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Небесная энциклопедия

Космические корабли и станции, автоматические КА и методы их проектирования, бортовые комплексы управления, системы и средства жизнеобеспечения, особенности технологии производства ракетно-космических систем

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Мониторинг СМИ

Мониторинг СМИ и социальных сетей. Сканирование интернета, новостных сайтов, специализированных контентных площадок на базе мессенджеров. Гибкие настройки фильтров и первоначальных источников.

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Форма поиска

Поддерживает ввод нескольких поисковых фраз (по одной на строку). При поиске обеспечивает поддержку морфологии русского и английского языка
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Применить Всего найдено 1019. Отображено 189.
04-12-2017 дата публикации

СПОСОБ ПОЛУЧЕНИЯ N-АЛКИЛ-О-АРИЛКАРБАМАТОВ

Номер: RU2637317C1

Изобретение относится к способу получения N-алкил-О-арилкарбаматов общей формулы I, где R означает арильные группы, a R- алкильные группы нормального или разветвленного строения с числом атомов углерода от 1 до 4. Способ заключается в том, что осуществляют взаимодействие фенолов с диалкилмочевиной общей формулы II при температуре 130-180°C при барботировании через реакционную массу хлористого водорода, являющегося одновременно катализатором процесса и акцептором выделяющегося алкиламина. Предлагаемый способ является экологически безопасным и при этом позволяет сохранить удовлетворительный выход и чистоту получаемого продукта. 3 пр.

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19-09-2018 дата публикации

Patent RU2016147986A3

Номер: RU2016147986A3
Автор: [UNK]
Принадлежит: [UNK]

ВИ“? 2016147986” АЗ Дата публикации: 19.09.2018 Форма № 18 ИЗ,ПМ-2011 Федеральная служба по интеллектуальной собственности Федеральное государственное бюджетное учреждение ж 5 «Федеральный институт промышленной собственности» (ФИПС) ОТЧЕТ О ПОИСКЕ 1. . ИДЕНТИФИКАЦИЯ ЗАЯВКИ Регистрационный номер Дата подачи 2016147986/04(077105) 13.04.2015 РСТ/ЕР2015/057966 13.04.2015 Приоритет установлен по дате: [ ] подачи заявки [ ] поступления дополнительных материалов от к ранее поданной заявке № [ ] приоритета по первоначальной заявке № из которой данная заявка выделена [ ] подачи первоначальной заявки № из которой данная заявка выделена [ ] подачи ранее поданной заявки № [Х] подачи первой(ых) заявки(ок) в государстве-участнике Парижской конвенции (31) Номер первой(ых) заявки(ок) (32) Дата подачи первой(ых) заявки(ок) (33) Код страны 1. 14/272,597 08.05.2014 05 Название изобретения (полезной модели): [Х] - как заявлено; [ ] - уточненное (см. Примечания) СПОСОБ ПРИМЕНЕНИЯ ТИТАНОВОГО КАТАЛИЗАТОРА ДЛЯ ПОЛУЧЕНИЯ МАТЕРИАЛОВ, СОДЕРЖАЩИХ КАРБАМАТНЫЕ ФУНКЦИОНАЛЬНЫЕ ГРУППЫ Заявитель: БАСФ КОАТИНГС ГМБХ, РЕ 2. ЕДИНСТВО ИЗОБРЕТЕНИЯ [Х] соблюдено [ ] не соблюдено. Пояснения: см. Примечания 3. ФОРМУЛА ИЗОБРЕТЕНИЯ: [Х] приняты во внимание все пункты (см. Примечания) [ ] приняты во внимание следующие пункты: [ ] принята во внимание измененная формула изобретения (см. Примечания) 4. КЛАССИФИКАЦИЯ ОБЪЕКТА ИЗОБРЕТЕНИЯ (ПОЛЕЗНОЙ МОДЕЛИ) (Указываются индексы МПК и индикатор текущей версии) С07С 269/06 (2006.01) С08С 71/04 (2006.01) СОЗЕ 8/30 (2006.01) С09О 175/04 (2006.01) 5. ОБЛАСТЬ ПОИСКА 5.1 Проверенный минимум документации РСТ (указывается индексами МПК) С07С 269/06 С08С 71/04 СО8Е 8/30 С09р 175/04 С09р 133/14 5.2 Другая проверенная документация в той мере, в какой она включена в поисковые подборки: 5.3 Электронные базы данных, использованные при поиске (название базы, и если, возможно, поисковые термины): Езрасепеё, боозе, РабЗеагсв 6. _ ДОКУМЕНТЫ, ОТНОСЯЩИЕСЯ К ПРЕДМЕТУ ПОИСКА (см. на ...

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09-12-2019 дата публикации

Соединение с органической аминовой солью, имеющее анион в качестве донора CO, и его использование в качестве вспенивающего агента

Номер: RU2708457C1

Изобретение относится к вспенивающему агенту, содержащему соединение соли органического амина формулы (I) или смесь соединений солей органического амина формулы (I). Формула (I): A[B](I), где A- анион - источник CO, имеющий -n валентность, где n=1, 2 или 3, Bпредставляет собой или содержит ион аммония с валентностью +1 и/или один или более катионов органического амина (B), в котором каждый катион (B) имеет группу -NRRH и/или группу -NRH- в количестве m, где m=1-5, 00 мас.% до 40 мас.%. Также предложены способы ...

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08-07-2020 дата публикации

Self-immolative systems

Номер: GB0002579899A
Принадлежит:

A self-immolative molecule suitable to be triggered by non-protic electrophilic agents, comprising a trigger portion linked to at least one releasable portion via a self-immolative portion, wherein the trigger portion comprises a neutral nucleophile selected from -R3­SR1, -R3NR1R2, -R3PR1R2, -R3AsR1R2 wherein R1 and R2 are hydrogen, alkyl, aryl or heteroaryl, wherein R3 is a chemical moiety capable of undergoing β-elimination and is at least a part of the self-immolative portion. The molecule provides a recognition/responsive system for electrophilic compounds, especially alkylating agents and chemical warfare agents. The releasable portion may be capable of generating a detection/measurable response upon release, e.g. colour or fluorescence. Preferably the self-immolative molecule has the formula: wherein Nu is S, P, As or N, R1 and R2 are hydrogen, alkyl, aryl or heteroaryl and R4-R8 comprise 0-3 methyl groups and at least one nitro group, the remainder being hydrogen atoms. Also claimed ...

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31-08-1978 дата публикации

MANUFACTURE OF CARBAMATES

Номер: GB0001523308A
Автор:
Принадлежит:

... 1523308 Polyether carbamates; methylolated carbamates; textile treating solutions BASF AG 17 Dec 1975 [18 Dec 1974] 51567/75 Heading C3R [Also in Division C2] Carbamates of the formula wherein R<1> is an aliphatic, cycloaliphatic or araliphatic radical which may be interrupted by one or more -CO-O-, -CO-NH- and/or -O- radicals, or R<1> is a NH2CO- or phenyl group or when (m is an integer) a hydrogen atom, R<2> is an aliphatic radical of at least 2 carbon atoms which is optionally interrupted by one or more -CO-O-, -CO-NH and/or -O- radicals, or it is an (-CHR<3>-)n radical, R<3> being a cycloaliphatic, araliphatic or aromatic radical and n being from 2 to 6, and m is 0 or an integer, are obtained by reacting the correspond. ing hydroxy compounds of the formula with urea in the presence of ion-exchangers containing nickel. An example illustrates the preparation of the carbamate The nickel-containing ion-exchanger may be obtained by treating a cation exchanger, after it had been standing ...

