ПРОИЗВОДНОЕ 2-АМИНОПРОПАН-1,3-ДИОЛА, ЕГО ФАРМАЦЕВТИЧЕСКОЕ ПРИМЕНЕНИЕ И ПРОМЕЖУТОЧНЫЕ ПРОДУКТЫ ДЛЯ ИХ СИНТЕЗА

Описывается производное 2-аминопропан-1,3-диола общей формулы где R1, R2, R3 и R4 одинаковы или различны, и каждый обозначает водород или прямой или разветвленный алканоил, содержащий от 1 до 6 атомов углерода; его фармацевтически приемлемая соль добавления кислоты или гидрат; фармацевтическая композиция, обладающая иммуносупрессивной активностью; 2-амино-2-(2-(4-(1-гидрокси-5-фенилпентил)фенил)этил) пропан-1,3-диол или его производное, где аминогруппа защищена алифатической ацильной группой и/или гидроксигруппа защищена трет-бутилдиметилсилильной группой, а также 2-амино-2-(2-(4-формилфенил)этил)-пропан-1,3-диол, его производное, где аминогруппа и/или гидроксигруппа защищены алифатической группой и/или гидроксигруппа защищена трет-бутилдиметилсилильной группой. Ввиду небольшой токсичности, высокой безопасности и иммуносупрессивного действия, эти производные могут использоваться в качестве предупреждающих или подавляющих реакцию отторжения при пересадке органов и для профилактики или лечения ...

Полиаминные аналоги в качестве цитотоксических агентов

... 1. Цитотоксический полиаминный аналог, имеющий структуру R1-X-R2, где R1 и R2 - независимо Н или радикал, выбранный из группы, включающей прямой или разветвленный C1-10 алифатический, алициклический, одно- или многокольцевой ароматический, одно- или многокольцевой арил-замещенный алифатический, алифатически замещенный одно- или многокольцевой ароматический, одно- или многокольцевой гетероциклический, одно- или многокольцевой гетероциклически замещенный алифатический и алифатически замещенный ароматический, а также их галогенированные формы; Х - полиамин с двумя концевыми аминогруппами, -(CH2)3-NH- или -СН2-Ph-СН2-, при этом R1 и R2 - не являются одновременно незамещенными бензиловыми радикалами. 2. Аналог по п.1, отличающийся тем, что Х выбирают из группы, содержащей путресцин, спермидин и спермин. 3. Аналог по п.1, отличающийся тем, что Х является путресцином. 4. Аналог по п.3, отличающийся тем, что указанная структура представляет собой соединение, которое выбрано из группы, включающей ...

СПОСОБ ПОЛУЧЕНИЯ α,β-ДИХЛОРКОРИЧНЫХ АЛЬДЕГИДАМИНОВ

Способ получения N-(антрахинонил-1)-w-аминоалифатических альдегидов и кетонов

Способ получения 5-[3-(бицикло[2.2.1]-гепт-2-илокси)-4-метоксифенил]гексагидро-2-пиримидинона

Изобретение относится к гетероциклическим соединениям, в частности к получению (бицикло 2.2„ ij-гепт- 2-илокси) -4-метоксиФенилТгексагидро- 2-пиримидинона, который может найти применение в медицине. Дель изобретения - разработка способа получения указанных соединений. Получение ведут циклизацией соответственно замещенного глутарамида в реакционно- инертном растворителе при комнатной температуре в присутствии тетрааце- тата свинца. I IB ...

Способ получения пиридиловых или фениловых соединений,или их гидрохлоридов,или сложных эфиров

Изобретение относится к гетероциклическим соединениям, в частности к способу получения пиридиповых или фениловых соединений общей формулы ...

Способ получения пиридиловых соединений или их солей, или сложных эфиров, или амидов

Изобретение касается гетероциклических соединений, в частности получения пиридиловых соединений общей формулы CH=CH-CH=C-(R1C(O)OH)-N=C-CA-(C6H4-пара-R2)-CHB-CH2-N-(CH2)N+2, где R1- -CH=CH- или -CH2-CH2- R2-C1-C4-алкил A и B - каждый в отдельности H или AC-CB означает C=C N=1-3, или их солей, или, когда R1-группа -CH=CH-, а AC-CB-группа -C=C-, их сложных эфиров или амидов, проявляющих антигистаминную активность, что может быть использовано в медицине. Цель - создание новых более активных соединений указанного класса. Синтез ведут дегидратацией соединения формулы: CH=CH-CH=C(CH=CH-C(O)OR3)-N=C-C(OH) (C6H4-пара-R2)-CH2-CH2-N-(CH2)N+2, где R2и N - См. выше R3-C1-C4-алкил. Полученное соединение, где AC-CB-группа -C=C-, в случае необходимости гидрируют с получением соединения, где AC-CB-группа -CH=CH- и R1-группа -CH2-CH2-. Целевой продукт выделяют в виде свободной кислоты или соли, или, когда AC-CB - группа -C=C- и R1-группа -CH=CH-, в виде сложного эфира или амида. Новые соединения по антигистаминной ...

Verfahren zur Hydrierung von Cyanopropanaldehyden enthaltend Cyanopropionaldehydacetalen

Synthesis of aldehyde, useful as intermediate for pharmaceutical and agricultural products and as flavoring agent, involves reacting carboxylic acid or its ester with hydrogen in the presence of a catalyst

Synthesis of aldehyde (I) involves reacting carboxylic acid (II) or its ester with hydrogen and water in gaseous phase, in the presence of a catalyst containing at least 60-99.9 weight% (wt.%) of zirconium oxide and 20 wt.% or less of lanthanides as catalyst active ingredients. Synthesis of aldehyde of formula (I) involves reacting carboxylic acid of formula (II) or its ester with hydrogen and water in the presence of a catalyst containing at least 60-99.9 wt.% of zirconium oxide and 20 wt.% or less of lanthanides as catalyst active ingredients. R<1>, R<2>, R<3>, R<4> = hydrogen, 1-6C alkyl, 3-8C cycloalkyl, aryl, 7-12C alkylphenyl or 7-12C phenylalkyl, preferably R<1>, R<2> together form 3-7C alicyclic ring, and preferably R<1>, R<3> = 1-4C alkoxy, phenoxy, methylamino, dimethylamino or halogen, more preferably R<1> = hydroxy or amino.

COMPOUNDS USEFUL IN OLEAGINOUS COMPOSITIONS

New derivatives of 6-(4-phenylbutoxy)hexylamine and process for producing salmeterol.

New derivatives of benzocycloheptene, their method of preparation and the compositions pharmaceutical containing them.

PROCEDURE AND INTERMEDIATE PRODUCTS FOR the PRODUCTION OF (1R, 2S, 5S) - 6,6-DIMETHYL-3-AZABICYCLOÄ3,1,0 ÜHEXAN-2-CARBOXYLATEN OR SALTS OF it

BASIC PHENYLACETALDEHYDE, YOUR PRODUCTION AND THESE CONTAINING DRUGS SUBSTITUTED.

