compound having an alkoxysilyl group in which an increase in the epoxy equivalent weight (EEW) of the epoxy compound is minimized because alkoxysilylation occurs through a simple one-step reaction using a hydroxyl group formed during the synthesis of the epoxy compound, an epoxy compound having an alkoxysilyl group prepared by the method, a composition comprising the same, and a use thereof. The method includes the reaction of an epoxy compound having a hydroxyl group with an isocyanate alkoxysilane in the presence of amine-based base catalyst, wherein the epoxy compound having an alkoxysilyl group has a mole ratio of [epoxide group]:[alkoxysilyl group] of n:1 ranging from 2:1 to 10:1, and an EEW increase of the epoxy compound having an alkoxysilyl group is less than 260/n. The epoxy compound has good physical properties when being cured.

TETRAZOLE SILANE COMPOUND, METHOD FOR SYNTHESIZING SAID COMPOUND AND USE THEREOF

The objectives of the present invention are: to provide a novel tetrazole silane compound, a method for synthesizing the same, and a silane coupling agent containing the tetrazole silane compound as a component; and to provide a surface treatment solution using the tetrazole silane compound, a method for surface treatment, and a method for adhering two different materials. The tetrazole silane compound according to the present invention is a compound represented by chemical formula (I). (In formula (I), X, R, and n are respectively the same as defined in the specification.) 134-. (canceled) The present invention relates to a novel tetrazole silane compound, a surface treatment solution and a surface treatment method using the tetrazole silane compound, and use thereof.As a component of a silane coupling agent, an organic compound having a silicon atom in its molecule has been used. Such a substance has functional groups having different affinities in the molecule, and exhibits a function as an intermediary between organic materials and inorganic materials that are not normally compatible. Therefore, it is an essential agent for development and production of composite materials.Patent Literature 1 proposes, as a component of a silane coupling agent used as a primer for bonding glass or metal to rubber, various substances having a structure where a nitrogen containing heterocyclic ring such as triazole or thiadiazole is connected to a silyl group such as a trimethoxysilyl group or a triethoxysilyl group, through an organic group having a thioether (sulfide) bond or the like.Patent Literature 2 proposes 1N-trimethoxysilylpropyl-1,2,4-triazole as a silane compound used as a corrosion inhibitor for aluminum and magnesium alloys.Patent Literature 1: JP-A-2002-363189Patent Literature 2: US-A-2012/0021232An object of the present invention is to provide a novel tetrazole silane compound, a synthesis method thereof, and a silane coupling agent containing the novel tetrazole ...

HYDROXYMETHYL-CARBOXAMIDO-SUBSTITUTED SILANE AND ITS USE FOR CURABLE, SILANE-TERMINATED POLYMERS

Specific hydroxysilanes of formula (I), a method for the production thereof, the use thereof as a constituent of moisture-curing compositions, and silane-functional compounds produced therefrom, in particular silane-functional polymers and isocyanatosilanes. The hydrosilanes can be produced in a simple process with a high degree of purity and are storage-stable after production. Production from the reaction of lactides with aminosilanes is particularly advantageous. Hydroxysilane of formula (I), where n is 1 or 2. 2. The hydroxysilane as claimed in claim 1 , wherein Rand R claim 1 , independently of one another claim 1 , are in each case a hydrogen atom or a methyl radical.3. The hydroxysilane as claimed in claim 1 , wherein Ris a hydrogen atom or an alkyl radical or a cycloalkyl radical or an alkoxysilylalkyl radical.4. The hydroxysilane as claimed in claim 1 , wherein Ris selected from the group consisting og 1 claim 1 ,3-propylene claim 1 , 4-aza-1 claim 1 ,6-hexylene claim 1 , 2-methyl-1 claim 1 ,3-propylene claim 1 , 1 claim 1 ,4-butylene claim 1 , 3-methyl-1 claim 1 ,4-butylene and 3 claim 1 ,3-dimethyl-1 claim 1 ,4-butylene.5. The hydroxysilane as claimed in claim 1 , wherein Ris a methyl radical or ethyl radical.6. The hydroxysilane as claimed in claim 1 , wherein x is 1 or 0.7. The hydroxysilane as claimed in claim 1 , wherein it is selected from the group consisting of N-(3-triethoxysilylpropyl)-2-hydroxyacetamide claim 1 , N-(3-trimethoxysilylpropyl)-2-hydroxyacetamide claim 1 , N-(3-diethoxymethylsilylpropyl)-2-hydroxyacetamide claim 1 , N-(3-dimethoxymethylsilylpropyl)-2-hydroxyacetamide claim 1 , N-(3-triethoxysilylpropyl)-2-hydroxypropanamide claim 1 , N-(3-trimethoxysilylpropyl)-2-hydroxypropanamide claim 1 , N-(3-diethoxymethylsilylpropyl)-2-hydroxypropanamide claim 1 , N-(3-dimethoxymethylsilylpropyl)-2-hydroxypropanamide claim 1 , N-(3-triethoxysilylpropyl)-2-hydroxy-2-methylpropanamide claim 1 , N-(3-trimethoxysilylpropyl)-2-hydroxy-2- ...

METHOD FOR PRODUCING RUTHENIUM CATALYST AND METHOD FOR PRODUCING ALKYL GROUP- OR ALKENYL GROUP-SUBSTITUTED COMPOUND USING RUTHENIUM CATALYST

This invention relates to a method for producing a ruthenium catalyst in which ruthenium supported on at least one metal oxide is pretreated with an aldehyde compound, a phosphorus compound, and a lower alcohol compound, and a method for producing alkyl- or alkenyl-substituted compound using the ruthenium catalyst. 2. The method for producing a ruthenium catalyst according to claim 1 , wherein the aldehyde compound is at least one member selected from the group consisting of formaldehyde claim 1 , 1 claim 1 ,3 claim 1 ,5-trioxane claim 1 , paraformaldehyde claim 1 , glyoxal claim 1 , methylglyoxal claim 1 , malonaldehyde claim 1 , acetaldehyde claim 1 , and propionaldehyde.3. The method for producing a ruthenium catalyst according to claim 1 , wherein the aldehyde compound is formaldehyde.4. The method for producing a ruthenium catalyst according to claim 1 , wherein the phosphorus compound is at least one member selected from the group consisting of phosphines claim 1 , phosphites claim 1 , and phosphine oxides.5. The method for producing a ruthenium catalyst according to claim 1 , wherein the phosphorus compound is triphenylphosphine.6. The method for producing a ruthenium catalyst according to claim 1 , wherein the lower alcohol compound is at least one member selected from the group consisting of lower alcohols claim 1 , lower alkylene glycols claim 1 , and lower alkoxy-lower alcohols.7. The method for producing a ruthenium catalyst according to claim 1 , wherein the lower alcohol compound is 2-methoxyethanol.8. The method for producing a ruthenium catalyst according to claim 1 , wherein the heating temperature is 40 to 200° C. The present invention relates to a method for producing a ruthenium catalyst supported on at least one metal oxide, and a method for producing an alkyl- or alkenyl-substituted compound using a heterogeneous catalyst that is a ruthenium catalyst supported on at least one metal oxide.A method for producing an alkyl- or alkenyl-substituted ...

METHOD FOR PRODUCING SILANE COMPOUND HAVING SULFONYL BOND

A method of producing a silane compound having a Formula (1) sulfonyl bond includes reacting a Formula (I) chlorosulfonyl compound with sodium sulfite in water as a solvent in the presence of a base, to produce a Formula (II) sulfinic acid sodium salt: and adding an aromatic hydrocarbon solvent to carry out azeotropic dehydration, and adding an aprotic polar solvent and a Formula (III) chloroalkylsilane compound. 2. The method according to claim 1 , wherein at the step (B) claim 1 , the reaction after addition of the aprotic polar solvent is carried out while the aromatic hydrocarbon solvent in the reaction system is distilled off.3. The method according to claim 1 , wherein the aprotic polar solvent is N-methyl-2-pyrrolidone.4. The method according to claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , R claim 1 , and Rare each independently a hydrogen atom claim 1 , a halogen atom claim 1 , a Calkyl group claim 1 , a Calkoxy group claim 1 , a Chaloalkyl group claim 1 , or a Chaloalkoxy group.5. The method according to claim 2 , wherein the aprotic polar solvent is N-methyl-2-pyrrolidone. The present invention relates to a novel method for producing a silane compound having a sulfonyl bond useful for a raw material for a composition for forming an underlayer film between a substrate and a resist (such as a photoresist, an electron beam resist, and an EUV resist) used in production of a semiconductor device.Fine processing by lithography using a photoresist has been conventionally carried out in production of a semiconductor device. The fine processing is a processing method in which a thin film of the photoresist is formed on a semiconductor substrate such as a silicon wafer, irradiated with an active light such as ultraviolet light through a mask pattern that has a pattern of the semiconductor device, and developed, and the substrate is etched using the obtained photoresist pattern as a protective film to form fine concaves and convexes corresponding to the ...