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10-06-1993 дата публикации

PROCESS FOR PRODUCING UNSATURATED CARBAMIC ACID ESTERS

Номер: AU0000637917B2
Принадлежит:

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27-08-1985 дата публикации

PROCESS FOR THE PREPARATION OF URETHANES

Номер: CA0001192570A1
Принадлежит:

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10-05-1988 дата публикации

PROCESS FOR THE PRODUCTION OF URETHANES

Номер: CA0001236479A1
Принадлежит:

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20-03-1979 дата публикации

MANUFACTURE OF CARBAMATES

Номер: CA0001051017A1
Принадлежит:

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04-05-2021 дата публикации

ORGANIC AMINE SALT COMPOUNDS HAVING CO2-DONATING ANIONS AND THEIR USE AS FOAMING AGENT

Номер: CA3025030C

An organic amine salt compound having the general formula (I): An-[Bm+]p. In the formula, An- is anions having -n valence serving as CO2 donors, wherein n = 1, 2, or 3; Bm+ is or contains: ammonium ions and/or organic amine B cations; m = 1-10; formula (AA); An- is selected from one or more of the following anions: (a) carbamate; (b) carbonate; (c) formate; (d) bicarbonate; (e) organic monocarbonate; (f) organic polycarbamate; formula (g) or formula (J); or (h) organic polycarbonate; the compound of general formula (I) has at least one hydroxyalkyl linked to N atoms, i.e. has alcohol amine residue. Same can serve as a polyurethane foaming agent, a polystyrene foaming agent, or a polyvinyl chloride foaming agent.

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13-11-2014 дата публикации

PHENOL DERIVATIVE AND PREPARATION METHOD AND USE IN MEDICINE THEREOF

Номер: CA0002911845A1
Принадлежит:

The invention relates to a phenol derivative and the preparation method and use in medicine thereof, and in particular, relates to a phenol derivative as shown in the general formula (A), or stereoisomers, solvates, metabolites, prodrugs, pharmaceutical acceptable salts or eutectic crystals thereof, and the preparation method thereof, a pharmaceutical composition comprising the same and use of the compounds or composition of the invention in the field of the central nervous system, wherein the definition of each substituent in general formula (A) is the same as the definition in the description.

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30-05-2014 дата публикации

PROCESS FOR THE PREPARATION OF (1S,4S,5S)-4-BROMO-6-OXABICYCLO[3.2.1] OCTAN-7-ONE

Номер: CA0002891932A1
Принадлежит:

The present invention relates to an improved and industrially advantageous process for the preparation of (1S, 4S, 5S) -4-bromo-6-oxabicyclo [3.2.1] octan-7-one represented by the following formula (I) which is a key intermediate in the synthesis of edoxaban, a compound that exhibits an inhibitory effect on activated blood coagulation factor X (also referred to as activated factor X or FXa), and is useful as a preventive and/or therapeutic drug for thrombotic diseases. The process includes reacting (1S) -cyclohex-3-ene-1-carboxylic acid of formula (II) with a brominating agent selected from the group consisting of N-bromosuccinimide or 1, 3-dibromo-5, 5-dimethylhydantoin in the presence of a base selected from calcium oxide or calcium hydroxide in a solvent selected from the group comprising of dichloromethane, toluene, tetrahydrofuran, ethy1 acetate, hexanes, cyclopentyl methyl ether (CPME) or a mixture thereof to get ( 1S, 4S, 5S) -4-bromo-6-oxabicyclo [3.2.1] octan-7-one of formula ( ...

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04-01-1992 дата публикации

PROCESS FOR PRODUCING UNSATURATED CARBAMIC ACID ESTERS

Номер: CA0002046068A1
Принадлежит:

The present invention provides a manufacturing method for unsaturated carbamic acid esters by allowing an unsaturated amide compound to react with a metallic base in an inert solvent, followed by a reaction with a halogenated formic acid ester. The invention also provides a manufacturing method of unsaturated carbamic acid esters by allowing an urethane derivative to react with a metallic base in an inert solvent, followed by a reaction with an unsaturated acid halide.

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10-02-2009 дата публикации

O-CARBAMOYL-PHENYLALANINOL HAVING SUBSTITUENT AT BENZENE RING, ITS PHARMACEUTICALLY USEFUL SALTS AND METHOD FOR PREPARING THE SAME

Номер: CA0002217771C
Принадлежит: SK HOLDINGS CO., LTD., YUKONG LTD, YUKONG LIMITED

O-carbamoyl-phenylalaninol having substituent at benzene ring, represented by general formula (I), and pharmaceutically useful salts thereof, which are useful for the prophylaxis and treatment of CNS disorder including depression and anxiety, are disclosed: wherein R is lower alkyl containing 1 to 8 carbon atoms; halogen such as F, Cl and I; alkoxy containing 1 to 3 carbon atoms; thioalkoxy containing 1 to 3 carbon atoms; nitro, hydroxy, or trifluorocarbon; and x is an integer of 1 to 3, with a proviso that R is the same or different when x is 2 or 3.

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28-02-1978 дата публикации

Номер: CH0000596154A5
Принадлежит: BASF AG

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28-10-2004 дата публикации

СПОСОБ ПОЛУЧЕНИЯ ЭФИРОВ АРИЛИМИНОМЕТИЛКАРБАМИНОВОЙ КИСЛОТЫ

Номер: EA0000005006B1

... 1. Способ получения соединений формулы (I) в которой R1 представляет собой остаток, выбранный из группы, включающей метил, этил, пропил, циклопентил, циклогексил, фенил, бензил и -C(Me2)фенил, каждый из которых может быть одно-, двух- или трехкратно замещен гидроксигруппой, R2представляет собой остаток, выбранный из группы, включающей метил, этил, пропил и бензил, отличающийся тем, что соединение формулы (II) в которой R1' представляет собой остаток, выбранный из группы, включающей метил, этил, пропил, циклопентил, циклогексил, фенил, бензил и -C(Me2 )фенил, каждый из которых может быть одно-, двух- или трехкратно замещен группой -O-PG, при этом такая группа -O-PG представляет собой защищенную гидроксильную функцию, выбранную из группы, включающей метоксиметилокси-, 2-метоксиэтоксиметилокси-, 1-этоксиэтилокси-, 2-тетрагидропиранилокси-, 1-бутоксиэтилокси-, трет-бутилокси-, бензилокси- и 4-метоксибензилоксигруппу, сначала в эфирном или ароматическом растворителе подвергают взаимодействию ...

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30-08-2011 дата публикации

СПОСОБ ПОЛУЧЕНИЯ СЛОЖНОГО ЭФИРА N-ЗАМЕЩЕННОЙ КАРБАМИНОВОЙ КИСЛОТЫ, СПОСОБ ПОЛУЧЕНИЯ ИЗОЦИАНАТА С ПРИМЕНЕНИЕМ ТАКОГО СЛОЖНОГО ЭФИРА N-ЗАМЕЩЕННОЙ КАРБАМИНОВОЙ КИСЛОТЫ И КОМПОЗИЦИЯ ДЛЯ ТРАНСПОРТИРОВКИ И ХРАНЕНИЯ СЛОЖНОГО ЭФИРА N-ЗАМЕЩЕННОЙ КАРБАМИНОВОЙ КИСЛОТЫ, СОДЕРЖАЩАЯ СЛОЖНЫЙ ЭФИР N-ЗАМЕЩЕННОЙ КАРБАМИНОВОЙ КИСЛОТЫ И АРОМАТИЧЕСКОЕ ГИДРОКСИСОЕДИНЕНИЕ

Номер: EA201070852A1
Принадлежит:

Данное изобретение представляет собой способ получения сложного эфира N-замещенной карбаминовой кислоты, получаемого из органического амина, производного угольной кислоты и гидроксикомпозиции, содержащей один или несколько видов гидроксисоединений, в котором органический амин, производное угольной кислоты и гидроксикомпозиция реагируют с применением реакционного резервуара для получения уретана, снабженного конденсатором, газ, содержащий гидроксикомпозицию, соединение, имеющее карбонильную группу, полученное из производного угольной кислоты, и аммиак, образованный в качестве побочного продукта в ходе реакционного взаимодействия, вводится в конденсатор, предусмотренный в реакционном резервуаре для получения уретана, и гидроксикомпозиция и соединение, имеющее карбонильную группу, полученное из производного угольной кислоты, конденсируются, и в котором гидроксисоединение, содержащееся в сконденсированной гидроксикомпозиции, содержится в расчете на стехиометрическое соотношение в количестве ...