DERIVATIVES OF BENZOCYCLOHEPTEN, PROCEDURES FOR YOUR PRODUCTION AND IT CONTAINING DRUGS.

LEUCOTRIEN ANTAGONIST.

ACETYLENE DERIVATIVES WITH ENZYMINHIBIERENDER EFFECT, THEIR PRODUCTION AND THEIR USE AS DRUGS.

HALOGENALKYLPHENYL ALCOHOLS, - KETONE AND THEIR HYDRATES.

SUBSTITUTED ALKYL DIAMINE DERIVATIVES AND YOUR USE AS TACHYKININ AN ANTAGONIST

POLYAMINE-SIMILAR AS CYTOTOXIC ACTIVE SUBSTANCES

PROCEDURE FOR THE PRODUCTION OF RETROVIAL PROTEASE RESTRAINING INTERMEDIATE PRODUCTS

New derivatives of 6-(4-phenylbutoxy)hexylamine and process for producing salmeterol

Substituted alkyldiamine derivatives and their use as tachykinin antagonists

N-ARYL(THIO)ANTHRANILIC ACID AMIDE DERIVATIVES, THEIR PREPARATION AND THEIR USE AS VEGF RECEPTOR TYROSINE KINASE INHIBITORS

Described are compounds of formula (I), wherein W is O or S; X is NR8; Y is CR9R10-(CH2)n wherein R9 and R10 are independently of each other hydrogen or lower alkyl, and n is an integer of from and including 0 to and including 3; or Y is SO2; R1 is aryl; R2 is a mono- or bicyclic heteroaryl group comprising one or more ring nitrogen atoms with the exception that R2 cannot represent 2- phthalimidyl, and in case of Y = SO2 cannot represent 2,1,3-benzothiadiazol-4- yl; any of R3, R4, R5 and R6, independently of the other, is H or a substituent other than hydrogen; and R7 and R8, independently of each other, are H or lower alkyl; or a N-oxide or a pharmaceutically acceptable salt thereof for the preparation of a pharmaceutical product for the treatment of a neoplastic disease which responds to an inhibition of the VEGF receptor tyrosine kinase activity. The compounds of formula (I) can be used for the treatment e.g. of a neoplastic disease, such as a tumor disease, of retinopathy and age-related ...

PROCESS FOR THE PREPARATION OF 4-PHENYLPYRROLE DERIVATIVES

3,3-DISUBSTITUTED PROPYLAMINES, THEIR USE AND PREPARATION

The invention relates to novel com-pounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, R7 and Ar are as defined in claim 1, their salts with physiologically ac-ceptable acids and, when the compounds can be in the form of optical isomers, the racemic mixture and the individual enantiomers. The compounds have anticholinergic activity, and the invention also relates to the compounds of Formula (I) for use as therapeutically ac-tive substances, pharmaceutical compositions containing compounds of Formula (I), the use of the compounds of Formula (I) for preparing anticholinergic drugs, the use of the compounds of Formula (I) for treating urinary incontinence, and methods for preparing the compounds of Formula (I). ...

NOVEL COMPOUNDS, THEIR USE AND PREPARATION

The invention relates to novel compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, R7 and Ar are as defined in claim 1, their salts with physiologically acceptable acids and, when the compounds can be in the form of optical isomers, the racemic mixture and the individual enantiomers. The compounds have anticholinergic activity, and the invention also relates to the compounds of Formula (I) for use as therapeutically active substances, pharmaceutical compositions containing compounds of Formula (I), the use of the compounds of Formula (I) for preparing anticholinergic drugs, the use of the compounds of Formula (I) for treating urinary incontinence, and methods for preparing the compounds of Formula (I).

BICYCLIC AROMATIC COMPOUNDS, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL AND COSMETIC COMPOSITIONS CONTAINING THEM.

СПОСОБ ПОЛУЧЕНИЯ ДИАРИЛПИРИДИНОВ, ПОЛЕЗНЫХ В КАЧЕСТВЕ ИНГИБИТОРОВ COX-2

Изобретение относится к способу получения соединений формулы I, полезных при лечении заболеваний, опосредуемых циклооксигеназой-2. Отчет о международном поиске был опубликован 1999.05.20.

ANTHRANILIC ACID AMIDES AND USE THEREOF AS MEDICAMENTS

NEW UNSATURATED AMINES, THEIR PREPARATION AND THEIR USE AS DRUGS

SYNTHESIS OF AMINO-ALKOXY-HEPTANOIC ALKYL ESTER

The present invention relates to a process (Mukaiyama Aldol reaction) for thepreparation of compounds of formula (I) wherein R is C alkyl, C cycloalkyl-C alkyl or aryl-C alkyl; R is C alkyl, benzyl, substituted benzyl or allyl; R is C alkyl or allyl; R is C alkyl, allyl, benzyl or substituted benzyl; R ' is benzyl or substituted benzyl; or R and R together form a (CH)-group.12344141-43-61-41-41-41-41-423 © KIPO & WIPO 2007 ...

A cationic lipid

The present invention provides a cationic lipid which can be used for a delivery of a nucleic acid into the cytoplasm of a cell. The cationic lipid of the present invention is, for an example, a compound or a pharmaceutically acceptable salt thereof represented by the following formula (1).

PROCESS FOR PREPARATION OF 2-(3-DIISOPROPYLAMINO-1-PHENYLPROPYL)-4-HYDROXYMETHYL-PHENOL, A METABOLITE OF TOLTERODINE

The present invention relates to processes for preparation of 2-(3-diisopropylamino-1-phenylpropyl)-4-hydroxymethyl-phenol of Formula I, which is a metabolite of tolterodine.

NEW DERIVATIVES OF 6-(4-PHENYLBUTOXY)HEXYLAMINE AND PROCESS FOR PRODUCING SALMETEROL

L'invention concerne de nouveaux dérivés de la 6-(4-phénylbutoxy)hexylamine de formule générale (I) dans laquelle: R¿1 désigne CHO ou CHOR¿3OR¿4, où R¿3 et R¿4 sont indépendamment un alkyle C¿1-C¿6, aralkyle ou forment des acétals cycliques à 5 ou 6 membres; R¿2 désigne H, benzyle ou un groupe alkyloxycarbonyle, aryloxycarbonyle, aralkyloxycarbonyle ou acyle; et son procédé d'obtention. L'invention concerne aussi un nouveau procédé d'obtention de salmétérol ou ses sels pharmaceutiquement acceptables consistant à mettre un composé organométallique en réaction avec un composé de formule générale (I) dans lequel R¿1 désigne CHO et R¿2 désigne un alkyloxycarbonyle, aryloxycarbonyle, aralkyloxycarbonyle ou un groupe acyle .