METHOD FOR PRODUCING IODINE-CONTAINING SILICON COMPOUND

A method for producing a silicon compound containing an iodophenyl group, including substituting iodine for a trialkylsilyl ((R)Si) group bonded to a phenyl group by using an iodine-containing electrophilic reagent (I-X) as shown by the following reaction equation: 2. The method for producing a silicon compound containing an iodophenyl group according to claim 1 , wherein the Ris a methyl group or an ethyl group.3. The method for producing a silicon compound containing an iodophenyl group according to claim 1 , wherein the iodine-containing electrophilic reagent is iodine monochloride.4. The method for producing a silicon compound containing an iodophenyl group according to claim 2 , wherein the iodine-containing electrophilic reagent is iodine monochloride. The present invention relates to a method for producing an iodine-containing silicon compound.Iodine-containing compounds highly efficient in absorbing EUV light are expected to improve the performance of resist for EUV, which is currently one of problems in the industrialization of EUV lithography. As a stable iodine-containing compound, an organic group having iodine directly bonded to an aromatic ring, particularly an iodophenyl group, is introduced into a silicon-containing resist underlayer film (hereinafter referred to as polysiloxane underlayer film). Such an underlayer film is expected to have a possibility of improving the performance of patterning an EUV resist.To obtain such a polysiloxane underlayer film having an iodophenyl group, a hydrolysable silicon compound having an iodophenyl group introduced therein is necessary (hereinafter referred to also as iodine-containing silicon compound). As methods for producing such an iodine-containing silicon compound, there have been known: a method in which a Grignard reagent is prepared from a bromophenylsilane compound and Mg and reacts with iodine (Patent Document 1: paragraph [0058]); a method in which iodophenylene and a certain Grignard reagent are ...

Method for producing arene compounds and arene compounds produced by the same

Provided is a method for producing (alkyl)arene compounds represented by Formulae 3-1, 3-2, and 3-3 by the Friedel-Crafts alkylation reaction of alkyl halide compounds and arene compounds using organic phosphine compounds as a catalyst.

SILYLATED POLYISOCYANATES

The present invention relates to silylated polyisocyanates, to processes for preparing them, to their use, and to coating compositions comprising them. 1. A process for preparing a polyisocyanate comprising a silyl group , the process comprising: reacting at least one compound (A) , which is a di- or polyisocyanate with at least one compound (B) , which is an unsaturated alcohol comprising a C═C double bond and a hydroxyl group to obtain a polyisocyanate comprising a urethane group , andsubsequently adding at least one compound (C), which is a silane compound comprising a Si—H bond, by a hydrosilylation, to at least some of the C═C double bonds bonded to the resultant polyisocyanate comprising the urethane group.2. The process according to claim 1 , wherein the di- or polyisocyanate comprises a aliphatic or cycloaliphatic diisocyanate or polyisocyanate which is obtained by reacting at least one aliphatic or cycloaliphatic diisocyanate.3. The process according to claim 2 , wherein the diisocyanate is selected from the group consisting of hexamethylene 1 claim 2 ,6-diisocyanate claim 2 , 1 claim 2 ,3-bis(isocyanatomethyl)cyclohexane claim 2 , isophorone diisocyanate claim 2 , and 4 claim 2 ,4′- or 2 claim 2 ,4′-di(isocyanatocyclohexyl)methane.4. The process according to claim 1 , wherein the compound (A) is a polyisocyanate comprising an isocyanurate group claim 1 , a biuret group claim 1 , a urethane group claim 1 , and/or an allophanate group.5. The process according to claim 1 , wherein the compound (A) is selected from the group consisting of a polyisocyanate comprising isocyanurate groups and derived from hexamethylene 1 claim 1 ,6-diisocyanate claim 1 , and a polyisocyanate comprising isocyanurate groups and derived from isophorone diisocyanate.7. A process according to claim 1 , wherein the compound (C) is selected from the group consisting of triethylsilane claim 1 , triisopropylsilane claim 1 , dimethylphenylsilane claim 1 , diethoxymethylsilane claim 1 , ...

POLYENE COMPOUND, PREPARATION METHOD AND USE THEREOF

Disclosed are a polyene compound, preparation method and use thereof. Provided in the present invention is the preparation method of a polyene compound I, comprising the following steps: under an action of a base and in an organic solvent, conducting a Witting reaction on a compound II and a compound III to obtain the polyene compound I. By the preparation method in the present invention, a coupling reaction results in good product purity without producing an obvious by-product and involves no heavy metal, thus facilitating a control over product quality and costs, having a simple operation and mild reaction condition, enabling high reaction conversion, a high yield, few by-products, high resultant product purity, low production costs and simple post-processing, and being suitable for industrial production. 3. The preparation method of the polyene compound I according to claim 2 , wherein:in the preparation method of the polyene compound I, the organic solvent is an ether solvent;or,in the preparation method of the polyene compound I, the volume-to-mass ratio of the organic solvent to the compound II is 5 mL/g-50 mL/g;or,in the preparation method of the polyene compound I, the base is an organic base;or,in the preparation method of the polyene compound I, the molar ratio of the base to the compound II is 0.8-1.5;or,in the preparation method of the polyene compound I, the molar ratio of the compound III to the compound II is 0.8-1.5;or,in the preparation method of the polyene compound I, the temperature of the Wittig-Horner reaction is −80° C. to −50° C.;or,in the preparation method of the polyene compound I, the reaction time of the Wittig-Horner reaction is 0.5 h-5.0 h;or,the preparation method of the polyene compound I is carried out in the presence of an inert gas;or,the preparation method of the polyene compound I is carried out under anhydrous conditions;or,the preparation method of the polyene compound I comprises step 1 or step 2,step 1: adding a base into a ...

Novel ceramide analogues, processes for preparing same and uses thereof

Compounds, ceramide analogues, having a cyclic structure derived from cyclopropane, cyclobutane or cyclopentane, the ring bearing two chains consisting of an amide function. Each amide function is attached to the ring by the nitrogen atom of the function and carries a hydrocarbon chain derived from a fatty acid. The amide functions can be cis or trans relative to one another. Processes for the preparation of these novel compounds as well as pharmaceutical and/or cosmetic compositions containing them.

Method of Synthesizing Siloxane Monomers and Use Thereof

A method for preparation and polymerization of siloxane monomers of Formula I is presented. The synthesis includes the selective reaction between silanol containing unit and alkoxy containing units in the presence of basic catalyst. The siloxane monomers of the invention can be used for preparation of siloxane polymers with good flexibility and cracking threshold, and functional sites, useful for applications requiring low metal content in semiconductor industry. 2. The method according to claim 1 , wherein the basic catalyst has a pKb of 2 to 8.3. The method according to claim 1 , wherein the basic catalyst is selected from the group consisting of ammonia claim 1 , pyridine claim 1 , picoline claim 1 , ethanolamine claim 1 , methylamine claim 1 , dimethylamine claim 1 , trimethylamine claim 1 , ethylamine claim 1 , diethylamine claim 1 , triethylamine claim 1 , isopropylamine claim 1 , diisopropylamine claim 1 , diisopropylethylamine claim 1 , propylamine claim 1 , butylamine claim 1 , and sec-butylamine.4. The method according to claim 1 , wherein the silanol containing silane of Formula II is selected from the group consisting of diethylsilanediol claim 1 , dimethylsilanediol claim 1 , dipropylsilanediol claim 1 , diisopropylsilanediol claim 1 , dibutylsilanediol claim 1 , di-tert-butylsilanediol claim 1 , di-iso-butylsilanediol claim 1 , di-sec-butyl-silanediol claim 1 , diphenylsilanediol claim 1 , dicyclohexylsilanediol claim 1 , cyclohexylmethylsilanediol claim 1 , cyclohexylethylsilanediol claim 1 , 1 claim 1 ,1 claim 1 ,3 claim 1 ,3-tetramethyldisiloxane-1 claim 1 ,3-diol or 1 claim 1 ,1 claim 1 ,3 claim 1 ,3-tetraphenyldisiloxane-1 claim 1 ,3-diol claim 1 , 1 claim 1 ,1 claim 1 ,3 claim 1 ,3 claim 1 ,5 claim 1 ,5-hexaphenyltrisiloxane-1 claim 1 ,5-diol claim 1 , bis(p-vinylphenyl)silanediol claim 1 , (p-vinylphenyl)phenylsilanediol claim 1 , phenylvinylsilanediol claim 1 , or 1-adamantylsilanetriol.5. The method according to claim 1 , wherein the ...