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03-08-2018 дата публикации

Method for preparing dialkyl carbonate by alcoholysis of urea

Номер: CN0108358786A
Принадлежит:

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25-08-1989 дата публикации

Procede de preparation de carbamates aromatiques

Номер: FR0002627489A
Принадлежит:

L'invention concerne un perfectionnement a un procede de preparation de carbamates aromatiques par reaction d'au moins un compose nitroaromatique, du monoxyde de carbone et d'au moins un compose organique porteur d'au moins un groupe hydroxyle en presence : a) d'un catalyseur a base de palladium, b) d'au moins un coordinat de formule :dans laquelle G et G', identiques ou differents, representent chacun un groupe pontant qui comporte 3 ou 4 atomes dont au moins 2 sont des atomes de carbone, G et G' pouvant par ailleurs etre relies l'un a l'autre, et, c) d'au moins un acide protonique dont aucun proton n'est relie a un atome d'halogene. Le perfectionnement comprend le fait que la quantite de palladium presente dans le milieu reactionnel est inferieure ou egale a 0,01 mole par litre dudit milieu et qu'on opere en respectant au moins l'une des conditions suivantes : - le rapport molaire (H+/Pd) est superieur a 150, - le rapport molaire (coordinat/Pd) est superieur a 20. Le procede selon l'invention ...

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15-05-2014 дата публикации

SYNTHESIS OF METHYL CARBAMATE AND DIMETHYL CARBONATE (DMC) IN PRESENCE OF STRIPPING WITH INERT GAS OR SUPERHEATED VAPOURS AND A REACTOR FOR THE SAME

Номер: WO2014072803A1
Принадлежит:

The invention relates to synthesis of methyl carbamate (MC) and dimethyl carabonate (DMC) in presence of stripping inert gas or superheated methanol vapors using packed column reactor and bubble column reactor.

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26-05-1992 дата публикации

Preparation of aromatic carbamates

Номер: US0005117036A1
Принадлежит: Rhone-Poulenc Chimie

Aromatic carbamates are selectively and actively prepared by reacting (a) at least one nitroaromatic compound with (b) carbon monoxide and (c) at least one organic compound bearing at least one hydroxyl group, in the presence of: (d) a palladium-based catalyst, (e) at least one coordinate of the formula: см. иллюстрацию в PDF-документе in which each of G and G', which may be identical or different, is a bridging group which contains 3 or 4 atoms, at least 2 of which are carbon atoms, with the proviso that G and G' may be linked to each other, and (f) at least one protonic acid in which no proton is linked to a halogen atom, and wherein the amount of palladium present in the reaction medium is less than or equal to 0.01 mole per liter of such reaction medium and the reaction is carried out such that: (i) either the molar ratio (H+ /Pd) is higher than 150, and/or (ii) the molar ratio (coordinate/Pd) is higher than 20.

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19-05-2020 дата публикации

Propellane derivates and synthesis

Номер: US0010654812B2

Disclosed herein are compounds of the general Formula (I), and methods of synthesizing substituted bicyclo[1.1.1 jpentanes. The synthetic methods described herein use a [1.1.1]propellane, a Group VIII transition metal compound, a hydride source and a reagent that can contribute a substituent to form a substituted bicyclo[1.1.1]pentane, such as a compound of the general Formula (I).

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11-01-2012 дата публикации

METHOD FOR PRODUCING HALOGEN-SUBSTITUTED BENZENE DIMETHANOL

Номер: EP2404897A1
Принадлежит:

A method for producing a halogen-substituted benzene dimethanol, the method including: a first step of reacting a compound represented by formula (1) with a compound represented by formula (2) to obtain a dicarboxamide compound represented by formula (3), and a second step of reducing the dicarboxamide compound using a borohydride compound to obtain a halogen-substituted benzene dimethanol represented by formula (4).

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20-12-2003 дата публикации

СПОСОБ ПОЛУЧЕНИЯ НЕСТЕРОИДНОГО МОДУЛЯТОРА ГЛЮКОКОРТИКОИДНЫХ РЕЦЕПТОРОВ И ПРОМЕЖУТОЧНЫЕ СОЕДИНЕНИЯ

Номер: RU2219170C2

Описывается способ получения соединения формулы (1) из карбоновой кислоты и амина в присутствии 1,1'-карбонилдиимидазола с использованием новых промежуточных соединений, а также новые промежуточные соединения. Технический результат - получение соединения, пригодного в качестве нестероидного модулятора глюкокортикоидных рецепторов. 7 с. и 9 з.п.ф-лы.

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27-06-2010 дата публикации

СПОСОБ ПОЛУЧЕНИЯ (S)-3-[(1-ДИМЕТИЛАМИНО)ЭТИЛ]-ФЕНИЛ-N-ЭТИЛ-N-МЕТИЛ-КАРБАМАТА

Номер: RU2393148C2

FIELD: chemistry. ^ SUBSTANCE: present invention relates to methods for synthesis of rivastigmine having formula (I), involving reacting 3-(1-dimethylaminoethyl)phenol of formula (V) or its S-enantiomer of formula (V-a) with carbonyl diimidazole, subsequent reaction of the reaction product with ethylmethylamine in an organic solvent to obtain a compound (II) or a compound (I) and optional splitting of the formula (II) compound to obtain a formula (I) compound or carry out a reaction of S-3-(1-dimethylaminoethyl) phenol of formula (V-a) with ethylmethyl carbamoylchloride in an inert organic solvent at high temperature and in the presence of a weak inorganic or organic base. ^ EFFECT: methods are cheap on an industrial scale and enable use of readily available industrially safe material. ^ 22 cl, 1 dwg, 8 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2 393 148 (13) C2 (51) МПК C07C C07C C07C C07C 269/04 271/44 269/00 269/08 (2006.01) (2006.01) (2006.01) (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ, ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (21), (22) Заявка: 2007115398/04, 29.10.2005 (24) Дата начала отсчета срока действия патента: 29.10.2005 R U (30) Конвенционный приоритет: 08.11.2004 IN 1207/MUM/2004 (72) Автор(ы): ГХАРПУР Милинд Морешвар (IN), БХАВАЛ Бабурао Маникрао (IN), ШАХ Вирал Бипинбхай (IN), ЗОП Умеш Ревай (IN), МЕХТА Сатиш Раманлал (IN) (45) Опубликовано: 27.06.2010 Бюл. № 18 2 3 9 3 1 4 8 (73) Патентообладатель(и): ЭМКЮР ФАРМАСЬЮТИКАЛЗ ЛИМИТЕД (IN) (43) Дата публикации заявки: 20.12.2008 2 3 9 3 1 4 8 R U (85) Дата перевода заявки PCT на национальную фазу: 08.06.2007 (86) Заявка PCT: IB 2005/003237 (29.10.2005) (87) Публикация PCT: WO 2006/048720 (11.05.2006) Адрес для переписки: 105215, Москва, а/я 26, Н.А.Рыбиной (54) СПОСОБ ПОЛУЧЕНИЯ (S)-3-[(1-ДИМЕТИЛАМИНО)ЭТИЛ]-ФЕНИЛ-N-ЭТИЛ-N-МЕТИЛКАРБАМАТА его S-энантиомера формулы (V-a) карбонилдиимидазолом, последующее взаимодействие продукта реакции этилметиламином в (57) Реферат: ...