N-ARYL(THIO)ANTHRANILIC ACID AMIDE DERIVATIVES, THEIR PREPARATION AND THEIR USE AS VEGF RECEPTOR TYROSINE KINASE INHIBITORS

L'invention concerne des composés représentés par la formule (I), un N-oxyde, ou l'un de leurs sels pharmaceutiquement acceptables, servant à la préparation d'un produit pharmaceutique pour le traitement des maladies néoplasiques réagissant à l'inhibition de l'activité tyrosine kinase du récepteur VEGF. W représente O ou S; X représente NR¿8; Y représente CR¿9R¿10-(CH¿2)¿n où R¿9 et R¿10 sont, indépendamment l'un de l'autre, hydrogène ou alkyle de faible poids moléculaire; et n est un entier de 0 à 3; ou bien Y représente SO¿2; R¿1 représente l'aryle; R¿2 représente un groupement hétéroaryle monocyclique ou bicyclique comprenant un ou plusieurs atomes d'azote cycliques à l'exception près que R¿2 ne doit pas être 2-phtalimidyle et, dans le cas où Y représente SO¿2, R¿2 ne doit pas représenter 2,1,3-benzothiadazol-4-yl; R3, R4, R5, R6, quels qu'ils soient représentent indépendamment les uns des autres, H ou substitut autre que l'hydrogène et R¿7 et R¿8 représentent, indépendamment l'un de ...

AMINE DERIVATIVES

L'invention concerne des dérivés d'amine représentés par la formule générale (1), ou leurs sels. Dans la formule, R1¿ est alkyle en C¿1-4; R2¿ représente (i), ou (ii); (iii); R3¿ est alkyle en C¿1-3 , alkyle en C¿1-5 hydroxylé, acyle en C¿1-5, alcényle en C¿2-5 ou halogéno; et k, l et m sont chacun un nombre entier compris entre 1 et 4. Ces composés possédant d'excellents effets antifongiques sont très utiles comme agents antifongiques, compositions antifongiques, médicaments, etc.

Method of preparing retroviral protease inhibitor intermediates

Chiral hydroxyethylamine, hydroxyethylurea or hydroxyethylsulfonamide isostere containing retroviral protease and renin inhibitors can be prepared by multi-step syntheses that utilize key chiral amine intermediates. This invention is a cost effective method of obtaining such key chiral amine intermediates enantiomerically, diastereomerically and chemically pure. The method is suitable for large scale (multikilogram) productions. This invention also encompasses organic acid and inorganic acid salts of the amine intermediates.

PROCESS FOR PREPARING ( ) TRANS-4-P-FLUOROPHENYL-3-HYDROXYMETHYL-1

The present invention relates to a process for preparing (±)-trans-4-p-fluorophenyl-3-hydroxymethyl-1-methylpiperidine of formula (I). The present invention also relates to novel intermediates of the formula (IX) and (IX') methods for preparing said intermediates and the use of said compounds for preparing Paroxetine and Omiloxetine.

ALKANOLAMINE DERIVATIVE

NEW MATERIAL:A compound of formula I (Ar is naphthyl or indolyl; R is H, lower alkyl, substituted lower alkyl, phenyl, or substituted phenyl; X is H or -COR). EXAMPLE: N-Isopropyl-N-[2-hydroxy-3-(1-naphthoxy)]propyl formamide. USE: An intermediate of a β-blocking agent having antiarrhythmic activity, e.g. propranolol. PROCESS: A compound of formula IV (Y is halogen) is acylated with an acylating agent such as RCOOH or its halide at a temperature between 0°C and the refluxing temp. of the solvent, to obtain a compound III, which is aryloxylated with a compound of formula ArOH in a solvent such as ethanol, in the presence of a base such as NaOH at ≥ room temp. in an inert gas atmosphere such as N2. COPYRIGHT: (C)1980,JPO&Japio ...

3-アミノ-3-シクロブチルメチル-2-ヒドロキシプロピオンアミドまたはその塩の合成のための方法

... 式Iの3-アミノ-3-シクロブチルメチル-2-ヒドロキシプロピオンアミド またはその塩の調製方法は、本明細書に記載の式VIの化合物を、大部分はジメチルスルホキシド(DMSO)を含む溶液中に準備し、本明細書に記載の式VIIの中間体化合物の後処理または単離を行うことなく、この化合物を本明細書に記載の式VIIIの化合物に直接変換するものである。本発明の別の態様は、式Zの(1R,2S,5S)-3-アザビシクロ[3,1,0]ヘキサン-2-カルボキサミド,N-[3-アミノ-1-(シクロブチルメチル)-2,3-ジオキソプロピル]-3-[(2S)-2-[[[1,1-ジメチルエチル)アミノ]カルボニルアミノ]-3,3-ジメチル-1-オキソブチル]-6,6-ジメチルまたはその塩の新規な調製方法である。 ...

N-АРИЛАМИДЫ АНТРАНИЛОВОЙ КИСЛОТЫ И ТИОАНТРАНИЛОВОЙ КИСЛОТЫ

Изобретение относится к бензамидным производным, обладающим ингибирующей активностью в отношении тирозинкиназного Flt-1-рецептора VEGF, которые могут быть использованы для лечения неопластического заболевания. Описывается фармацевтический продукт, включающий соединения группы 2-[(4-пиридил)метил] амино-N-[R1] бензамида, где R1 - 4-хлорфенил, 4-метилфенил, 4-хлор-3-(трифторметил)фенил или 3-(трифторметил)фенил, обладающий ингибирующей активностью в отношении тирозинкиназного Flt5-1-рецептора VEGF, связанного с неопластическим заболеванием и ангиогенезом. Описываются также новые соединения группы 2-[(азотсодержащий гетероцикл)метил] амино-N-[R1] бензамида, где азотсодержащим гетероциклом является 4-пиридил, 4- или 5-хинолинил, 2-имидазолил, и способ их получения. Описывается также фармацевтическая композиция, включающая указанные выше соединения, обладающая ингибирующей активностью в отношении тирозинкиназного рецептора VEGF, для лечения неопластического заболевания. 5 н. и 12 з.п. ф-лы, ...

МАСЛЯНИСТЫЕ КОМПОЗИЦИИ

Сущность изобретения: в качестве присадок к маслянистым композициям могут быть использованы соединения формулыгде B обозначает ароматическую систему, А обозначает гидрокарбильную группу, каждый из Rи Rодинаковые или различные и независимо друг от друга обозначают алифатическую гидрокарбильную группу, содержащую 10-40 углеродных атомов, при условии, что один из Rи Rобозначают водород; z ровно по меньшей мере 1 и где ароматическая система включает в себя по меньшей мере одну замещающую группу , которая является активирующей группой для укольцевой системы, или производное активирующей группы.