SILANE MIXTURES AND PROCESSES FOR PREPARATION THEREOF

The invention relates to silane mixtures comprising a silane of the formula I 1. Silane mixture comprising a silane of the formula I{'br': None, 'sup': 1', '2', '3', '4', '5, 'sub': y', '3-y', 'n, '(R)(R)Si—R—(S—R)—S—R\u2003\u2003(I)'} {'br': None, 'sup': 1', '2', '3', '4', '3', '1', '2, 'sub': y', '3-y', 'z', 'y', '3-y, '(R)(R)Si—R—(S—R)—S—R—Si(R)(R)\u2003\u2003(II)'}, 'and a silane of the formula II'}{'sup': 1', '6', '7', '6', '7, 'sub': 'r', 'where Rare the same or different and are C1-C10-alkoxy groups, phenoxy group, C4-C10-cycloalkoxy groups or alkyl polyether group —O—(R—O)—Rwhere Rare the same or different and are a branched or unbranched, saturated or unsaturated, aliphatic, aromatic or mixed aliphatic/aromatic divalent C1-C30 hydrocarbon group, r is an integer from 1 to 30 and Ris an unsubstituted or substituted, branched or unbranched monovalent alkyl, alkenyl, aryl or aralkyl group,'}{'sup': '2', 'Rare the same or different and are C6-C20-aryl groups, C1-C10-alkyl groups, C2-C20-alkenyl group, C7-C20-aralkyl group or halogen,'}{'sup': '3', 'Rare the same or different and are a branched or unbranched, saturated or unsaturated, aliphatic, aromatic or mixed aliphatic/aromatic divalent C1-C30 hydrocarbon group,'}{'sup': '4', 'Rare the same or different and are a branched or unbranched, saturated or unsaturated, aliphatic, aromatic or mixed aliphatic/aromatic divalent C1-C30 hydrocarbon group,'}{'sup': 5', '8', '8, 'Ris hydrogen or a —C(═O)—Rgroup with R=hydrogen, a C1-C20-alkyl group, C6-C20-aryl groups, C2-C20-alkenyl group, C7-C20-aralkyl group,'}and n is 1, 2 or 3, y are the same or different and are 1, 2 or 3, z is 1, 2 or 3,and the molar ratio of silane of the formula I to silane of the formula II is 20:80-90:10.2. Silane mixture according to claim 1 , characterized in that n is 1 and z is 1.3. Silane mixture according to claim 1 , characterized in that the silane of the formula I is (EtO)Si—(CH)—(S—(CH))—S—C(═O)—Rand the silane of the formula II is ( ...

Preparation of Phenol- or Thiophenyl-Sulfonic Acid Functionalized Solid Acids

Some aryl sulfonic acid-functionalized solids were prepared by a new method. The catalytic activities of esterification by the prepared aryl sulfonic acid-functionalized solids were also tested. 1. A method of preparing an aryl sulfonic acid-functionalized solid , comprising:forming a 3-arylpropyl trimethoxysilane by reacting 3-chloropropyl trimethoxysilane with an aromatic compound;forming an aryl-functionalized solid by grafting the 3-arylpropyl trimethoxysilane onto an inorganic solid material having free —OH groups thereon in an organic solvent under a reflux condition; andforming an aryl sulfonic acid-functionalized solid by sulfonating the aryl-functionalized solid by a sulfonating agent.2. The method of claim 1 , wherein the aromatic compound is phenol claim 1 , alkyl phenol claim 1 , thiophene claim 1 , or alkyl thiophene.3. The method of claim 1 , wherein the inorganic solid material is silica gel claim 1 , porous silica claim 1 , or Zr(OH)powders.4. The method of claim 1 , wherein the organic solvent is toluene claim 1 , xylene claim 1 , ethylbenzene claim 1 , or octane.5. The method of claim 1 , wherein the aryl-functionalized solid is sulfonated at 60-90° C. for 6-36 hours.6. The method of claim 1 , wherein the sulfonating agent is concentrated sulfuric acid claim 1 , a mixture of oleum and concentrated sulfuric acid claim 1 , or SOCl.7. A method of preparing an aryl sulfonic acid-functionalized solid claim 1 , comprising:forming a 3-arylpropyl trimethoxysilane by reacting 3-chloropropyl trimethoxysilane with an aromatic compound;forming an aryl-functionalized solid by co-condensing the 3-arylpropyl trimethoxysilane and a precursor of an inorganic solid by a hydrothermal reaction; andforming an aryl sulfonic acid-functionalized solid by sulfonating the aryl-functionalized solid in concentrated sulfuric acid.8. The method of claim 7 , wherein the aromatic compound is phenol claim 7 , alkyl phenol claim 7 , thiophene claim 7 , or alkyl thiophene.9. The ...

Silicon-containing azodicarboxamides, their preparation and use

A silicon-containing azodicarboxamide is obtainable by reacting an azodicarboxy compound with an aminosilane. The silicon-containing azodicarboxamides are suitable for use in cable sheathing, hoses, drive belts, conveyor belts, roll coverings, footwear soles, ring seals and damping elements. 1. A silicon-containing azodicarboxamide of the general formula I{'br': None, 'sup': 1', '2', '1', '1', '1', '1', '1', '2, 'sub': x', '(3-x)', 'x', '(3-x), '(A)(A)Si—R—N(D)—CO—N═N—CO—N(D)—R—Si(A)(A)\u2003\u2003(I),'}{'sup': 1', '1', '1, 'sub': 2', 'w, 'wherein Ais an alkyl polyether group —O—(CR)—O—),-Alk, wherein v=1-60, w=1-20, each Ris independently H, a phenyl group, an unbranched alkyl group or a branched alkyl group,'}{'sub': 1', '35, 'Alk is a branched or unbranched, saturated or unsaturated, substituted or unsubstituted, aliphatic, aromatic or mixed aliphatic/aromatic monovalent C-Chydrocarbon group,'}{'sup': '2', 'sub': 2', '25', '6', '35', '7', '35', '7', '35, 'each Ais independently a branched or unbranched alkyl, a branched or unbranched alkoxy, a branched or unbranched C-Calkenyloxy, a C-Caryloxy group, a branched or unbranched C-Callcylaryloxy group, a branched or unbranched C-Caralkyloxy group or a hydroxyl group (—OH),'}{'sup': '1', 'sub': 1', '18', '5', '18', '6', '18, 'each Dis independently an H or an Alk′ wherein Alk′ is a C-Calkyl group, a C-Ccycloalkyl group or a C-Caryl group,'}{'sup': '1', 'sub': 1', '30, 'each Ris independently a branched or unbranched, saturated or unsaturated, aliphatic, aromatic or mixed aliphatic/aromatic divalent C-Chydrocarbon group which is optionally substituted by F—, Cl—, Br—, I—, —CN or HS—, and'}wherein an average polyether fraction x=1.3-1.7.2. The silicon-containing azodicarboxamide according to claim 1 , wherein Ais —O—((CH)—O—)CH.3. The silicon-containing azodicarboxamide according to claim 1 , wherein the silicon-containing azodicarboxamide is at least one selected from the group consisting of [(CH(—O—CH—CH)—O—)(EtO)Si—( ...

METHOD OF PRODUCING BERAPROST

An improved method is described for making single isomers of synthetic benzoprostacyclin analogue compounds, in particular the pharmacologically active 314-d isomer of beraprost. In contrast to the prior art, the method is stereoselective and requires fewer steps than the known methods for making these compounds. 16-. (canceled)8. The process of claim 7 , wherein Rand Reach independently represent trimethylsilyl claim 7 , triethylsilyl claim 7 , t-butyldimethylsilyl claim 7 , t-butyldiphenylsilyl claim 7 , phenyldimethylsilyl claim 7 , or tetrahydropyranyl.9. The process of claim 7 , wherein the cycloaddition of step (1) is an inverse electron demand Diels Alder reaction followed by thermal decarboxylation.10. The process of claim 7 , wherein the aromatization step (2) is treatment of the compound of formula (IV) with palladium on carbon.12. The process of claim 11 , wherein the compound of formula (VII) is produced as a substantially pure single isomer.14. The compound of claim 13 , wherein Rand Rare each CH.1520-. (canceled) This application claims priority from U.S. Provisional Application No. 61/497,754, filed Jun. 16, 2011, the entirety of which is incorporated herein by reference.The present application relates to a process for selectively producing single-isomer benzoprostacyclin derivatives including beraprost and its derivatives.The present invention also relates to a novel process for attaching the alpha side-chain to single-isomer key intermediate leading to beraprost and related derivatives.Prostacyclin derivatives are useful pharmaceutical compounds possessing activities such as platelet aggregation inhibition, gastric secretion reduction, lesion inhibition, and bronchodilation. Beraprost is a synthetic benzoprostacyclin analogue of natural prostacyclin that is currently under clinical trials for the treatment of pulmonary hypertension and vascular disease (excluding renal disease) in North America and Europe.Beraprost and related benzoprostacyclin ...