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Номер: RU2018147263A

РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2018 147 263 A (51) МПК C07C 271/28 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2018147263, 09.06.2017 (71) Заявитель(и): САЙФЛУОР ЛАЙФ САЙЕНСИЗ, ИНК (US) Приоритет(ы): (30) Конвенционный приоритет: 10.06.2016 US 62/348,481 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 10.01.2019 R U (43) Дата публикации заявки: 10.07.2020 Бюл. № 19 (72) Автор(ы): ЭДВАРДС, Д. Скотт (US), АСКЬЮ, Бен С. (US), ФУРУЯ, Такеру (US) (86) Заявка PCT: (87) Публикация заявки PCT: WO 2017/214539 (14.12.2017) A Адрес для переписки: 129090, Москва, ул. Б. Спасская, 25, стр. 3, ООО "Юридическая фирма Городисский и Партнеры" R U (57) Формула изобретения 1. Соединение формулы А: A 2 0 1 8 1 4 7 2 6 3 (54) ФТОРИРОВАННЫЕ 2-АМИНО-4-(ЗАМЕЩЕННЫЕ АМИНО)ФЕНИЛКАРБАМАТНЫЕ ПРОИЗВОДНЫЕ 2 0 1 8 1 4 7 2 6 3 US 2017/036802 (09.06.2017) (A) или его фармацевтически приемлемая соль или сольват, в которой: X1, X2, X3 и X9 представляют собой каждый независимо H, дейтерий, F, NH2 или C1-C4алкил, необязательно замещенный одним или более F; X10 представляет собой C(O)(C7X7)nX6 или CO2(C7X7)nX6; X4 представляет собой H, C1-C4алкил, C2-C6алкенил или C2-C6алкинил; X5 представляет собой фенил-(CX8X8)m, в которой фенил замещен одним или более заместителями, независимо выбранными из дейтерия, C1-C4алкила, C1-C4алкила, замещенного одним или более F, F и SF5, и в которой, по меньшей мере, один заместитель выбран из C1-C4алкила, замещенного одним или более F, F и SF5, или Стр.: 1 Стр.: 2 A 2 0 1 8 1 4 7 2 6 3 R U A или его фармацевтически приемлемая соль или сольват, в которой X1, X2 и X3 представляют собой каждый независимо H, дейтерий или F, в которой, когда X1, X2, X3 и X6 представляют собой каждый H, n равно 2, каждый X7 представляет собой H и X5 представляет собой 4-фторбензил, тогда X4 не 2 0 1 8 1 4 7 2 6 3 (I) R U X4 и X5 вместе с атомом азота, к которому они присоединены, образуют 5-7-членное ...

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20-11-2005 дата публикации

СПОСОБ ПОЛУЧЕНИЯ ПРОМЕЖУТОЧНЫХ СОЕДИНЕНИЙ, ИСПОЛЬЗУЕМЫХ В СИНТЕЗЕ ИНГИБИТОРОВ ТУБУЛИНА

Номер: RU2005111753A

ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß (19) RU (51) ÌÏÊ 7 (11) 2005 111 753 (13) A C 07 C 269/08 ÔÅÄÅÐÀËÜÍÀß ÑËÓÆÁÀ ÏÎ ÈÍÒÅËËÅÊÒÓÀËÜÍÎÉ ÑÎÁÑÒÂÅÍÍÎÑÒÈ, ÏÀÒÅÍÒÀÌ È ÒÎÂÀÐÍÛÌ ÇÍÀÊÀÌ (12) ÇÀßÂÊÀ ÍÀ ÈÇÎÁÐÅÒÅÍÈÅ (21), (22) Çà âêà: 2005111753/04, 12.09.2003 (71) Çà âèòåëü(è): ÓÀÉÒ ÕÎËÄÈÍÃÇ ÊÎÐÏÎÐÅÉØÍ (US) (30) Ïðèîðèòåò: 20.09.2002 US 60/412,024 (43) Äàòà ïóáëèêàöèè çà âêè: 20.11.2005 Áþë. ¹ 32 (86) Çà âêà PCT: US 03/28661 (12.09.2003) (74) Ïàòåíòíûé ïîâåðåííûé: Åãîðîâà Ãàëèíà Áîðèñîâíà Àäðåñ äë ïåðåïèñêè: 129010, Ìîñêâà, óë. Á.Ñïàññêà , 25, ñòð.3, ÎÎÎ "Þðèäè÷åñêà ôèðìà Ãîðîäèññêèé è Ïàðòíåðû", ïàò.ïîâ. Ã.Á. Åãîðîâîé (54) ÑÏÎÑÎÁ ÏÎËÓ×ÅÍÈß ÏÐÎÌÅÆÓÒÎ×ÍÛÕ ÑÎÅÄÈÍÅÍÈÉ, ÈÑÏÎËÜÇÓÅÌÛÕ Â ÑÈÍÒÅÇÅ R U Ôîðìóëà èçîáðåòåíè 1. Ñïîñîá ïîëó÷åíè ñîåäèíåíè ôîðìóëû I A 2 0 0 5 1 1 1 7 5 3 A ÈÍÃÈÁÈÒÎÐΠÒÓÁÓËÈÍÀ I ãäå R1 è R2 íåçàâèñèìî âûáèðàþò èç Í, ëèíåéíîãî àëêèëà, ñîäåðæàùåãî îò 1 äî 4 àòîìîâ óãëåðîäà, ãàëîãåíà è àëêîêñè, ñîäåðæàùåãî îò 1 äî 4 àòîìîâ óãëåðîäà; R3 ïðåäñòàâë åò ñîáîé ëèíåéíûé àëêèë, ñîäåðæàùèé îò 1 äî 4 àòîìîâ óãëåðîäà; R4 ïðåäñòàâë åò ñîáîé ëèíåéíûé àëêèë, ñîäåðæàùèé îò 1 äî 4 àòîìîâ óãëåðîäà, è ðàçâåòâëåííûé àëêèë, ñîäåðæàùèé îò 3 äî 4 àòîìîâ óãëåðîäà; R5 ïðåäñòàâë åò ñîáîé ëèíåéíûé àëêèë, ñîäåðæàùèé îò 1 äî 4 àòîìîâ óãëåðîäà; âêëþ÷àþùèé à) îáðàáîòêó íèòðèëà ôîðìóëû Ñòðàíèöà: 1 RU 2 0 0 5 1 1 1 7 5 3 (87) Ïóáëèêàöè PCT: WO 2004/026814 (01.04.2004) R U (85) Äàòà ïåðåâîäà çà âêè PCT íà íàöèîíàëüíóþ ôàçó: 20.04.2005 (72) Àâòîð(û): Ó ßíüäæóí (US), ÌÅÃÀÒÈ Ñðèíèâàñóëó (US), ÃËÅÒÑÎÑ Êîíñòàíòèí (US), ÊÅÍÄÀËË Äæîí Òîìàñ (US), ÓÈËÊ Áîãäàí Êàçèìåæ (US), ÏÀÄÌÀÍÀÒÀÍ Òóðåéðàäæàõ (US), ÐÀÂÈÍÄÐÀÍÀÒ Ïàíîëèë (US) âîññòàíàâëèâàþùèì àãåíòîì ñ ïîñëåäóþùèì êèñëîòíûì ãèäðîëèçîì ñ ïîëó÷åíèåì àëüäåãèäà ôîðìóëû b) âçàèìîäåéñòâèå àëüäåãèäà (ñòàäè à) ñ öèàíèäîì ùåëî÷íîãî ìåòàëëà â ïðèñóòñòâèè àëêèëàìèíà ôîðìóëû R5NH2 ñ ïîëó÷åíèåì íèòðèëà ôîðìóëû R U A e) ãèäðîëèç òðèçàùèùåííîãî àìèäà (ñòàäè d) ñ ïîìîùüþ ãèäðîêñèäà ùåëî÷íîãî ìåòàëëà ñ ïîëó÷åíèåì ðàöåìè÷åñêîãî çàùèùåííîãî àìèíà ôîðìóëû A R U 2 0 0 5 1 1 1 7 5 3 d) ...