6-N,N'-ДИМЕТИЛАМИНОМЕТИЛ-1-ОКСИБЕНЗАЛЬДЕГИД В КАЧЕСТВЕ ОТВЕРДИТЕЛЯ ЭПОКСИДНЫХ СМОЛ И СПОСОБ ЕГО ПОЛУЧЕНИЯ

Изобретение относится к органической химии, а именно - к способу получения нового полифункционального соединения, производного салицилового альдегида - 6,6-N, N-диметиламинометил-1-оксибензальдегида, которое может найти применение в качестве отвердителя эпоксидных смол, в качестве базового вещества для синтеза нового класса органических соединений. Цель изобретения - получение нового полифункционального соединения, производного салицилового альдегида - 6,6-N,N-диметиламинометил-1-оксибензальдегида, которое может найти применение в качестве отвердителя эпоксидных смол, в качестве базового вещества для синтеза нового класса органических соединений, например, в качестве промежуточного продукта для получения пестицидов, стабилизаторов к полимерным материалам и нефтепродуктам. Цель достигается тем, что исходный салициловый альдегид подвергают взаимодействию с N,N-тетраметилметиленбисамином при мольном соотношении салициловый альдегид : N,N-тетраметилметиленбисамин, равном 0,1 - 0,25 : 0,5, при ...

Способ получения N-(антрахинонил-1)-дельта-аминовалерианового альдегида

N-GESCHÜTZTE/N-SUBSTITUIERTE BETA-AMINOHYDROXYSULFONATE

3,3-DIPHENYLPROPYLAMINE, IHRE VERWENDUNG UND HERSTELLUNG

NEUE BICYCLISCHE AROMATISCHE DERIVATE, VERFAHREN ZU IHRER HERSTELLUNG UND IHRE VERWENDUNG IN KOSMETIKA UND IN DER HUMAN- UND TIERMEDIZIN

N-GESCHÜTZTE/N-SUBSTITUTING BETA AMINOHYDROXYSULFONATE

DERIVATIVES the 6 (4-PHENYLBUTOXY) HEXYLAMINS AND PROCEDURES FOR the PRODUCTION OF SALMETEROL

PROCEDURE FOR THE PRODUCTION OF (+) - TRANS-4-PFLUOROPHENYL-3-HYDROXYMETHYL-1-METHYLPIPERIDIN

PROCEDURE FOR THE PRODUCTION OF ALPHA ALKYLAMINOALDEHYDEN.

PROCEDURE FOR the PRODUCTION OF 4-PHENYL-PYRROLDERIVATEN.

USE FROM PEPTIDASE HEMMER TO THE PRODUCTION OF MEDICINES FOR THE TREATMENT OF APOPLEXIES

PROCEDURE FOR THE PRODUCTION OF INTERMEDIATE PRODUCTS, WHICH ARE FOR THE PRODUCTION OF RETROVIRAL PROTEASE RESTRAINING CONNECTIONS USABLE

PROCEDURE FOR THE PRODUCTION OF INTERMEDIATE PRODUCTS, WHICH ARE FOR THE PRODUCTION OF RETROVIRAL PROTEASE RESTRAINING CONNECTIONS USABLE

2-TRIFLUOROMETHYL BENZOCYCLOHEPTANES

BICYCLO 4,2,0 OCTA- 1,3,5-TRIENE-7-METHANAMINES

Method for making intermediates useful in synthesis of retroviral protease inhibitors

BICYCLIC NAPHTHALENIC DERIVATIVES, PROCESS FOR THEIR PREPARATION AND USE IN HUMAN AND VETERINARY MEDICINE

L'invention concerne les composés de formule générale (I) (I) dans laquelle: - A représente un radical méthylène ou diméthylène, substitués ou non par un radical alkyle inférieur, - R1, R2, R3 et R4, identiques ou différents, représentent un atome d'hydrogène ou un radical alkyle inférieur ayant de 1 à 6 atomes de carbone, ou R1 et R3, pris ensemble, forment un pont méthylène ou diméthylène, quand A représente un radical diméthylène, - R' représente un atome d'hydrogène, un radical OH, un radical alkoxy ayant de 1 à 4 atomes de carbone, un radical acyloxy ayant de 1 à 4 atomes de carbone ou un radical amino, - R" représente un atome d'hydrogène ou un radical alkoxy ayant de 1 à 4 atomes de carbone, ou - R' et R", pris ensemble, forment un radical oxo (=O), méthano (=CH2) ou hydroxyimino (=N-OH), et - R représente le radical -CH2OH ou le radical -COR5, R5 représentant un atome d'hydrogène, le radical OR6 où R6 représente un atome d'hydrogène, un radical alkyle ayant de 1 à 20 atomes ...

PROCESS FOR PREPARING 3-DIMETHYLAMINO-2,2- DIMETHYLPROPANAL

An improved process for preparing 3-dimethylamino-2,2-dimethylpropanal from isobutyraldehyde, dimethylamine and a source of formaldehyde is disclosed wherein the process is carried out at a pH value of 9 to 11. 3-Dimethylamino-2,2-dimethylpropanal is useful as an intermediate in the preparation of a variety of compounds such as pharmaceuticals, plant growth hormones, fungicides, herbicides and flotation auxiliaries.

CALCIUM INDEPENDENT CAMP PHOSPHODIESTERASE INHIBITOR ANTIDEPRESSANT

Antidepressant agents having the formula wherein R1 is a polycycloalkyl group; R2 is methyl or ethyl, X is O or NH and Y comprises a 5- or 6-membered heterocyclic ring having one or two nitrogens; or fused bicyclic heterocyclic rings having a total of three nitrogen atoms, one in each ring and one angular nitrogen.

CALCIUM RECEPTOR-ACTIVE COMPOUNDS

The present invention features compounds of general formulae a), b), c), abl e to modulate one or more activities of an inorganic ion receptor and methods for treating diseases or disorders by modulating inorganic ion receptor activity. Preferably, the compound can mimic or block the effect of extracellular Ca2+ on a calcium receptor.

СПОСОБ ПОЛУЧЕНИЯ ДИАРИЛПИРИДИНОВ, ПОЛЕЗНЫХ В КАЧЕСТВЕ ИНГИБИТОРОВ COX-2

... 1. Способ получения соединений формулы 5 в которой R1выбран из группы, включающей (a) СН3 , (b) NH2, (c) NНС(O)СF3, (d) NНСН3; и Аr представляет моно-, ди- или тризамещенный фенил или пиридинил (или его N-оксид), в которых заместители выбраны из группы, включающей (a) водород, (b) галоген, (c) С1-4алкокси, (d) С1-4алкилтио, (e) CN, (f) С1-4алкил, (g) С1-4фторалкил; включающий взаимодействие соединения формулы 13 в которой Х представляет галоген, принадлежащий к группе, включающей йод, хлор, бром и фтор, с соединением формулы 9 с получением соединения формулы 15 и окисление соединения формулы 15 с использованием окисляющего агента и необязательно катализатора и кислоты, с получением соединения формулы 5. 2. Способ по п.1, в котором окисляющий агент принадлежит к группе, включающей перекись водорода, оксон и смесь перекись водорода/уксусная кислота, а кислота представляет уксусную, пропионовую, метансульфоновую кислоту или серную кислоту. 3. Способ по п.1, в котором катализатором является ...