NITROGEN-CONTAINING CYCLIC ORGANOXYSILANE COMPOUND AND METHOD FOR PRODUCING THE SAME

A nitrogen-containing cyclic organoxysilane compound having a formula (1): 3. The method for producing the nitrogen-containing cyclic organoxysilane compound of claim 2 , wherein the reaction is performed in presence of a basic catalyst or an acidic catalyst. This non-provisional application claims priority under 35 U.S.C. § 119(a) on Patent Application No. 2018-221342 filed in Japan on Nov. 27, 2018, the entire contents of which are hereby incorporated by reference.The present invention relates to a nitrogen-containing cyclic organoxysilane compound and a method for producing the same, and more specifically, the present invention relates to a nitrogen-containing cyclic organoxysilane compound useful as, for example, a silane coupling agent, a surface treatment agent, a resin additive, a paint additive, an adhesive, and the like, and a method for producing the same.A silane compound having an amino group is useful as a silane coupling agent, a surface treatment agent, a resin additive, a paint additive, an adhesive, and the like. As such a silane compound having an amino group, for example, there are known organoxysilane compounds having primary amino groups such as aminopropyltrimethoxysilane and aminopropyltriethoxysilane, organoxysilane compounds having secondary amino groups such as N-phenylaminopropyltrimethoxysilane, and organoxysilane compounds having tertiary amino groups such as dimethylaminopropyltrimethoxysilane and diethylaminopropyltriethoxysilane.However, since each of these silane compounds has a methoxy group or an ethoxy group as an organoxy group bonded to a silicon atom, when used as a silane coupling agent, a surface treatment agent, a resin additive, a paint additive, an adhesive, or the like, the silane compound generates a low-boiling-point alcohol such as methanol or ethanol, so-called a volatile organic compound, through hydrolysis reaction, which may increase the environmental burden and harm the health of the user.In recent years, as ...

SELECTIVE OLEFIN METATHESIS WITH CYCLOMETALATED RUTHENIUM COMPLEXES

This invention relates generally to C—H activated ruthenium olefin metathesis catalyst compounds which are stereogenic at the ruthenium center, to their preparation, and the use of such catalysts in the metathesis of olefins and olefin compounds. In particular, the invention relates to the use of C—H activated ruthenium olefin metathesis catalyst compounds in Z-selective olefin metathesis reactions, enantio-selective olefin metathesis reactions, and enantio-Z-selective olefin metathesis reactions. The invention has utility in the fields of catalysis, organic synthesis, polymer chemistry, and industrial and fine chemicals chemistry. 2. The olefin metathesis catalyst complex claim 1 , according to claim 1 , wherein:{'sup': '1', 'sub': 1', '6', '1', '6, 'Ris C-Calkyl, C-Calkoxy, or halide;'}{'sup': '2', 'sub': 2', '6', '1', '6', '2', '2', '3', '5', '8', '5', '8', '1', '6', '1', '6, 'Ris C-Calkyl, substituted C-Calkyl, (e.g., CFH, CFH, CF, etc.), C-Ccycloalkyl, C-Csubstituted cycloalkyl, heteroatom-containing hydrocarbyl, or substituted heteroatom-containing hydrocarbyl, where the substituents are selected from C-Calkyl, C-Calkoxy, or halide;'}{'sup': 4', '5', '6', '7', '8, 'R, R, R, Rand Rare independently hydrogen;'}Y is O;{'sub': 1', '6, 'Z is C-Calkyl;'}n is 1; and{'sup': 1', '−, 'sub': 3', '2, 'Xis NO or t-BuCO.'}3. The olefin metathesis catalyst complex claim 2 , according to claim 2 , wherein:{'sup': '1', 'Ris Me, OMe or F;'}{'sup': '2', 'sub': '3', 'Ris MeO, iPr, Me, F, or CF; and'}Z is i-Pr.4. The olefin metathesis catalyst complex claim 2 , according to claim 2 , wherein:{'sup': '1', 'Ris Me, OMe, or F;'}{'sup': '2', 'sub': '3', 'Ris MeO, Me, iPr, or CF;'}Z is i-Pr; and{'sup': 1', '−, 'sub': '3', 'Xis NO.'}5. The olefin metathesis catalyst complex claim 2 , according to claim 2 , wherein:{'sup': '1', 'Ris MeO, Me or F;'}{'sup': '2', 'sub': '3', 'Ris MeO, iPr, Me or CF;'}Z is i-Pr; and{'sup': '1', 'sub': '2', 'Xis t-BuCO.'}7. A method for performing an enantio- ...

SILANE AND SILICIC ACID (HETERO)POLYCONDENSATE HAVING AROMATIC COMPOUNDS LINKED VIA COUPLING GROUPS WHICH ARE SUITABLE AS OR FOR MATRIX SYSTEMS HAVING HIGH TRANSLUCENCY AND GOOD MECHANICAL PROPERTIES

The present invention relates to compounds and silicic acid (hetero)polycondensates comprising structures of formulas (1) and/or (2), 120-. (canceled)22. Silicic acid (hetero)polycondensate comprising structures of formula (1) claim 21 , (2) claim 21 , or (3) as claimed in claim 21 , further comprising a particulate filler dispersed therein.23. Silicic acid (hetero)polycondensate comprising structures of formula (1) claim 22 , (2) claim 22 , or (3) as claimed in claim 22 , wherein the silicic acid (hetero)polycondensate and the filler have a refractive index difference Δin the region of ±0.001 claim 22 , preferably of ±0.0005.24. Silicic acid (hetero)polycondensate comprising structures of formula (1) claim 21 , (2) claim 21 , or (3) claim 21 , as claimed in claim 21 , in the form of bulk materials claim 21 , composites claim 21 , cements claim 21 , adhesives claim 21 , casting compounds claim 21 , coating materials claim 21 , adhesion promoters claim 21 , fillers claim 21 , fibers claim 21 , and priming materials for fillers of fibers claim 21 , preferably in the field of optics or dental applications.25. Silicic acid (hetero)polycondensate comprising structures of formula (1) claim 22 , (2) claim 22 , or (3) claim 22 , as claimed in claim 22 , in the form of bulk materials claim 22 , composites claim 22 , cements claim 22 , adhesives claim 22 , casting compounds claim 22 , coating materials claim 22 , adhesion promoters claim 22 , fillers claim 22 , fibers claim 22 , and priming materials for fillers of fibers claim 22 , preferably in the field of optics or dental applications.26. Compound mixture or silicic acid (hetero)polycondensate according to claim 21 , comprising(i) a compound or structures as specified in formula (1) and a compound or structures of formula (2), or(ii) a compound or structures as specified in formula (1) and a compound or structures of formula (3), or(iii) a compound or structures as specified in formula (1), a compound or structure of ...

Guanidine-Functionalized Particles and Methods of Making and Using

Guanidine-functionalized particles and methods of making and using such particles. 1. A guanidine-functionalized silica gel particle , comprising:{'sub': n', 'm, 'claim-text': where —O is an oxygen atom that is covalently bonded to the surface of the silica gel particle,', 'n is 1, 2 or 3,', 'S is a spacer group comprising a backbone with m atoms,', 'm is 2-16, inclusive,', {'sub': '2', 'claim-text': 'and wherein the guanidine group is charged and comprises an associated counterion and wherein the counterion does not comprise a halogen.', 'G is a guanidine group of the formula NH—C(NH)—NH,'}], 'a silica gel particle comprising at least one ligand comprising a guanidine group, the ligand comprising the formula —OSi—S-G,'}2. The particle of wherein all m atoms of the backbone of the spacer group S are carbon atoms.3. The particle of wherein m=3.4. The particle of wherein the spacer group S comprises a secondary amine.5. The particle of wherein the guanidine group is the reaction product of a primary amine and O-methylisourea hemisulfate.6. The particle of wherein the silica gel particle comprises a particle size of about 25-100 microns and a pore size of about 60-2000 Angstroms.7. The particle of wherein the ligand is the reaction product of one or more hydroxyl groups of the silica particle with one or more reactive groups of a silane coupling agent moiety of the ligand.8. The particle of wherein the counterion that is associated with the guanidine group is a sulfate ion.9. The particle of wherein the counterion that is associated with the guanidine group is a bisulfate ion.10. The particle of wherein the counterion that is associated with the guanidine group is a hydroxide ion.11. The particle of wherein the guanidine group is the reaction product of a primary amine with O-methylisourea hemisulfate.12. The particle of wherein residual hydroxyl groups are present on the surface of the particle.13. The particle of wherein each ligand has only a single guanidine group. ...