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20-12-2008 дата публикации

СПОСОБ ПОЛУЧЕНИЯ (S)-3-[1-ДИМЕТИЛАМИНОЭТИЛ]-ФЕНИЛ-N-ЭТИЛ-N-МЕТИЛ-КАРБАМАТА

Номер: RU2007115398A

1. Способ получения ривастигмина по формуле (I)включающий:а) реакцию 3-(1-диметиламиноэтил)фенола по формуле (V) с карбонилдиимидазолом иb) проведение стадии реакции продукта по стадии а) с этилметиламином в органическом растворителе для получения соединения (II);с) произвольное расщепление соединения (II) для получения соединения (I).2. Способ по п.1, в котором 3-(1-диметиламиноэтил)фенол является оптически активным (S)-3-(1-диметиламиноэтил)фенолом3. Способ по пп.1 и 2, в котором ривастигмин по формуле (I) получают путем проведения реакции (S)-3-(1-диметиламиноэтил)фенола по формуле (V-a) с карбонил имидазолом и этилметиламином в органическом растворителе.4. Способ по п.1, в котором количество используемого карбонилдиимидазола составляет от 1,5 до 3,0 молей на моль соединения по формуле (V) или соединения по формуле (V-a).5. Способ по п.4, в котором количество используемого карбонилдиимидазола составляет предпочтительно от 1,75 до 2,25 молей на моль соединения по формуле (V) или соединения по формуле (V-a).6. Способ по п.1, в котором количество используемого этилметиламина составляет от 1,0 до 3,0 молей на моль соединения по формуле (V) или соединения по формуле (V-a).7. Способ по п.6, в котором количество используемого этилметиламина составляет предпочтительно от 1,75 до 2,25 молей на моль соединения по формуле (V) или соединения по формуле (V-a).8. Способ по п.1, в котором используемый растворитель выбирают из группы, включающей алифатические углеводороды, сложные эфиры и хлорированные растворители.9. Способ по п.8, в котором предпочтительным растворителем является хлорированный углеводород.10. Способ по п.9, в котором хлорированный растворитель выбирают из группы, вк ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß RU (19) (11) 2007 115 398 (13) A (51) ÌÏÊ C07C 269/04 (2006.01) ÔÅÄÅÐÀËÜÍÀß ÑËÓÆÁÀ ÏÎ ÈÍÒÅËËÅÊÒÓÀËÜÍÎÉ ÑÎÁÑÒÂÅÍÍÎÑÒÈ, ÏÀÒÅÍÒÀÌ È ÒÎÂÀÐÍÛÌ ÇÍÀÊÀÌ (12) ÇÀßÂÊÀ ÍÀ ÈÇÎÁÐÅÒÅÍÈÅ (21), (22) Çà âêà: 2007115398/04, 29.10.2005 (71) Çà âèòåëü(è): ÝÌÊÞÐ ÔÀÐÌÀÑÜÞÒÈÊÀËÇ ËÈÌÈÒÅÄ (IN) (30) ...

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Verfahren zur Herstellung von Urethanen

Номер: DE102008006881A1
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Die Erfindung betrifft ein Verfahren zur Herstellung von Urethanen durch oxidative Carbonylierung von Aminoverbindungen in Gegenwart von Kohlenmonoxid, Sauerstoff und organischen, Hydroxylgruppen tragenden Verbindungen, dadurch gekennzeichnet, dass die Carbonylierung in Abwesenheit von halogenhaltigen Promotoren und in Anwesenheit von Metallkomplexkatalysatoren durchgeführt wird, die neutrale zweizähnige N-Chelatliganden des Typs (N ~ N), zwei mono-anionische N,O-Chelatliganen des allgemeinen Typs (N ~ O)- oder vierzähnige dianionische Chelatliganden (O ~ N ~ N ~ O)2- enthalten.

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22-03-1973 дата публикации

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Номер: DE0002146069A1
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Products of phosgene with R1R2C=NR3 (I) (where R1-3 are each opt. satd. aliphatic, cycloaliphatic, araliphatic or aromatic gps. opt. substd. by halogen, -CN, -NO2, ether, thioether, ester, acyl and/or sulphonyl gps., or R1 and R2 are H, CN, sulphonyl, NO2, acyl or ester, and/or R1, R2 and R3 together form polycyclic carbo- or heterocyclic rings), opt. as hydrochlorides, or with di-molecular cpds. of formula (I) (where one of R1-3 is a bivalent link) are prepd. by mixing (I), opt. with inert diluents and catalysts, with >= stoichiometric amt. of phosgene at -20 to 200 degrees C; heating to 40-300 (40-200) degrees C with addn. of excess phosgene to 1.5-10 moles/mole (i) total, and opt. heating to separate tert. alkyl chloride and/or HCl. Pref. products are R1R2ClC-NR3COCl and R1R2ClCNCO, useful as raw materials and inters. for lacquers, plastics, coatings, plant protective agents, dyes and pharmaceuticals.

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08-08-1974 дата публикации

Номер: DE0001618401C3
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Stereoselective process for making substituted amino acid derivatives

Номер: GB0002318788A
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The invention encompasses a method for the stereoselective synthesis of alkyl proline and other amino acid derivatives which are intermediates of the farnesyl-protein transferase inhibiting CA 1 A 2 X motif of the protein Ras. The instant process employs an efficient diastereoselective 2,3-Wittig rearrangement of * small Greek alpha *-allyloxy amide enolates mediated by a chiral auxiliary to provide acyclic and cyclic precursors.

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Номер: AT0000512129T
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Номер: AU2017278093A1
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Номер: AU2013272015A1
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08-05-1984 дата публикации

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Номер: CA1167056A
Принадлежит: BAYER AG, BAYER AKTIENGESELLSCHAFT

Mo-2274 LeA 20,595 PROCESS FOR THE PRODUCTION OF N,O-DISUBSTITUTED URETHANES AND USE THEREOF AS STARTING MATERIALS FOR THE PRODUCTION OF ORGANIC ISOCYANATES The present invention is directed to a process for the production of N,O-disubstituted urethanes comprising reacting N-mono- or N,N'-disubstituted ureas or linear polyureas with aliphatic carbonic esters. Mo-2274 LeA 20,595 ...

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29-12-1981 дата публикации

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Номер: CA1115285A
Принадлежит: BAYER AG, BAYER AKTIENGESELLSCHAFT

PROCESS FOR THE PREPARATION OF URETHANES The instant invention relates to an improved process for the preparation of urethanes by the reaction of aromatic nitro compounds with alcohols and carbon monoxide in the presence of catalyst systems which contain selenium.

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29-12-1981 дата публикации

PROCESS FOR THE PREPARATION OF URETHANES

Номер: CA1115286A
Принадлежит: BAYER AG, BAYER AKTIENGESELLSCHAFT

PROCESS FOR THE PREPARATION OF URETHANES ABSTRACT OF THE DISCLOSURE The instant invention relates to an improved pro-cess for the preparation of urethanes by the reaction of aromatic nitro compounds with alcohols and carbon monoxide in the presence of catalyst systems which contain selenium.

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29-12-1981 дата публикации

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01-08-2006 дата публикации

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A process for preparing a compound of the formula useful as a non-steroidal glucocorticoid receptor modulator.

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11-12-2008 дата публикации

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Номер: CA0002591431A1
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This invention relates to a process for the preparation of an aminoalkyl phenyl carbamate compound of formula 1, (see formula I) wherein R1 and R2 independently are hydrogen or C1-6 alkyl; R3 and R4 are the same or different and each is a lower alkyl; or R3 and R4 together with the nitrogen to which they are attached form a cyclic moiety of a three to eight- member ring, with or without a hetero atom like nitrogen or oxygen; R5 and R6 independently are hydrogen, linear, branched or cyclic C1-6 alkyl, allyl, propargyl or benzyl; or R5 and R6 together with the nitrogen to which they are attached form a cyclic moiety of three to eight member ring, with or without a hetero atom like nitrogen or oxygen; the carbon center marked with "*" is racemic or enantiomerically enriched (R)- or (S)- configuration; and pharmaceutically acceptable addition salts, and crystalline and amorphous forms thereof comprising the steps of: i) converting an amine R5R6NH to a carbamoylimidazolium salt of formula 3 ...

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07-12-2017 дата публикации

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Номер: CA0003024202A1
Принадлежит:

An organic amine salt compound having the general formula (I): An-[Bm+]p. In the formula, An- is anions having -n valence serving as CO2 donors, wherein n = 1, 2, or 3; Bm+ is or contains: ammonium ions, hydrazine ions and/or organic amine B cations; m = 1-10; 0 Подробнее

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Номер: CA0002724634C

The present invention provides a method for producing N-substituted carbamic acid-O-aryl ester derived from a compound having an ureido group, the method comprising the step of carrying out esterification or esterification and transesterification from the compound having the ureido group and a hydroxy composition containing one type or a plurality of types of hydroxy compounds.