NOVEL DERIVATIVES OF BENZOCYCLOHEPTEN, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

2-AMINOPROPANE-1,3-DIOL COMPOUNDS, MEDICINAL USE THEREOF, AND INTERMEDIATES IN SYNTHESIZING THE SAME

ALDEHYDES THAT PRESENT GROUPS HIDROXILA

ERYTHRO-(E)-3,5-DIHYDROXY-7-[3'-(4''-FLUOROPHENYL)-1'-(1''- -METHYLETHYL)INDOL-2'-YL]-HEPT-6-ENOIC ACID AND PROCESS FOR PREPARING THEREOF

Method of producing amines

A method for producing amines, the method comprising contacting at reactive conditions at least one alcohol, aldehyde or ketone, or a mixture thereof, with an aminating agent in the presence of a catalyst, is improved by employing as the catalyst a composition comprising cobalt, copper, and a third component selected from a group consisting of iron, zinc, zirconium and mixtures thereof.

Bicyclic naphthalenic derivatives, a process for preparing the same and human or veterinary medicines and cosmetic compositions containing said derivatives

A bicyclic naphthalenic compound has the formula (I) wherein A represents methylene or dimethylene, substituted or not by lower alkyl, R1, R2, R3 and R4 represent hydrogen or lower alkyl, or R1 and R3 taken together form a methylene or dimethylene bridge when A represents dimethylene, R' represents hydrogen, OH, alkoxy having 1-4 carbon atoms, acyloxy having 1-4 carbon atoms or amino, R'' represents hydrogen or alkoxy having 1-4 carbon atoms, or r' and R'' taken together form an oxo, methano or hydroxyimino group, R represents -CH2OH or -COR5, R5 represents hydrogen, -OR6 or R6 represents hydrogen, alkyl having 1-20 carbon atoms, monohydroxyalkyl, polyhydroxyalkyl, aryl or aralkyl optionally substituted, the residue of a sugar or p is 1, 2 or 3, and r' and r'', each independently, represent hydrogen, lower alkyl, monohydroxyalkyl optionally interrupted by a heteroatom, polyhydroxyalkyl, aryl or benzyl optionally substituted, the residue of an amino acid, an aminoester ...

POLYAMINE ANALOGUES AS CYTOTOXIC AGENTS

Calcium independent camp phosphodiestrerase inhibitor antidepressant

Способ получения бета-аминоакролеинов

Способ получения b-аминоакролеина

VERFAHREN ZUR HERSTELLUNG VON ZWISCHENPRODUKTEN, DIE FÜR DIE HERSTELLUNG VON RETROVIRAL-PROTEASE HEMMENDEN VERBINDUNGEN VERWENDBAR SIND

VERFAHREN ZUR HERSTELLUNG VON INTERMEDIATEN IN DER SYNTHESE VON RETROVIRALEN PROTEASE INHIBITOREN

2-Aminopropan-1,3-diol-Verbindungen, ihre medizinische Anwendung und Zwischenprodukte zu ihrer Synthese

OPTISCH AKTIVE (ALPHA)-AMINOALDEHYDE, VERFAHREN ZU IHRER HERSTELLUNG UND IHRE VERWENDUNG ZUR STEREOSELEKTIVEN HERSTELLUNG OPTISCH AKTIVER SS-AMINOALKOHOLE

ANTITUMORALE CONNECTIONS

BICYCLI NAPHTHALINDERIVATE, PROCEDURES FOR THEIR PRODUCTION AND YOUR USE IN HUMAN AND VETERINAERER MEDICINE AND COSMETICS.

PROCEDURE FOR THE PRODUCTION OF INTERMEDIATEN INHIBITORS PROTEASE IN THE SYNTHESIS OF RETROVIRALEN

PEPTIDASE HEMMER

3,3-DIARYLPROPYLAMINE, YOUR USE AND PRODUCTION

DIPHENYLHETEROALKYLDERIVATE, YOUR PRODUCTION AND FROM IT MANUFACTURED DRUGS AND KOSMETIKA.

USE OF AMINES IN OIL COMPOSITIONS

PROCEDURE FOR the PRODUCTION OF 7-SUBSTITUIERTEN HEPT-6-EN AND HEPTANSAEUREN AND DERIVATIVES OF it.

Antitumoral compounds

METHODS AND INTERMEDIATES FOR THE SYNTHESIS OF AZEPINES

IMPROVEMENTS IN OR RELATING TO LEUKOTRIENE ANTAGONISTS

PHENYLACETALDEHYDES SUBSTITUTED BY BASIC GROUPS, THEIR PREPARATION AND DRUGS CONTAINING THESE COMPOUNDS

.alpha.-VINYL-.beta.-AMINO ACROLEIN COMPOUNDS

COSMETIC COMPOSITIONS CONTAINING AS ACTIVE INGREDIENT AT LEAST ONE BICYCLIC NAPHTOIC COMPOUND

L'invention concerne des compositions cosmétiques contenant dans un excipient cosmétiquement acceptable, au moins un composé bicyclique naphtalénique répondant à la formule générale (I): (I) dans laquelle: - A représente un radical méthylène ou diméthylène, substitues ou non par un radical alkyle inférieur, - R1, R2, R3 et R4, identiques ou différents, représentent un atome d'hydrogène ou un radical alkyle inferieur ayant de 1 à 6 atomes de carbone, ou R1 et R3, pris ensemble, forment un pont méthylène ou diméthylène, quand A represente un radical diméthylène, - R' représente un atome d'hydrogène, un radical OH, un radical alkoxy ayant de 1 à 4 atomes de carbone, un radical acyloxy ayant de 1 à 4 atomes de carbone ou un radical amino, - R" représente un atome d'hydrogène ou un radical alkoxy ayant de 1 à 4 atomes de carbone, ou - R' et R", pris ensemble, forment un radical oxo (=O), méthano (=CH2) ou hydroxyimino (=N-OH), et - R représente le radical -CH2OH ou le radical -COR5, R5 ...

PEPTIDASE INHIBITORS

This invention relates to analogs of peptidase substrates in which the nitrogen atom of the scissile amide group of the substrate peptide has been replaced by H, or a substituted malonyl moiety. These analogs of the peptidase substrates provide specific enzyme inhibitors for a variety of proteases, the inhibition of which will have useful physiological consequences in a variety of disease states. M01368B ...

PROCESS FOR SYNTHESIS OF ALPHA ALKYL AMINO ALDEHYDES

PROCESS AND INTERMEDIATES FOR THE PREPARATION OF (1R,2S,5S)-6,6-DIMETHYL-3-AZABICYCLO[3,1,0]HEXANE-2-CARBOXYLATES OR SALTS THEREOF

In one embodiment, the present application relates to a process of making a compound of Formula (I); and to certain intermediate compounds that are made within the process of making the compound Formula (I).

HALOGENOALKYLPHENYL-ALCOHOLS, KETONES AND HYDRATES THEREOF

... - 20 - 100-7540 HALOGONOALKYLPHENYL-ALCOHOLS, KETONES AND HYDRATES THEREOF of the disclosure Halogenoalkylphenyl-alcohols, ketones and their hydrates of formula I, (I) wherein R1 to R8 are as defined in the description, are useful as acetylcholinesterase inhibitors. 6300/WY/ER ...