Modifier, Method For Preparing The Same, And Modified Conjugated Diene-Based Polymer Including The Same

The present invention relates to a modifier useful for the modification of a conjugated diene-based polymer, having excellent affinity with a filler, and capable of improving the compounding properties of a conjugated diene-based polymer, a method for preparing the same, a modified conjugated diene-based polymer including the modifier, and a method for preparing the polymer. 2. The modifier of claim 1 , whereinin Formula 1,{'sub': '1', 'Ris an alkyl group of 1 to 20 carbon atoms, an alkenyl group of 2 to 20 carbon atoms, an alkynyl group of 2 to 20 carbon atoms, a heteroalkyl group of 1 to 20 carbon atoms, a cycloalkyl group of 5 to 20 carbon atoms, an aryl group of 6 to 20 carbon atoms, or a heterocycle of 3 to 20 carbon atoms, which is substituted with the substituent X or unsubstituted,'}{'sub': 2', '3, 'Ris a hydrogen atom; or —Si(R),'}{'sub': 3', '4, 'Rand Rare each independently the substituent represented by Formula 1a,'}B is N or S,{'sub': 1', '3', '3', '4, 'if B is S, Ris an alkyl group of 1 to 20 carbon atoms, an alkenyl group of 2 to 20 carbon atoms, an alkynyl group of 2 to 20 carbon atoms, a heteroalkyl group of 1 to 20 carbon atoms, a cycloalkyl group of 5 to 20 carbon atoms, an aryl group of 6 to 20 carbon atoms, or a heterocycle of 3 to 20 carbon atoms, which is substituted with a nitro group among the substituent X; or a heteroalkyl group of 1 to 20 carbon atoms or a heterocycle of 3 to 20 carbon atoms, which is unsubstituted, and only Ramong Rand Ris present.'}5. The method for preparing a modifier of claim 4 , wherein the compound represented by Formula 2 and the compound represented by Formula 3 react in a molar ratio of 1:0.8 to 1:1.2.6. The method for preparing a modifier of claim 4 , wherein the compound represented by Formula 4 and the alkaline compound are each independently added in 1.0 to 2.0 moles with respect to 1 mol of the compound represented by Formula 2.7. The method for preparing a modifier of claim 4 , wherein the alkaline ...

PROCESS FOR THE PREPARATION OF 4-AMINO-1-((1S,4R,5S)-2-FLUORO-4,5-DIHYDROXY-3-HYDROXYMETHYL-CYCLOPENT-2-ENYL)-1H-PYRIMIDIN-2-ONE

Processes for the preparation of 4-amino-1-((1S,4R,5S)-2-fluoro-4,5-dihydroxy-3-hydroxymethyl-cyclopent-2-enyl)-1H-pyrimidin-2-one (13, RX-3117) and its intermediates are described. 2. The process of claim 1 , wherein the acid is HCl.3. The process of claim 1 , further comprising isolating substantially pure 4-amino-1-((1S claim 1 ,4R claim 1 ,5S)-2-fluoro-4 claim 1 ,5-dihydroxy-3-(hydroxymethyl)-cyclopent-2-en-1-yl)-pyrimidin-2(1H)-one (13).5. The process of claim 4 , further comprising isolating substantially pure 4-amino-1-(3aS claim 4 ,4S claim 4 ,6aR)-5-fluoro-2 claim 4 ,2-dimethyl-6-((trityloxy)methyl)-4 claim 4 ,6a-dihydro-3aH-cyclopenta[d][1 claim 4 ,3]dioxol-4-yl)pyrimidin-2(1H)-one (12).7. The process of claim 6 , further comprising preparing (3aS claim 6 ,4R claim 6 ,6aR)-5-fluoro-2 claim 6 ,2-dimethyl-6-((trityloxy)methyl)-4 claim 6 ,6a-dihydro-3aH-cyclopenta[d][1 claim 6 ,3]dioxol-4-ol (10) by deprotection of tert-butyl(((3aR claim 6 ,4R claim 6 ,6aR)-5-fluoro-2 claim 6 ,2-dimethyl-6-((trityloxy)methyl)-4 claim 6 ,6a-dihydro-3aH-cyclopenta[d][1 claim 6 ,3]dioxol-4-yl)oxy)diphenylsilane (9).8. A process for the preparation of tert-butyl(((3aR claim 6 ,4R claim 6 ,6aR)-5-fluoro-2 claim 6 ,2-dimethyl-6-((trityloxy)methyl)-4 claim 6 ,6a-dihydro-3aH-cyclopenta[d][1 claim 6 ,3]dioxol-4-yl)oxy)diphenylsilane (9) comprising:reacting tert-butyl(((3aR,4R,6aR)-5-iodo-2,2-dimethyl-6-((trityloxy)methyl)-4,6a-dihydro-3aH-cyclopenta[d][1,3]dioxol-4-yl)oxy)diphenylsilane (8) with NFSI (N-fluorobenzenesulfonimide) to obtain tert-butyl(((3aR,4R,6aR)-5-fluoro-2,2-dimethyl-6-((trityloxy)methyl)-4,6a-dihydro-3aH-cyclopenta[d][1,3]dioxol-4-yl)oxy)diphenylsilane (9).9. The process of claim 8 , further comprising preparing tert-butyl(((3aR claim 8 ,4R claim 8 ,6aR)-5-iodo-2 claim 8 ,2-dimethyl-6-((trityloxy)methyl)-4 claim 8 ,6a-dihydro-3aH-cyclopenta[d][1 claim 8 ,3]dioxol-4-yl)oxy)diphenylsilane (8) by reacting (3aS claim 8 ,4R claim 8 ,6aR)-5-iodo-2 claim 8 ,2-dimethyl-6-(( ...

Silicon dioxide composite particle with far-infrared radioactivity; precursor of the same and application thereof

The present invention relates to a silicon dioxide composite particle with far-infrared radioactivity, which is formed by the hydrolysis, condensation and polymerization of an organic silane precursor having the structure of the formula (I) with a tetra-alkoxysilane. The high stability of organic silane precursor compounds and the low biotoxicity of silicon dioxide composite particles make the present far-infrared radioactive silicon dioxide composite particles of great potential for extensive use in related bio-products. A-R 1 —Si(OR 2 ) 3    Formula (I)

SYSTEMS AND PROCESSES FOR PRODUCING ORGANIC ACIDS DIRECTLY FROM BETA-LACTONES

Provided herein are reactor systems and processes for producing organic acids directly from beta-lactones. Such reactor systems and processes involve the use of a heterogeneous catalyst, such as a zeolite at vapor phase conditions. The reactor systems and processes may use a fixed bed, moving bed or fluidized contacting zone as reactor configurations. 2. The process of claim 1 , wherein the heterogenous catalyst comprises a microporous solid.3. The process of claim 1 , wherein the microporous solid is selected from the group consisting of alkaline-earth phosphates claim 1 , supported phosphate salts claim 1 , calcium hydroxyapatites claim 1 , inorganic salts claim 1 , metal oxides claim 1 , and zeolites claim 1 , or any combination thereof.4. The process of any one of to claim 1 , wherein the heterogenous catalyst comprises an alumina-silicate molecular sieve having Lewis or Brönsted acidity.5. The process of claim 1 , wherein the heterogenous catalyst comprises a zeolite.6. (canceled)7. The process of claim 5 , wherein the zeolite catalyst is in a hydrogen form or in metal cation exchanged form.8. The process of claim 7 , wherein the metal cation is Na claim 7 , K claim 7 , Ca claim 7 , Mg claim 7 , Cu claim 7 , or Cu.9. The process of claim 1 , wherein the at least one organic acid product is produced continuously.10. The process of claim 1 , wherein the at least one beta-lactone reagent is introduced to the at least one reaction vessel combined with a solvent.11. The process of claim 1 , wherein the at least one reaction vessel further comprises a continuous fixed-bed reactor operating at a reduced pressure.12. The process of claim 1 , wherein the at least one reaction vessel further comprises a continuous fixed-bed reactor configured for receiving at least one beta-lactone reagent diluted with inert gas.13. The process of claim 1 , wherein the least one reaction vessel further comprises a fluidized bed reactor configured to receive at least one beta-lactone ...

COMPOUNDS FROM ANTRODIA CAMPHORATE AND THEIR USE IN TREATMENT OF DIABETES MELLITUS

The present invention relates to a method or composition for treating diabetes mellitus, comprising administering a subject with a pharmaceutical composition comprising a therapeutically effective amount of an active compound from , such as antroquinonols, and a pharmaceutically acceptable carrier. In addition, the prevent invention provides a new process for the total synthesis of antroquinonol. Also provided are the new compounds produced during the process for preparing of antroquinonol. 2. (canceled)3. The method of claim 1 , wherein the compound having the general formula (I) is antroquinonol.4. The method of claim 1 , wherein the compound having the general formula (I) is (+)-antroquinonol.5. The method of claim 1 , wherein the compound having the general formula (I) is (−)-antroquinonol.6. (canceled)7. The method of claim 1 , wherein the diabetes mellitus is type 2 diabetes mellitus.8. The method of claim 1 , wherein the subject is a patient suffered from diabetes mellitus with insulin resistance.9. The method of claim 1 , wherein the compound having the general formula (I) is effective for improving glucose uptake.10. The method of claim 1 , wherein the compound having the general formula (I) provides an effect on the glycemic control.11. The method of claim 1 , wherein antroquinonol is effective for inhibiting Dipeptidyl peptidase-4 (DPP4) activity and enhancing AMP-activated protein kinase (AMPK) activation.12. The method of claim 1 , wherein antroquinonol provides synergistic effects in combination of and insulin.13. A process for preparation of antroquinonol comprising the steps of asymmetric addition of diethyl zinc claim 1 , Claisen rearrangement claim 1 , ring-closing metathesis claim 1 , and lactonization.15. (canceled)17. A pharmaceutical composition for treating diabetes mellitus comprising the compound of .18. A pharmaceutical composition for treating diabetes mellitus comprising insulin or an insulin analogue in combination of the compound of ...