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26-01-1991 дата публикации

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Номер: CA0002020692A1
Принадлежит:

Mo-3427 LeA 27,021 A PROCESS FOR THE PREPARATION OF MONO- AND OLIGOURETHANES This invention relates to a process for the preparation of N,N-disubstituted mono- and oligourethanes by the reaction of N-aromatically, N-aliphatically, N-cyclo-aliphatically, and N-araliphatically substituted mono- and oligourethanes with dialkyl carbonates in the presence of at least stoichiometrically equivalent quantities of solid alkali or alkaline-earth carbonate in excess dialkyl carbonate and/or an aprotic organic solvent and in the presence of a phase transfer catalyst. Le A 27 021 ...

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17-09-1998 дата публикации

PROCESS FOR THE PREPARATION OF N-CARBOXYALKYL-3-FLUORO-4-DIALKLYLAMIOANILINES

Номер: CA0002283336A1
Принадлежит:

The present invention relates to a method for producing N-carboxyalkyl-3-fluoro-4-dialkylaminonilines by reacting an ortho-nitrochlorobenzene of formula (1), wherein X stands for Cl or F, with a secondary amine of formula (2) HNR1R2, wherein R1 and R2 are independently similar or different and stand for an alkyl radical with 1 to 10 carbon atoms or jointly form a ring with 3 to 7 links together with the N atom on which they stand, in the presence of a base in the presence or absence of a solvent agent at -10 to 120 ~C in a first step. In a second step, the 2-chloro-4-dialkylamino-5-fluoronitrobenzene is made to react with hydrogen at 30 to 150 ~C and at 1 to 100 bars in the presence of a base and a noble metal catalyst. In a third step, the 3-fluoro-4-dialkylaminoaniline is extracted from the reaction mixture with an aqueous acid solution in the form of a salt dissolved in water, the aqueous phase is separated and the salt from the 3-fluoro-4-dialkylaminoaniline dissolved in water is made ...

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15-10-2002 дата публикации

METHOD FOR PRODUCING ETHERS OF ARYLIMINOMETHYLCARBAMINE ACID

Номер: UA0000071664C2
Автор:
Принадлежит:

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29-07-2016 дата публикации

DERIVATIVE OF PHENOL, METHOD OF ITS PRODUCTION AND ITS USE IN MEDICINE

Номер: EA0201592144A1
Автор:
Принадлежит:

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20-01-2016 дата публикации

Method for producing m-xylylene diisocyanate

Номер: CN0105263903A
Принадлежит:

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14-11-1980 дата публикации

METHOD OF PREPARATION OF CARBAMATES

Номер: FR0002295019B1
Автор:
Принадлежит:

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25-04-1969 дата публикации

PROCESS FOR THE PREPARATION OF 2-CHLOROALKYL ISOCYANIDE DICHLORIDE IN ADDITION TO DICHLOROALKANES

Номер: FR0001565023A
Автор:
Принадлежит:

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23-01-2019 дата публикации

플로오르화 2-아미노-4-(치환된 아미노)페닐 카르밤산염 유도체

Номер: KR1020190008411A
Принадлежит:

... 본 출원은 KCNQ2/3 칼륨 채널 조절제로서의 2-아미노-4-(치환 아미노)페닐 카르밤산염 유도체, 또는 약제학적으로 허용 가능한 염 또는 이의 용매 화합물, 및 이를 사용하는 방법에 관한 것이다.

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19-07-2007 дата публикации

NOVEL PROCESS

Номер: WO000002007080430A1
Принадлежит:

The present invention relates to a process for the preparation of a carbamoyl chloride RR’N-CO-Cl (I).

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09-07-2002 дата публикации

Process for preparing aryl-iminomethyl-carbamino acid esters

Номер: US0006417382B1
Принадлежит: Boehringer Ingelheim Pharma KG

The invention relates to a process suitable for large-scale industrial use for preparing compounds of general formula (I) wherein: R1 denotes a group selected from among methyl, ethyl, propyl, cyclopentyl, cyclohexyl, phenyl, benzyl and —C(Me2)phenyl, each of which is optionally mono-, di- or trisubstituted by hydroxy; and, R2 denotes a group selected from among methyl, ethyl, propyl and benzyl.

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26-06-2003 дата публикации

Process for the preparation of non-steroidal glucocorticoid receptor modulators

Номер: US20030120081A1
Автор: Jerry Murry, Timothy White
Принадлежит:

A process for preparing a compound of the formula useful as a non-steroidal glucocorticoid receptor modulator.

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22-03-2018 дата публикации

(HETERO)ARYL CYCLOPROPYLAMINE COMPOUNDS AS LSD1 INHIBITORS

Номер: US20180079709A1
Принадлежит:

The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection. 1140-. (canceled)141. A compound chosen from N-(4′-((trans)-2-((4-aminocyclohexyl)amino) cyclopropyl)-[1 ,1′-biphenyl]-3-yl)-2-cyanobenzenesulfonamide , an optically active stereoisomer thereof , and a salt or solvate thereof.142. The compound of claim 141 , wherein the compound is an optically active stereoisomer.143. The compound of claim 141 , wherein the compound is N-(4′-((trans)-2-((4-aminocyclohexyl)amino) cyclopropyl)-[1 claim 141 ,1′-biphenyl]-3-yl)-2-cyanobenzenesulfonamide or a pharmaceutically acceptable salt or solvate thereof.144. The compound of claim 141 , wherein the compound is a hydrochloride salt of N-(4′-((trans)-2-((4-aminocyclohexyl)amino) cyclopropyl)-[1 claim 141 ,1′-biphenyl]-3-yl)-2-cyanobenzenesulfonamide.145. A pharmaceutical composition comprising a compound chosen from N-(4′-((trans)-2-((4-aminocyclohexyl)amino)cyclopropyl)-[1 claim 141 ,1′-biphenyl]-3-yl)-2-cyanobenzenesulfonamide claim 141 , an optically active stereoisomer thereof claim 141 , and a pharmaceutically acceptable salt or solvate thereof claim 141 , and a pharmaceutically acceptable carrier.146. The pharmaceutical composition of claim 145 , wherein the compound is an optically active stereoisomer.147. The pharmaceutical composition of claim 145 , wherein the compound is N-(4′-((trans)-2-((4-aminocyclohexyl)amino)cyclopropyl)-[1 claim 145 ,1′-biphenyl]-3-yl)-2-cyanobenzenesulfonamide or a pharmaceutically acceptable salt or solvate thereof.148. The pharmaceutical composition of claim 145 , wherein the compound is a hydrochloride salt of N-(4′-((trans)-2-((4-aminocyclohexyl)amino)cyclopropyl)-[1 claim 145 ,1′-biphenyl]-3-yl)-2-cyanobenzenesulfonamide.149. A method of treating cancer ...

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27-10-2020 дата публикации

High water content ophthalmic devices

Номер: US0010816698B2
Принадлежит: Bausch & Lomb Incorporated, BAUSCH & LOMB

An ophthalmic device is disclosed which is a polymerization product of a monomeric mixture comprising: (a) a major amount of one or more first non-silicone-containing hydrophilic monomers; (b) one or more hydrophobic monomers; and (c) a crosslinking agent mixture comprising (i) one or more di-, tri- or tetra(meth)acrylate-containing crosslinking agents and (ii) one or more di-, tri- or tetracarbamate-containing crosslinking agents, wherein the ophthalmic device has an equilibrium water content of at least about 65 weight percent.

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02-07-2008 дата публикации

METHOD OF OBTAINING PHENYL CARBAMATES

Номер: EP0001939172A2
Принадлежит:

The invention relates to a method of obtaining phenyl carbamates (I), wherein R1 is lower alkyl C1-C5 or benzyl and R2 is methyl, ethyl or propyl, consisting in reacting L-(S)-3-[(1-methylamino)ethyl]phenol, in the presence of a base, with a carbamoyl halide in order to obtain an intermediate and, subsequently, subjecting said intermediate to a reducing amination reaction or a methylation reaction by reacting same with a methyl halide. The above-mentioned compounds (I) include rivastigmine, a compound that inhibits cholinesterase in the central nervous system, and can be used in the treatment of neurodegenerative diseases (E.g. senile dementia and Alzheimer's disease).