DIPHENYLHETEROALKYL DERIVATIVES, THE PREPARATION THEREOF AND DRUGS AND COSMETICS PREPARED THEREFROM

O.Z. 0050/40549 Diphenylheteroalkyl derivatives of the formula I (I) where A and R1-R6 have the meanings specified in the description, and the preparation thereof are described. The substances are suitable for controlling diseases and as cosmetic agents.

METHOD FOR THE SYNTHESIS OF ALPHA ALKYLAMINO ALDEHYDES

CALCIUM INDEPENDENT cAMP PHOSPHODIESTERASE INHIBITOR ANTIDEPRESSANT

The method for preparing bicyclic heterocyclic ring compds. for calcium independent cAMP phosphodiesterase inhibitor antidepressant is presented. In the process, bicyclic[2.2.1 hept-2-yl ether 0.014 mole was dissolved in 50ml of ethanol, and then added with 0.736g of sodium cyanatc and 1.0g of methyl amine HCl. The above mixture soln. is stirred for 18hrs at room temp. and reacting soln. is diluted with saturated sodium bicarbonate soln. and extracted with 30ml of ethylether three times. The obtained organic layer is washed with 30ml of saturated sodium chloride solution and dried with anhydrous sodium sulphate. Copyright 1997 KIPO ...

DEUTERIUM-ENRICHED BUPROPION

The present application describes deuterium-enriched bupropion, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. 2. The compound of claim 1 , wherein the compound is a compound of Formula I.5. The compound of claim 1 , wherein the compound is a compound of Formula II.8. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.9. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.10. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.11. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.12. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.13. A method of treating depression claim 1 , comprising administering a therapeutically effective amount of a compound of to a patient in need thereof to treat the depression.14. A method of treating depression claim 2 , comprising administering a therapeutically effective amount of a compound of to a patient in need thereof to treat the depression.15. A method of treating depression claim 3 , comprising administering a therapeutically effective amount of a compound of to a patient in need thereof to treat the depression.16. A method of treating depression claim 5 , comprising administering a therapeutically effective amount of a compound of to a patient in need thereof to treat the depression.17. A method of treating depression claim 6 , comprising administering a therapeutically effective amount of a compound of to a patient in need thereof to treat the depression.18. A method of treating a patient in need of smoking cessation claim 1 , comprising administering a therapeutically effective amount of a compound of to a patient in need thereof to ameliorate smoking by the patient.19. A method of treating a patient in need of smoking cessation claim 2 , comprising administering ...

Aldehydes containing hydroxyl groups

Process for the preparation of N-formylamine derivatives

본 발명은 의약, 농약등의 생리활성물질의 중간체 또는 기능성 고분자 물질을 합성할 수 있는 중간체로 유용한 질소에 포밀(formyl)기를 갖는 아민유도체의 새로운 제조방법으로 1차아민 또는 2차아민기를 갖는 화합물을 포름산(formic acid)과 bis(trichloromethyl)carbonate 존재 하에서 상압, 실온 부근의 온화한 조건에서 반응시킴으로써 질소(N)를 포밀(formyl)기로 보호 한 아민 유도체를 얻는 새로운 방법이다. The present invention is a novel method for preparing an amine derivative having a formyl group in nitrogen, which is useful as an intermediate for synthesizing intermediates or functional polymers of physiologically active substances such as medicines and pesticides, and compounds having primary or secondary amine groups. It is a new method to obtain an amine derivative which protects nitrogen (N) with formyl group by reacting with formic acid in the presence of bis (trichloromethyl) carbonate under normal pressure and room temperature.

Alpha- (dialkoylamino) trifluoromethylpropiophenones.

Compounds for treating nervous system diseases

本发明属于医药技术领域，具有式I结构的化合物及其药学上可接受的盐，

Method for producing substituted phenylethanolamines

Aldehydes containing hydroxl groups

The present invention relates to aldehydes of the formula (I) which contain tertiary amino groups and at least one hydroxyl group. Aldehydes of this kind can be utilized broadly. Aldehydes of particular advantage can be incorporated into a polymer, and find use as curing agents and/or catalysts. Preferably they find use in adhesives and sealants

Therapeutic compounds and preparation thereof

The invention relates to compounds of the formula <FORM:1019128/C2/1> in which R and R1 are alkyl groups of 1-5 carbon atoms. The compounds may be prepared by (1) forming a trifluoromethylpropiophenone, (2) halogenating this to form an a -halotrifluoromethylpropiophenone and (3) aminating the latter with an appropriate dialkylamine. Reaction (1) may be effected by treating a trifluoromethylphenyl magnesium halide with propionic anhydride at below 0 DEG C. in an anhydrous solvent, or alternatively by treating a trifluoromethylbenzonitrile with ethyl magnesium halide to form an intermediate ketimine, which is then hydrolysed with aqueous mineral acid. Reaction (2) is preferably affected at a temperature up to 100 DEG C. with elemental bromine or chlorine, but other halogenating agents may also be used, e.g. N-bromosuccinimide, N - bromacetamide, sulphuryl chloride or N-chlorosuccinimide. Reaction (3) may be effected at 50-125 DEG C. in the presence of a solvent, which may be an excess of the dialkylamine. The products may be converted into salts, e.g. with hydrochloric, sulphuric, phosphoric, acetic, citric or benzoic acid. Examples are given of the manufacture of the hydrochlorides of a -diethylamino-o-, -m-, and -p-trifluoromethyl - propiophenones. The products are of therapeutic value (see Division A5).ALSO:As anorexigenic agents in pharmaceutical compositions, use is made of compounds of the formula <FORM:1019128/A5-A6/1> in which R and R1 are alkyl groups of 1-5 carbon atoms (see Division C2). The compounds may be used in the form of their salts. They may be mixed with solid or liquid pharmaceutical carriers suitable for oral or suppository administration, and examples are given of the preparation of tablets containing a -diethylamino-m-(or p-)-trifluoron methylpropiophenone hydrochloride. The compounds may also be included in food supplement compositions, e.g. in vitamin compositions, or used with other therapeutically active compounds, such as ...

aldehydes containing hydroxyl groups

本发明涉及式(I)的醛，其具有叔氨基和至少一个羟基。这种醛能广泛使用。特别令人感兴趣的醛能插入到聚合物中并用作固化剂和/或催化剂。优选将其用于粘合剂和密封剂中。

Process for synthesis of alpha alkyl amino aldehydes

IN THE CANADIAN PATENT & TRADEMARK OFFICE PATENT APPLICATION entitled: Process for synthesis of alpha alkyl amino aldehydes in the names of: Bertrand CASTRO Jean FEHRENTZ ABSTRACT OF THE DISCLOSURE The present invention relates to a process for the preparation of alpha alkyl amino aldehydes of formula in which R is alkyl or aralkyl possibly substituted, characterized in that N,O-dimethylhydroxylamine is reacted, in a basic medium, on a blocked amine ester of an aminoacid of formula