Convenient process for the preparation of statins

Object of the present invention is an improved process for the preparation of key intermediates for the synthesis of statins.

METHOD FOR PRODUCING CARBAMATOORGANOSILANES

Carbamatoorganosilanes are produced in exceptionally high yield with a high degree of purity, by reacting an aminoorganosilane with a dialkylcarbonate in the presence of a basic catalyst, wherein a first reaction period proceeds at a temperature in the range of 35-65° C., followed by a later reaction period at a temperature at least 10° C. higher. A low level of catalyst allows its removal by simple exit filtration, without a separate filtration step. 19.-. (canceled)11. The process of claim 10 , where the radical Ris an unsubstituted monovalent hydrocarbon radical having from 1 to 6 carbon atoms.12. The process of claim 10 , wherein the radical Ris an substituted alkyl radical having from 1 to 4 carbon atoms.13. The process of claim 10 , wherein the radical Ris an unsubstituted alkylene radical having from 1 to 6 carbon atoms.14. The process of claim 10 , wherein the temperature during the first reaction period is from 45° C. to 65° C.15. The process of claim 10 , wherein the temperature during the later reaction period is at least 20° C. higher than in the first reaction period.16. The process of claim 10 , wherein the aminosilanes of the formula (4) and the dialkyl carbonates of the formula (5) are used in a mole ratio of from 1.0:1.0 to 1.0:2.0.17. The process of claim 10 , wherein a metal alkoxide is used as a catalyst.18. The process of claim 10 , wherein the content of the catalyst is not more than 0.2% by weight claim 10 , based on the weight of the total reaction mixture. This application is the U.S. National Phase of PCT Appln. No. PCT/EP2014/069818 filed Sep. 17, 2014, which claims priority to German Application No. 10 2013 218 972.9 filed Sep. 20, 2013, the disclosures of which are incorporated in their entirety by reference herein.1. Field of the InventionThe invention relates to a process for preparing carbamatoorganosilanes from corresponding aminoorganosilanes and dialkyl carbonate.2. Description of the Related ArtVarious processes for preparing 3- ...

CROSS-METATHESIS REACTION OF FUNCTIONALIZED AND SUBSTITUTED OLEFINS USING GROUP 8 TRANSITION METAL CARBENE COMPLEXES AS METATHESIS CATALYSTS

The invention pertains to the use of Group 8 transition metal carbene complexes as catalysts for olefin cross-metathesis reactions. In particular, ruthenium and osmium alkylidene complexes substituted with an N-heterocyclic carbene ligand are used to catalyze cross-metathesis reactions to provide a variety of substituted and functionalized olefins, including phosphonate-substituted olefins, directly halogenated olefins, 1,1,2-trisubstituted olefins, and quaternary allylic olefins. The invention further provides a method for creating functional diversity using the aforementioned complexes to catalyze cross-metathesis reactions of a first olefinic reactant, which may or may not be substituted with a functional group, with each of a plurality of different olefinic reactants, which may or may not be substituted with functional groups, to give a plurality of structurally distinct olefinic products. The methodology of the invention is also useful in facilitating the stereoselective synthesis of 1,2-disubstituted olefins in the cis configuration. 27-. (canceled)9. The method of claim 8 , wherein:M is Ru;{'sup': 1', '2, 'sub': 3', '2', '3', '2', '2', '2', '3', '3', '3', '2', '3', '3', '3', '2, 'Xand Xare independently selected from the group consisting of halide, CFCO, CHCO, CFHCO, (CH)CO, (CF)(CH)CO, (CF)(CH)CO, PhO, MeO, EtO, tosylate, mesylate, and trifluoromethanesulfonate;'}{'sup': 1', '2, 'sub': 1', '20', '2', '20, 'Ris hydrogen and Ris selected from the group consisting of C-Calkyl, C-Calkenyl, and aryl;'}L is a neutral electron donor ligand selected from the group consisting of phosphine, phosphite, phosphinite, phosphonite, ether, amine, amide, imine, carboxyl, pyridine, substituted pyridine, imidazole, and substituted imidazole;{'sup': 3', '4, 'Rand Rare aromatic, substituted aromatic, heteroaromatic, substituted heteroaromatic, alicyclic, substituted alicyclic, heteroatom-containing alicyclic, or substituted heteroatom-containing alicyclic, composed of from one ...

Therapeutic compounds

The invention provides compounds useful as anti-cancer agents.

METHOD OF PRODUCING BERAPROST

An improved method is described for making single isomers of synthetic benzoprostacyclin analogue compounds, in particular the pharmacologically active 314-d isomer of beraprost. In contrast to the prior art, the method is stereoselective and requires fewer steps than the known methods for making these compounds. 120-. (canceled)22. The method of claim 21 , wherein Ris initially a Calkyl.23. The method of claim 22 , wherein Ris initially a methyl or ethyl.24. The method of claim 21 , wherein said converting comprises a base hydrolysis of an ester at the Rposition.25. The method of claim 24 , wherein the base hydrolysis comprises reacting the ester with sodium hydroxide.26. The method of claim 21 , wherein said converting comprises converting Rinto H and then converting H into the cation.27. The method of claim 21 , wherein each of the substantially pure ester compound and the salt of the substantially pure beraprost has an isomeric purity of at least 90%.28. The method of claim 21 , wherein each of the substantially pure ester compound and the salt of the substantially pure beraprost has an isomeric purity of at least 95%.29. The method of claim 21 , wherein each of the substantially pure ester compound and the salt of the substantially pure beraprost has an isomeric purity of at least 98%.30. The method of claim 21 , wherein each of the substantially pure ester compound and the salt of the substantially pure beraprost has an isomeric purity of at least 99%.31. The method of claim 21 , wherein each of the substantially pure ester compound and the salt of the substantially pure beraprost has an isomeric purity of more than 99%.32. The method of claim 21 , wherein the cation is K.33. The method of claim 32 , wherein each of the substantially pure ester compound and the salt of the substantially pure beraprost an isomeric purity of at least 90%.34. The method of claim 32 , wherein each of the substantially pure ester compound and the salt of the substantially pure ...

NOVEL METAL COMPLEXES, ESPECIALLY THE RUTHENIUM COMPLEXES, AND USE THEREOF

The object of the invention is a novel metal complex of the formula (1), the parameters of which are as defined in the description of the invention, as well as use of the metal complex of the formula (1) in the olefin metathesis reactions. 2. The complex according to claim 1 , characterised in thatM is ruthenium;{'sup': 1', '11', '12', '17', '18', '19′', '20′', '21′', '22′', '11', '12', '11', '17′', '18′', '19′', '12', '20′', '21', '22′, 'sub': 1', '25', '1', '25', '2', '25', '4', '16', '4', '10', '4', '12, 'Lis a N-heterocyclic carbene ligand, where R, R, R′, R′, R, R, R, and R are independently hydrogen, C-Calkyl, C-Calkoxy, or C-Calkenyl, where Rand Rmay be joined together to form a cyclic C-Csystem, optionally the substituents R, R, R, R and/or the substituents R, R, R′, R may be joined together to form a substituted or unsubstituted cyclic C-Cor polycyclic C-Csystem;'}{'sup': 13', '14', '15', '16', '13', '14', '15', '16, 'sub': 1', '25, 'R, R, R,and Rare independently hydrogen or C-Calkyl, where Rand/or Rmay be joined to Rand/or R, to form a cyclic system;'}n is 0 or 1;{'sup': 2', '17', '18', '19', '17', '18', '19', '17', '18', '19', '2, 'sub': 1', '12', '1', '12', '3', '12', '5', '12', '5', '12', '5', '12', '1', '12', '1', '12', '1', '12, 'Lis described by the formula P(R)(R)(R), where R, Rand Rare independently C-Calkyl, C-Calkoxy, C-Ccycloalkyl, C-Caryl, C-Caryloxy, or C-Cheteroaryl, where two substituents selected from R, Rand Rmay be joined together to form a cyclic or polycyclic system; or also Lis selected from the group comprising nitrogen-containing heterocycles, such as 1,2,3-triazole, 1,3,4-triazole, pyridine, 4-(N,N/-dimethylamino)pyridine (DMAP), piperidine, morpholine, thiomorpholine, pyridazine, pyrimidine, pyrazine, piperazine, 1,2,3-triazine, 1,2,4-triazine, 1,3,5-triazine, quinoline, isoquinoline, quinuclidine, phthalazine, indoline, thiazole, benzothiazole, benzimidazole, purine, 1,8-naphthyridine, quinoxaline, pteridine, carbazole, phenazine ...