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06-10-2010 дата публикации

METHOD FOR PRODUCING AMINES FROM HYDROXAMIC ACIDS

Номер: EP1904433B1
Принадлежит: Archimica GmbH

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05-10-2018 дата публикации

(ГЕТЕРО)АРИЛЦИКЛОПРОПИЛАМИНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ LSD1

Номер: RU2668952C2

Изобретение относится к новому (гетеро)арилциклопропиламину формулы I или его фармацевтически приемлемой соли, где заместители -А-В и -NH-D циклопропильного фрагмента могут находиться в транс-конфигурации или соединение может быть оптически активным стереоизомером. Соединения обладают свойствами ингибитора лизинспецифической деметилазы-1 (LSD1) и могут найти применение для лечения рака, выбранного из группы, включающей рак молочной железы, рак легких, рак предстательной железы, колоректальный рак, рак головного мозга, рак кожи, рак крови, лейкоз, лимфому и миелому. При этом лейкоз может представлять собой острый миелолейкоз (ОМЛ), хронический миелолейкоз (ХМЛ), хронический нейтрофильный лейкоз, хронический эозинофильный лейкоз, хронический лимфолейкоз (ХЛЛ), острый лимфобластный лейкоз (ОЛЛ) и волосатоклеточный лейкоз. Соединения также могут найти применение для лечения или предупреждения вирусной инфекции, в том числе для лечения или предупреждения реактивации вируса после латентного периода, который связан с LSD1. В соединении формулы IА обозначает фенил, нафтил, пиридил, тиофенил, пирролил, фуранил или тиазолил, где указанный фенил, указанный нафтил, указанный пиридил, указанный тиофенил, указанный пирролил, указанный фуранил или указанный тиазолил необязательно замещен одним или большим количеством R; В обозначает водород, Rили -L-E; Е обозначает фенил, пиридинил, пиразолил или индазолил, где указанный фенил, указанный пиридинил, указанный пиразолил или указанный индазолил необязательно замещен одним или большим количеством R; L обозначает связь, -О-, -NH-, -CH-NH- или -СН-О-, где указанные группы -CH-NH- и -СН-О- связаны с кольцом А через атом N или О соответственно и связаны с кольцом Е через группу -СН-, содержащуюся в указанных группах -CH-NH- и -СН-О-; D выбран из D1, D2, D3 и D4:где циклобутильное кольцо, содержащееся в D1, циклопентильное кольцо, содержащееся в D2, циклогексильное кольцо, содержащееся в D3, и циклогептильное кольцо, содержащееся в D4, ...

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26-07-2022 дата публикации

СПОСОБ ПОЛУЧЕНИЯ ПРОИЗВОДНЫХ 7H-ПИРРОЛО[2,3-D]ПИРИМИДИНА И ПРОМЕЖУТОЧНЫХ ПРОДУКТОВ ДЛЯ ИХ СИНТЕЗА

Номер: RU2776802C2

Настоящее изобретение относится к способу получения соединения, имеющего формулу [17], или его соли с использованием соединения, имеющего формулу [13], или его соли. Способ включает следующие стадии, на которых: (1) соединение, имеющее формулу [10], или его соль с органической кислотой вводят в реакцию с соединением, имеющим формулу [12], с получением соединения, имеющего формулу [13], или его соли; (2) из соединения, имеющего формулу [13], или его соли удаляют бензил с получением соединения, имеющего формулу [14], или его соли; и (3) осуществляют цианоацетилирование соединения, имеющего формулу [14], или его соли с получением соединения, имеющего формулу [17], или его соли. Также предложены промежуточные соединения, используемые в синтезе. Предложенный способ позволяет получить соединение формулы [17] за меньшее количество стадий с высокой химической и оптической чистотой. 8 н. и 18 з.п. ф-лы, 15 ил., 12 табл., 50 пр.

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08-06-2018 дата публикации

СПОСОБ ПРИМЕНЕНИЯ ЦИРКОНИЕВОГО КАТАЛИЗАТОРА ДЛЯ ПОЛУЧЕНИЯ МАТЕРИАЛОВ, СОДЕРЖАЩИХ КАРБАМАТНЫЕ ФУНКЦИОНАЛЬНЫЕ ГРУППЫ

Номер: RU2016147985A
Принадлежит: БАСФ Коатингс ГмбХ

РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2016 147 985 A (51) МПК C08G 71/04 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2016147985, 14.04.2015 (71) Заявитель(и): БАСФ КОАТИНГС ГМБХ (DE) Приоритет(ы): (30) Конвенционный приоритет: (72) Автор(ы): ЯДХАВ Абхийит (US) 08.05.2014 US 14/272593 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 08.12.2016 R U (43) Дата публикации заявки: 08.06.2018 Бюл. № 16 (86) Заявка PCT: (87) Публикация заявки PCT: WO 2015/169550 (12.11.2015) R U (54) СПОСОБ ПРИМЕНЕНИЯ ЦИРКОНИЕВОГО КАТАЛИЗАТОРА ДЛЯ ПОЛУЧЕНИЯ МАТЕРИАЛОВ, СОДЕРЖАЩИХ КАРБАМАТНЫЕ ФУНКЦИОНАЛЬНЫЕ ГРУППЫ (57) Формула изобретения 1. Способ получения материала, содержащего карбаматные функциональные группы, который включает реакцию соединения карбамата с материалом, содержащим гидроксильные функциональные группы, с применением ацетилацетоната циркония в качестве катализатора. 2. Способ по п. 1, где соединение карбамата представляет собой алкилкарбамат. 3. Способ по п. 2, где соединение карбамата выбирают из группы, состоящей из метилкарбамата, этилкарбамата, н-пропилкарбамата, изопропилкарбамата, нбутилкарбамата, изобутилкарбамата, трет-бутилкарбамата, н-гексилкарбамата, 2этилгексилкарбамата, циклогексилкарбамата, фенилкарбамата, и их комбинаций. 4. Способ по любому из пп. 1-3, где материал, содержащий гидроксильные функциональные группы, представляет собой мономерное соединение, имеющее от 1 до 160 атомов углерода. 5. Способ по любому из пп. 1-3, где материал, содержащий гидроксильные функциональные группы, имеет от 12 до 72 атомов углерода и по меньшей мере две гидроксильные группы. 6. Способ по любому из пп. 1-3, где материал, содержащий гидроксильные функциональные группы, представляет собой продукт, полученный в результате восстановления продукта присоединения ненасыщенных жирных кислот. 7. Способ по любому из пп. 1-3, где материал, содержащий гидроксильные Стр.: 1 A 2 0 1 6 1 4 7 9 8 5 A Адрес для ...

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20-11-2007 дата публикации

СПОСОБ ПОЛУЧЕНИЯ СОЕДИНЕНИЙ О-КАРБАМОИЛА

Номер: RU2006115520A
Принадлежит:

... 1. Способ получения O-карбамоилированного аминоспирта формулы I где n - целое число от 0 до 5; R1, R2, R3 и R4 каждый в отдельности выбраны из группы, состоящей из водорода, алкила, циклоалкила, замещенного или незамещенного арила и арилалкила, причем арил может быть незамещенным или замещенным (X')m, где m обозначает целое число от 0 до 4 и X' выбран из группы, состоящей из водорода, алкила, алкокси, алкилтио, галогена, гидрокси, нитро и трифторметила; R5 и R6 каждый в отдельности выбраны из группы, состоящей из водорода, алкила или арилалкила, причем арил может быть незамещенным или замещенным (Х')m, причем m и X' определены выше, или R1 и R5 вместе с углеродом и азотом, к которому они присоединены образуют неконденсированное или конденсированное гетероциклическое кольцо, содержащее от 4 до 10 членов, включающий реакцию аминоспирта формулы II. где n, R1, R2, R3, R4, R5 и R6 определены выше, с цианатом и избытком кислоты в среде органического растворителя. 2. Способ по п.1, отличающийся ...