一种基于高度共轭COFs的光响应模拟氧化酶及其制备方法与应用

本发明公开了一种基于高度共轭COFs的光响应模拟氧化酶及其制备方法及应用。本发明利用1,3,5‑三[4‑氨基(1,1‑联苯‑4‑基)]苯和2,5‑二乙烯基‑1,4‑苯二甲醛合成了具优异光响应模拟氧化酶性质的TABB‑BDB COF材料，可以用于5‑160mg/L范围内的尿酸检测，满足一般情况下人血清中尿酸检测需求。本发明通过设计高度共轭的共价有机框架可以实现光的有效收集和利用，并催化有色底物2,2‑联氮‑二(3‑乙基‑苯并噻唑‑6‑磺酸)二铵盐生成具氧化性的自由基(oxABTS)与具抗氧化活性的尿酸反应，通过监测体系的颜色变化实现尿酸的高效检测。

一种基于高度共轭COFs的光响应模拟氧化酶及其制备方法与应用

本发明公开了一种基于高度共轭COFs的光响应模拟氧化酶及其制备方法及应用。本发明利用1,3,5‑三[4‑氨基(1,1‑联苯‑4‑基)]苯和2,5‑二乙烯基‑1,4‑苯二甲醛合成了具优异光响应模拟氧化酶性质的TABB‑BDB COF材料，可以用于5‑160mg/L范围内的尿酸检测，满足一般情况下人血清中尿酸检测需求。本发明通过设计高度共轭的共价有机框架可以实现光的有效收集和利用，并催化有色底物2,2‑联氮‑二(3‑乙基‑苯并噻唑‑6‑磺酸)二铵盐生成具氧化性的自由基(oxABTS)与具抗氧化活性的尿酸反应，通过监测体系的颜色变化实现尿酸的高效检测。

Verfahren zur bestimmung eines analyts mit einer primären aminogruppe und kit zur etikettierung dieses analyts

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A process for the production of 1(p-hydroxyphenyl)-1-hydroxy-2-(aralkyl-amino)-propanes

Aminopropanols of the formula <FORM:0669574/IV (b)/1> (where R is an aliphatic hydrocarbon residue of 2-5 carbon atoms) are prepared by the following methods: (1) hydrogenating the ketone <FORM:0669574/IV (b)/2> or a salt thereof (R1=H or group split off during hydrogenation, e.g. benzyl) with a noble metal or nickel catalyst; in the latter case, when using a salt, 1 mol. of alkali is added either initially or after 1 mol. of hydrogen has been taken up (by elimination of R1); (2) decomposing the derivative <FORM:0669574/IV (b)/3> by hydrogenation with palladium or heating with mineral acid (when R2=benzyl) or saponification (when R2=residue of a carboxylic or sulphonic acid); (3) reacting an aralkylamine with HO-C6H4-CO.CO.CH3 (or a benzyl ether or carboxylic or sulphonic ester thereof) to give a Schiff's base or aldehyde ammonia; the product is then hydrogenated with a noble metal or nickel catalyst whereby C=N and C=O bonds are reduced and the benzyloxy group if present is converted to a hydroxy group; where an ester was used as starting material, final hydrolysis gives the free p-hydroxy group; (4) an aralkyl or aralkenyl aldehyde or ketone is condensed with <FORM:0669574/IV (b)/4> (or the corresponding R2O- compound) with simultaneous or subsequent reduction; the residue R2 if present is then eliminated as in (2); (5) suspending <FORM:0669574/IV (b)/5> in an organic solvent in which it is sparingly soluble and hydrogenating it together with an aldehyde or ketone R5-CO-R4-C6H5, where R4 and R5 are aliphatic hydrocarbon residues or R5 may be hydrogen, and the sum of the carbon atoms in R4 and R5 is 1-4. In method (1) the reduction and splitting off of R1 may occur simultaneously or successively in either order, depending on the reaction conditions. Suitable solvents for method (5) are methanol, ethanol and isopropanol, with or without water. The products may be obtained as mixtures of stereoisomers which may be separated; ...

Method for the determination of an analyte comprising a primary amino group, and kit for labeling said analyte

The invention provides a method for labeling an analyte comprising a primary amino group, the method comprising: a. a labeling process comprising reacting the analyte with a dialdehyde in the presence of a label, wherein the label bears a charge, and b. an analysis process comprising subjecting the labeled analyte to MS, preferably LC-MS-MS. Herein, preferably, the labeling process comprises reacting an analyte with a dialdehyde, wherein the dialdehyde carries a label bearing a charge, to provide a labeled analyte carrying the charge. The present invention also provides a labeling method to provide a labeled analyte carrying a charge, wherein the labeling method comprises a labeling process comprising reacting an analyte with a dialdehyde, wherein the analyte comprises a primary amino group and wherein the dialdehyde carries a label bearing the charge. The dialdehyde is preferably an aromatic dialdehyde, most preferably an aromatic 1,2- or 1,3-dicarboxaldehyde. The label preferably comprises a quaternary ammonium group and/or a quaternary phosphonium group. The present invention also provides for a kit for labeling the analyte.

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Method for the determination of an analyte comprising a primary amino group, and kit for labeling said analyte

The invention provides a method for labeling an analyte comprising a primary amino group, the method comprising: a. a labeling process comprising reacting the analyte with a dialdehyde in the presence of a label, wherein the label bears a charge, and b. an analysis process comprising subjecting the labeled analyte to MS, preferably LC-MS-MS. Herein, preferably, the labeling process comprises reacting an analyte with a dialdehyde, wherein the dialdehyde carries a label bearing a charge, to provide a labeled analyte carrying the charge. The present invention also provides a labeling method to provide a labeled analyte carrying a charge, wherein the labeling method comprises a labeling process comprising reacting an analyte with a dialdehyde, wherein the analyte comprises a primary amino group and wherein the dialdehyde carries a label bearing the charge. The dialdehyde is preferably an aromatic dialdehyde, most preferably an aromatic 1,2- or 1,3-dicarboxaldehyde. The label preferably comprises a quaternary ammonium group and/or a quaternary phosphonium group. The present invention also provides for a kit for labeling the analyte.

Method for the determination of an analyte comprising a primary amino group, and kit for labeling said analyte

The invention provides a method for labeling an analyte comprising a primary amino group, the method comprising: (a.) a labeling process comprising reacting the analyte with a dialdehyde in the presence of a label, wherein the label bears a charge, and (b.) an analysis process comprising subjecting the labeled analyte to MS, preferably LC-MS-MS. Herein, preferably, the labeling process comprises reacting an analyte with a dialdehyde, wherein the dialdehyde carries a label bearing a charge, to provide a labeled analyte carrying the charge. The present invention also pro vides a labeling method to provide a labeled analyte carrying a charge, wherein the labeling method comprises a labeling process comprising reacting an analyte with a dialdehyde, wherein the analyte comprises a primary amino group and wherein the dialdeh yde carries a label bearing the charge. The dialdehyde is preferably an aromatic dialdehyde, most preferably an aromatic 1,2- or 1,3-dicarboxaldehyde. The label preferably comprises a quaternary ammonium group and/or a quaternary phosponium group. The present invention also provides for a kit for labeling the analyte.