Hydrophilic Organosilanes

The present disclosure relates to compositions comprising an organosilane having the formula; (R)n(RO) (3.n)SiRO(CHCHO)a(CHO)b Rwhere n is 1 or 2, a≧1, b may vary from 0 to 30, with the proviso a≧b, Ris a hydrocarbon group containing 1 to 12 carbon atoms, Ris hydrogen or an alkyl group containing 1 to 6 carbon atoms, Ris a divalent hydrocarbon group containing 2 to 12 carbon atoms, Ris hydrogen, R, or an acetyl group. The present organosilane compositions are particularly useful to treat various surfaces to render them more hydrophilic. 1. A composition comprising an organosilane having the formula;{'br': None, 'sup': 1', '2', '3', '4, 'sub': (3-n)', 'n', '2', '2', 'a', '3', '6', '6, '(R)(RO)SiRO(CHCHO)(CHO)R'}wheren is 1 or 2,a≧1, b may vary from 0 to 30, with the proviso a≧b,{'sup': '1', 'Ris a hydrocarbon group containing 1 to 12 carbon atoms,'}{'sup': '2', 'Ris hydrogen or an alkyl group containing 1 to 6 carbon atoms,'}{'sup': '3', 'Ris a divalent hydrocarbon group containing 2 to 12 carbon atoms,'}{'sup': 4', '1, 'Ris hydrogen, R, or an acetyl group.'}2. The composition of where n is 2.3. The composition of where a ranges from 4 to 30.4. The composition of where Ris methyl and Ris methyl or ethyl.5. The composition of where Ris propylene or —CHCHC(CH)—.6. The composition of where the organosilane has the average formula{'br': None, 'sub': 3', '3', '2', '2', '2', '2', '2', '2', '2', '7', '3, '(CH)(CHCHO)SiCHCHCHO(CHCHO)CH, or'}{'br': None, 'sub': 3', '3', '2', '2', '2', '3', '2', '2', '4', '18', '3', '6', '18, '(CH)(CHO)SiCHCHC(CH)O(CHO)(CHO)H.'}7. A process for preparing an organosilane composition comprising reacting:{'sup': 1', '2, 'sub': (3-n)', 'n, 'claim-text': where', {'sup': '1', 'Ris an alkyl group containing 1 to 4 carbon atoms,'}, {'sup': '2', 'Ris an alkyl group containing 1 to 4 carbon atoms,'}, 'the subscript n is 1 or 2,, 'a) an organosilane of the formula (R)(RO)H,'}{'sup': 5', '4, 'sub': 2', '2', 'a', '3', '6', 'b, 'claim-text': [{'sup': 4', '1 ...

PRODUCTION METHOD FOR ORGANIC SILICON COMPOUND HAVING KETIMINE STRUCTURE

An organic silicon compound having a ketimine structure having good storage stability can be obtained by a production method that produces an organic silicon compound having a ketimine structure indicated by formula (1) 2. The method of wherein step (II) is conducted after step (I).3. The method of wherein step (II) of reducing a chlorine content includes using an inorganic adsorbent.4. The method of wherein the inorganic adsorbent is at least one compound selected from silica claim 3 , aluminum hydroxide claim 3 , hydrotalcite claim 3 , magnesium silicate claim 3 , aluminum silicate claim 3 , aluminum oxide claim 3 , and magnesium oxide.5. The method of wherein Ris methyl or ethyl claim 1 , Ris isobutyl claim 1 , Ris methyl claim 1 , and both m and n are 3. This invention relates to a method for preparing an organosilicon compound having a ketimine structure.Silane coupling agents are compounds including both a moiety which is reactive with inorganic matter (i.e., silicon-bonded hydrolyzable group) and another moiety which is fully reactive with and soluble in organic matter, within their molecule. They are widely used as a resin modifier.Among these, silane coupling agents having a ketimine structure are under study as a modifier for conjugated diene copolymers (Patent Document 1).The ketimine structure-bearing organosilicon compounds, however, have poor storage stability and turn to active hydrogen-containing organosilicon compounds with a lapse of time, which can adversely affect a composition having the relevant compound admixed.It is thus desired to improve the storage stability of ketimine structure-bearing organosilicon compounds.An object of the invention, which has been made under the above-mentioned circumstances, is to provide a method for preparing a ketimine structure-bearing organosilicon compound which is improved in storage stability.Making extensive investigations to attain the above object, the inventors have found that a ketimine structure- ...

Amidite compound and method for producing polynucleotide using said compound

The present invention provides an amidite compound represented by formula (1) which enables a synthesis of RNA with high purity, and the method for preparing a polynucleotide by using the same compound. (In the formula (1), wherein R represents the following formula (wherein Ra and Rb are identical to or different from each other and each represents a methyl group, an ethyl group, or a hydrogen atom, with the proviso that Ra and Rb does not represent a hydrogen atom, n is an integer of 1 to 5), and Ba represents a group containing optionally protected nucleobase structure, and G1 and G2 are identical to or different from each other and each represents a protecting group for a hydroxy group, and G3 are identical to or different from each other and each represents an alkyl group.

ASYMMETRIC SYNTHESIS OF ORGANIC COMPOUNDS

The present invention provides processes for the production of chiral compounds in a stereoisomeric excess. The present processes involve reacting a hydrometallated alkene compound with a compound comprising a conjugated-bond system under conditions such that the compounds undergo an asymmetric 1,4- or 1,6-conjugate addition reaction, generating a chiral compound in a stereoisomeric excess. The reaction is performed in the presence of a metal catalyst, which catalyst preferably comprises a non-racemic chiral ligand. 1. A process for producing a chiral compound in a stereoisomeric excess , the process comprising:(i) contacting a first compound comprising an alkene bond with a hydrometallating agent, wherein the first compound and the hydrometallating agent are contacted under conditions such that the first compound is hydrometallated by said hydrometallating agent; and(ii) contacting the hydrometallated first compound with a second compound, wherein the second compound comprises a conjugated π-bond system which is capable of undergoing a 1,4-conjugate addition reaction and which has a carbon atom at said 4-position, wherein the hydrometallated first compound and the second compound are contacted under conditions such that they undergo an asymmetric 1,4-conjugate addition reaction in which a carbon atom of said hydrometallated first compound binds to the carbon atom at said 4-position of the second compound, forming a stereoisomeric excess of a compound having a chiral carbon atom at said 4-position, wherein said asymmetric conjugate addition reaction is performed in the presence of a metal catalyst comprising a non-racemic chiral ligand.4. A process according to claim 2 , wherein Ris hydrocarbyl optionally substituted with 1 claim 2 , 2 claim 2 , 3 claim 2 , 4 or 5 R claim 2 , e.g. Ris alkyl claim 2 , cycloalkyl or aralkyl claim 2 , any of which is optionally substituted with 1 claim 2 , 2 claim 2 , 3 claim 2 , 4 or 5 R.5. (canceled)6. A process according to claim 2 ...

[N]CYCLOPARAPHENYLENES (CCP),MACROCYCLE INTERMEDIATES AND METHODS OF MAKING SAME

The present invention provides the compound [6]-cycloparaphenylene, cycloparaphenylene intermediates (e.g. [n]macrocycles), and methods for making [n]cycloparaphenylenes and [n]cycloparaphenylene intermediates in quantities not previously available. The cycloparaphenylene compounds and their intermediates can be useful in nanotube preparation and in the preparation of other supramolecular structures. 151.-. (canceled)54. The compound of claim 53 , wherein A is oxygen.55. The compound of claim 53 , wherein X is bromine.56. The compound of claim 53 , wherein subscript n is an integer from 1 to 5.57. The compound of claim 53 , wherein each Ris independently methyl or ethyl.58. The compound of claim 53 , wherein each Ris independently hydrogen claim 53 , methyl or ethyl.61. The method of claim 60 , wherein the group —ORis a silyl ether.62. The method of claim 61 , wherein Ris tert-butyldimethylsilyl.63. The method of any of claims 60 , wherein X is bromine.64. The method of any of claims 60 , wherein M is lithium.65. The method of any of claims 60 , wherein A is oxygen.66. The method of any of claims 60 , wherein subscript m is 0 claims 60 , 1 or 2.67. The method of any of claims 60 , wherein subscript f is 0 claims 60 , 1 claims 60 , 2 or 3.68. The method of any of claims 60 , wherein each Ris independently methyl or ethyl.69. The method of any of claims 60 , wherein each Ris independently hydrogen claims 60 , methyl or ethyl.72. The method of claim 71 , wherein each X is bromine73. The method of claim 71 , wherein M is lithium.74. The method of claim 71 , wherein A is oxygen.75. The method of claim 71 , wherein n is 1 claim 71 , 2 or 3.76. The method of claim 71 , wherein p is 1 or 2.77. The method of claim 71 , wherein each Ris independently methyl or ethyl.78. The method of claim 71 , wherein each Ris independently hydrogen claim 71 , methyl or ethyl.80. A composition comprising at least two molecules of 6-cycloparaphenylene interacting to form a structure.81. The ...

A process for the preparation of palbociclib

The present invention relates to a process for the preparation of palbociclib utilizing a silyl-protected crotonic acid derivative to produce a silyl-protected 2-chloro-4-(cyclopentylamino)-5-(1-methyl-2-carboxy-ethen-1-yl)pyrmidine followed by intramolecular cyclization of the pyrmidine intermediate to produce 2-chloro-8-cyclopentyl-5-methyl-8H-pyrido[2,3-d]pyrimidin-7-one which is then converted to palbociclib.

Guanidine-Functionalized Particles and Methods of Making and Using

Guanidine-functionalized particles and methods of making and using such particles. 1. A method of making a guanidine-functionalized particle , comprising: [{'br': None, 'sub': n', '3-n', 'm, 'sup': 'a', '(RO)RSi—S—X'}, 'where RO is an alkoxy group comprising one or two carbons, or is an acetoxy group,', 'where n is 1, 2 or 3,', {'sup': 'a', 'where Ris an unreactive group,'}, 'where S is a spacer group comprising a backbone with m atoms,', 'm is from 2-16, inclusive, and', 'where X is a primary amine that is capable of reacting with the O-methylisourea to form a guanidine group;, 'reacting O-methylisourea hemisulfate with a linker molecule comprising the formula'}and,reacting at least one of the RO groups of the linker molecule with a hydroxyl group of the particle to form a covalent bond between the linker molecule and the particle.2. The method of wherein the (RO)Si moiety comprises a trimethoxysilane moiety.3. The method of wherein the linker molecule is 3-aminopropyltrimethoxysilane.4. The method of wherein the (RO)Si moiety comprises a triethoxysilane moiety.5. The method of wherein all m atoms of the backbone of the spacer group S are carbon atoms.6. The method of wherein m=3.7. The method of wherein the spacer group S comprises at least one hetero atom.8. The method of wherein the spacer group S comprises at least one secondary amine.9. The method of wherein the linker molecule is N-(2-aminoethyl)-3-aminopropyltrimethoxysilane.10. The method of wherein the step of reacting at least one of the RO groups of the linker molecule with a hydroxyl group of the particle to form a covalent bond between the linker molecule and the particle claim 1 , is performed after the reacting of the O-methylisourea hemisulfate with the linker molecule.11. The method of wherein the step of reacting at least one of the RO groups of the linker molecule with a hydroxyl group of the particle to form a covalent bond between the linker molecule and the particle claim 1 , is performed ...

PROCESS FOR PREPARING POLYSULFANE SILANES

Process for preparing polysulfane silanes of the formula I 2. Process for preparing polysulfane silanes of the formula I according to claim 1 , characterized in that the process is carried out at temperatures from 0° C. to 180° C.3. Process for preparing polysulfane silanes of the formula I according to claim 1 , characterized in that the polysulfane silanes of the formula I are [(EtO)Si(CH)]S claim 1 , [(EtO)Si(CH)]S claim 1 , [(EtO)Si(CH)]S claim 1 , [(EtO)Si(CH)]S claim 1 , [(EtO)Si(CH)]S claim 1 , [(EtO)Si(CH)]S claim 1 , [(EtO)Si(CH)]S claim 1 , [(EtO)Si(CH)]S claim 1 , [(EtO)Si(CH)]Sor [(EtO)Si(CH)]S.4. Process for preparing polysulfane silanes of the formula I according to claim 1 , characterized in that the process steps a and b are carried out in parallel.5. Process for preparing polysulfane silanes of the formula I according to claim 1 , characterized in that the process is carried out continuously or batchwise.6. Process for preparing polysulfane silanes of the formula I according to claim 1 , characterized in that claim 1 , if carried out in a batchwise operation claim 1 , the wash solution in process step a originates from step d of a previous batch7. Process for preparing polysulfane silanes of the formula I according to claim 1 , characterized in that claim 1 , in process step d claim 1 , the washed solid may be separated from the wash solution using solid-bowl decanter centrifuges claim 1 , filter dryers claim 1 , filter presses or filter centrifuges.8. Process for preparing polysulfane silanes of the formula I according to claim 1 , characterized in that a wetting agent is added before or during the process steps.9. Process for preparing polysulfane silanes of the formula I according to claim 1 , characterized in that the removal of solvent by distillation in process step b takes place in a temperature range from 0° C. to 150° C. at a pressure from 0.5 kPa absolute to 150 kPa absolute. The invention provides a process for preparing polysulfane ...

An aqueous, storage-stable composition containing N-benzyl-substituted N-(2-aminoethyl)-3-aminopropylsiloxane hydrochlorides, processes for production thereof and use thereof

An aqueous composition contains N-benzyl-substituted N-(2-aminoethyl)-3-aminopropylsiloxane hydrochlorides, wherein the composition after storage for 6 weeks at 60° C. has a color number of ≤1 Gardner, a content of methanol of ≤0.5% by weight, an active substance content of ≤60% by weight, and a content of water of ≥40% to ≤60% by weight, and wherein the components in the composition sum to 100% by weight. 1: An aqueous composition , comprising:an active substance comprising N-benzyl-substituted N-(2-aminoethyl)-3-aminopropylsiloxane hydrochlorides,whereinthe composition after storage for 6 weeks at 60° C. has a color number of ≤1 Gardner,a content of methanol of ≤0.5% by weight,an active substance content of ≤60% by weight, anda content of water of ≥40% to ≤60% by weight, andwherein components in the composition sum to 100% by weight.2: The composition according to claim 1 , wherein the active substance comprises N-benzyl-substituted N-(2-aminoethyl)-3-aminopropylsiloxane hydrochlorides as a mixture of isomeric N-benzyl-substituted N-(2-aminoethyl)-3-aminopropylsiloxanes claim 1 , wherein at least one of the isomeric N-benzyl-substituted N-(2-aminoethyl)-3-aminopropylsiloxanes conforms to formula (I);{'br': None, 'sub': (1−y)', 'y', '(1−z)', 'z', 'x, 'HO(RO)[(A)SiO(OH)(OR)]—R \u2003\u2003(I),'}wherein R represents methyl or ethyl,x≥1,y=0 or 1 and z=0 or 1,with the proviso that (y+z)≤1, and {'br': None, 'sub': 2', '3', '(1−a)', 'a', '2', '2', '[2−(b+c)]', 'b', 'c', 'd, 'sup': 1', '2', '3, '[—(CH)N(HR)(CH)(NHRR)].(HCl)\u2003\u2003(II),'}, 'A represents an aminoalkyl group according to formula (II),'}where a=0 or 1,b=0 or 1 or c=0 or 1,with the proviso that (b+c)=0, 1, or 2,{'sup': 1', '2', '3, 'wherein groups R, R, and Rrepresent benzyl, and'}d=0, 1, 2, or 3.3: The composition according to claim 1 , wherein the composition is storage-stable for at least 12 months at room temperature.4: The composition according to claim 1 , wherein the composition is storage-stable ...

TERMINAL ALKENE MONOISOMERIZATION CATALYSTS AND METHODS

The invention provides novel catalysts and methods of using catalysts for controlling the position of a double bond and cis/trans-selectivity in isomerization of terminal alkenes to their 2-isomers. Catalysts such as (pentamethylcyclopentadienyl)Ru formulas 1 and 3 having a bifunctional phosphine can be used in the methods. A catalyst loading of 1 mol % of formulas 1+3 can be employed for the production of (E)-2-alkenes at 40-70° C.; lower temperatures can be used with higher catalyst loading. Acetonitrile-free catalysts can be used at lower loadings, room temperature, and in less than a day to accomplish the same results as catalysts 1+3. The novel catalyst systems minimize thermodynamic equilibration of alkene isomers, so that the trans-2-alkenes of both non-functionalized and functionalized alkenes can be generated. 2. The catalyst of wherein Ris iso-propyl claim 1 , iso-butyl claim 1 , tert-butyl or 1-adamantyl.3. The catalyst of wherein Ris alkyl nitrile claim 1 , cycloalkyl nitrile claim 1 , aryl nitrile claim 1 , heteroaryl nitrile claim 1 , heterocycloalkyl nitrile claim 1 , alkylcarbonyl claim 1 , CO claim 1 , alkylamine claim 1 , alkenylamine claim 1 , arylamine claim 1 , amide claim 1 , alkanol claim 1 , water claim 1 , (C-C)-alkenol claim 1 , cycloalkanol claim 1 , aryl alcohol claim 1 , ketone claim 1 , ether claim 1 , aldehyde claim 1 , alkene claim 1 , halo claim 1 , carboxylate claim 1 , sulfonyl claim 1 , sulfonate claim 1 , phosphonyl claim 1 , phosphinyl claim 1 , or N.4. The catalyst of wherein Ris carbonyl claim 3 , CO claim 3 , alkylamine claim 3 , alkenylamine claim 3 , arylamine claim 3 , amide claim 3 , alkanol claim 3 , water claim 3 , (C-C)-alkenol claim 3 , cycloalkanol claim 3 , aryl alcohol claim 3 , ketone claim 3 , ether claim 3 , aldehyde claim 3 , alkene claim 3 , halo claim 3 , carboxylate claim 3 , sulfonyl claim 3 , sulfonate claim 3 , phosphonyl claim 3 , phosphinyl claim 3 , or N.5. The catalyst of wherein Ris acetonitrile ...