Method for the determination of an analyte comprising a primary amino group, and kit for labeling said analyte

The invention provides a method for labeling an analyte comprising a primary amino group, the method comprising: a. a labeling process comprising reacting the analyte with a dialdehyde in the presence of a label, wherein the label bears a charge, and b. an analysis process comprising subjecting the labeled analyte to MS, preferably LC-MS-MS. Herein, preferably, the labeling process comprises reacting an analyte with a dialdehyde, wherein the dialdehyde carries a label bearing a charge, to provide a labeled analyte carrying the charge. The present invention also provides a labeling method to provide a labeled analyte carrying a charge, wherein the labeling method comprises a labeling process comprising reacting an analyte with a dialdehyde, wherein the analyte comprises a primary amino group and wherein the dialdehyde carries a label bearing the charge. The dialdehyde is preferably an aromatic dialdehyde, most preferably an aromatic 1,2- or 1,3-dicarboxaldehyde. The label preferably comprises a quaternary ammonium group and/or a quaternary phosphonium group. The present invention also provides for a kit for labeling the analyte.

1-(4-hydroxy-3-alkoxyphenyl)-2-(1-methyl-2-phenoxyethylamino)-alkanols and derivatives and process for preparing the same

The invention comprises compounds (including the stereoisomeric forms thereof) of the general formula <FORM:0995356/C2/1> (wherein R1 is a C1-5 alkyl group and R2 is a hydrogen atom or a methyl group) and the pharmaceutically acceptable, non-toxic acid addition salts thereof, pharmaceutical preparations containing them, and their preparation by (a) reacting a compound (I) of the formula <FORM:0995356/C2/2> (wherein R3 is a hydrogen atom or a group which is replaceable by a hydrogen atom, Z is a CO or CHOH group and Y1 is an amino group or a halogen atom) with a compound of the formula <FORM:0995356/C2/3> (wherein Y2 is a Hal-CH(CH3)- group when Y1 is an amino group and a H2N-CH)CH3)-group when Y1 is a halogen atom) and, when R3 is not a hydrogen atom or Z is a CO group catalytically hydrogenating the product of the formula <FORM:0995356/C2/4> or an acid addition salt thereof, or (b) catalytically hydrogenating a mixture of phenoxyacetone and a compound (I) in which Y1 is an amino group, optionally followed in either case by acid addition salt formation. The product may be separated into individual racemates, or this separation may be effected before the catalytic hydrogenation in process (a). a - Bromo - 4 - benzyloxy - 3 - methoxypropiophenone is prepared from 4-hydroxy-3-methoxypropiophenone, via 4-benzyloxy-3-methoxypropiophenone. 4-Hydroxy-3-ethoxyacetophenone is prepared from 2-ethoxyphenol. The compounds of the invention are uterine muscle relaxants, anti-hypertensive agents and vasodilators, and may be administered orally or parenterally in the form of pharmaceutical preparations (e.g. elixirs, solutions, suspensions, tablets and capsules) containing them together with a carrier.

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Composés cétoniques de la série du diphényl méthane et leur préparation

Verfahren zur Herstellung von 1-(3',4'-Dioxy-phenyl)-2-(a-methyl-y-phenyl-propylamino)-1-oxo-propan

1-(4-hydroxy-3-alcoxyphényl)-2-(1-méthyl-2-phénoxyéthylamino)alcanols et dérivés de ces composés.

Procédé de préparation de 1-(4-hydroxy-3-alcoxyphényl)-2-(1-méthyl-2-phénoxyéthylamino) alcanols et des dérivés de ces composés, et produits obtenus

Verfahren zur Herstellung von 1-(3',4'-Dioxy-phenyl)-2-(a-methyl-y-phenyl-propylamino)-1-oxo-propan

Werkwijze voor het vervaardigen van gelaagd vloerbedekkingsmateriaal.

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Diphenyl ketones of pharmaceutical value and the preparation thereof

The invention comprises the compounds 6-ethylmethylamino-5-methyl-4, 4-diphenylhexan-3-one and 6-ethylmethylamino-4, 4-diphenylheptan-3-one, and their salts. The compounds are analgesics and may be prepared by treating 3-ethylmethylamino-2-methyl-1, 1-diphenyl-propyl cyanide or 3-ethylmethylamino-1, 1-diphenylbutyl cyanide, respectively, with ethyl magnesium bromide. In examples, ethylmethylamine is heated with propylene oxide to give 1-ethylmethylamino-2-propanol which is reacted with thionyl chloride in chloroform to yield 1-ethylmethylamino-2-chloropropane; this is then refluxed with diphenylmethyl cyanide and sodamide in benzene to produce a mixture of the isomers 3-ethylmethylamino-1, 1-diphenylbutyl cyanide and 3-ethylmethylamino-2-methyl-1, 1-diphenylpropyl cyanide. After separation, these compounds are reacted with ethyl magnesium bromide according to the Grignard process. The oxalate and the hydroiodide of 6-ethylmethylamino-5-methyl-4, 4-diphenylhexan-3-one, and the hydrobromide of 6-ethylmethylamino-4, 4-diphenylheptan-3-one are described. The Provisional Specification refers to Specifications 654,975, 677,522 and 688,481.

一种基于高度共轭COFs的光响应模拟氧化酶及其制备方法与应用

本发明公开了一种基于高度共轭COFs的光响应模拟氧化酶及其制备方法及应用。本发明利用1,3,5‑三[4‑氨基(1,1‑联苯‑4‑基)]苯和2,5‑二乙烯基‑1,4‑苯二甲醛合成了具优异光响应模拟氧化酶性质的TABB‑BDB COF材料，可以用于5‑160mg/L范围内的尿酸检测，满足一般情况下人血清中尿酸检测需求。本发明通过设计高度共轭的共价有机框架可以实现光的有效收集和利用，并催化有色底物2,2‑联氮‑二(3‑乙基‑苯并噻唑‑6‑磺酸)二铵盐生成具氧化性的自由基(oxABTS)与具抗氧化活性的尿酸反应，通过监测体系的颜色变化实现尿酸的高效检测。

多取代烯胺醛衍生物及其制备方法

本发明提供了一种多取代烯胺醛衍生物及其制备方法，包括：将丙烯醛或丙烯醛衍生物、叠氮化合物或叠氮衍生物、强酸和溶剂置于反应容器中，在0℃以下反应10～60min，再加入甲醇，继续反应10～120min，反应完成后加入三乙胺终止反应；将反应液用二氯甲烷稀释，再经水洗，得有机相；其中，二氯甲烷的用量是所述溶剂体积的5～10倍；将得到的有机相经干燥、浓缩和柱层析纯化，得到多取代烯胺醛衍生物；所述多取代烯胺醛衍生物的结构式如下：