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27-02-2005 дата публикации

СПОСОБ КАРБАМОИЛИРОВАНИЯ СПИРТОВ

Номер: RU2003123791A

ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß (19) RU (51) ÌÏÊ 7 (11) 2003 123 791 (13) A C 07 D 401/06, C 07 C 269/02 ÔÅÄÅÐÀËÜÍÀß ÑËÓÆÁÀ ÏÎ ÈÍÒÅËËÅÊÒÓÀËÜÍÎÉ ÑÎÁÑÒÂÅÍÍÎÑÒÈ, ÏÀÒÅÍÒÀÌ È ÒÎÂÀÐÍÛÌ ÇÍÀÊÀÌ (12) ÇÀßÂÊÀ ÍÀ ÈÇÎÁÐÅÒÅÍÈÅ (21), (22) Çà âêà: 2003123791/04, 11.01.2002 (71) Çà âèòåëü(è): ÓÎÐÍÅÐ-ËÀÌÁÅÐÒ ÊÎÌÏÀÍÈ ËËÑ (US) (30) Ïðèîðèòåò: 31.01.2001 US 60/265,502 (72) Àâòîð(û): ÝËËÈÑ Äæåéìñ Ýäâàðä (US) (85) Äàòà ïåðåâîäà çà âêè PCT íà íàöèîíàëüíóþ ôàçó: 30.07.2003 (74) Ïàòåíòíûé ïîâåðåííûé: Íàçèíà Åëåíà Åâãåíüåâíà (86) Çà âêà PCT: IB 02/00082 (11.01.2002) Àäðåñ äë ïåðåïèñêè: 129010, Ìîñêâà, óë. Á.Ñïàññêà , 25, ñòð.3, ÎÎÎ "Þðèäè÷åñêà ôèðìà Ãîðîäèññêèé è Ïàðòíåðû", ïàò.ïîâ. Å.Å.Íàçèíîé R U Ôîðìóëà èçîáðåòåíè 1. Ñïîñîá êàðáàìîèëèðîâàíè ñïèðòà, âêëþ÷àþùèé âçàèìîäåéñòâèå ñïèðòà ñ öèàíàòîì íàòðè â ïðèñóòñòâèè ìåòàíñóëüôîêèñëîòû â áåçâîäíûõ óñëîâè õ. 2. Ñïîñîá ïî ïóíêòó 1, ãäå ñïèðò äîïîëíèòåëüíî ñîäåðæèò ñóëüôåíèëüíóþ ÷àñòü è àçîòñîäåðæàùóþ ãåòåðîöèêëè÷åñêóþ ÷àñòü. 3. Ñïîñîá ïî ïóíêòó 1, ãäå ñïèðòîì âë åòñ êàïðàâèðèíñóëüôåíèëîâûé ñïèðò. 4. Ñïîñîá êàðáàìîèëèðîâàíè ñïèðòà, âêëþ÷àþùèé ñìåøèâàíèå ñïèðòà ñ öèàíàòîì â èíåðòíîì ðàñòâîðèòåëå â áåçâîäíûõ óñëîâè õ, ãäå ñïèðò ñîäåðæèò äðóãèå ÷àñòè; îõëàæäåíèå îáðàçóþùåéñ ðåàêöèîííîé ñìåñè äî òåìïåðàòóðû îò ïðèìåðíî -25 äî ïðèìåðíî 40°Ñ; äîáàâëåíèå êèñëîòû ê îõëàæäåííîé ðåàêöèîííîé ñìåñè ñî ñêîðîñòüþ, ïîääåðæèâàþùåé òåìïåðàòóðó íèæå ïðèìåðíî 0°Ñ; ïåðåìåøèâàíèå ðåàêöèîííîé ñìåñè, ñîäåðæàùåé ìåòàíñóëüôîêèñëîòó, ïðè òåìïåðàòóðå îò ïðèìåðíî -10°Ñ äî ïðèìåðíî 0°Ñ â òå÷åíèå ïðèìåðíî îò 8 äî 10 ÷; è ãàøåíèå ðåàêöèîííîé ñìåñè âîäîé. 5. Ñïîñîá ïî ïóíêòó 4, ãäå ñïèðò ñîäåðæèò ñóëüôåíèëüíóþ ÷àñòü è àçîòñîäåðæàùóþ ãåòåðîöèêëè÷åñêóþ ÷àñòü, êîòîðà âûáðàíà èç èìèäàçîëèëà è ïèðèäèëà. 6. Ñïîñîá ïî ïóíêòó 4, ãäå ñïèðòîì âë åòñ êàïðàâèðèíñóëüôåíèëîâûé ñïèðò. 7. Ñïîñîá ïî ïóíêòó 4, ãäå öèàíàò ïðåäñòàâë åò öèàíàò íàòðè , öèàíàò êàëè , öèàíàò öåçè èëè èõ ñìåñü, è êèñëîòà ïðåäñòàâë åò ìåòàíñóëüôîêèñëîòó, óêñóñíóþ êèñëîòó, ñåðíóþ êèñëîòó èëè èõ ñìåñü. Ñòðàíèöà: 1 RU A 2 0 0 3 1 2 3 ...

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02-03-2000 дата публикации

One-pot preparation of N-alkoxycarbonyl-protected acrylate, phosphonate or phosphinate esters comprises reacting N-acyl-protected esters with dicarbonate ester and then hydrazine

Номер: DE0019840861A1
Принадлежит:

One-pot process for preparing N-alkoxycarbonyl-protected esters (I)-(III) comprises reacting N-acyl-protected esters (IV) or N-benzoyl-protected esters (V) or (VI) with a dicarbonate ester (VII) in a dry organic solvent at -50 to +50 deg C in the presence of a base, cooling the reaction mixture, adding methanol and hydrazine, and purifying the reaction mixture. One-pot process for preparing N-alkoxycarbonyl-protected esters of formula (I)-(III) comprises reacting N-acyl-protected esters of formula (IV) or N-benzoyl-protected esters of formula (V) or (VI) with a dicarbonate ester of formula (VII) in a dry organic solvent at -50 to +50 deg C in the presence of a base, cooling the reaction mixture, adding methanol and hydrazine, and purifying the reaction mixture. R<1> = H, optionally substituted alkyl, optionally substituted aryl, heteroaryl, cycloalkyl, alkoxy, alkylamino, aryloxy or arylamino; R<2> = methyl, substituted alkyl, optionally substituted aryl or cycloalkyl; R<3> = OR<2>, optionally ...

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13-08-2015 дата публикации

Process for preparing the anti-tumor agent 6-(7-((1-aminocyclopropyl) methoxy)-6-methoxyquinolin-4-yloxy)-N-methyl-1-naphthamide and its crystalline

Номер: AU2014207482A1
Принадлежит:

The present invention relates a new process to synthesize 6-(7-((l-aminocyclo-propyl)- methoxy)-6-methoxyquinolin-4-yloxy)-N-methyl- l -naphthamide (AL3810) by deprotection of substituted benzyl 1 -((6-methoxy-4-(5-(methylcarbamoyl)naphthalen-2-yloxy)quinolin-7-yloxy)- methyl)cyc-lopropylcarbamate (Formula I) under a diluted or weak acidic condition. A stable crystalline form of 6-(7-((l-aminocyclo-propyl)-methoxy)-6-methoxyquinolin-4-yloxy)-N- methyl- 1 -naphthamide has also been prepared.

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14-12-2017 дата публикации

FLUORINATED 2-AMINO-4-(SUBSTITUTED AMINO)PHENYL CARBAMATE DERIVATIVES

Номер: CA0003023340A1
Принадлежит:

The application relates to 2-amino-4-(substituted amino)phenyl carbamate derivatives, or pharmaceutically acceptable salts or solvates thereof, as KCNQ2/3 potassium channel modulators, and methods of their uses.

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10-05-1988 дата публикации

PROCESS FOR THE PRODUCTION OF URETHANES

Номер: CA1236479A
Принадлежит: BAYER AG, BAYER AKTIENGESELLSCHAFT

A PROCESS FOR THE PRODUCTION OF URETHANES Urethanes are made by reacting an organic nitro compound with an organic compound containing at least one hydroxyl group in the presence of carbon monoxide, hydrogen and a catalyst system. The carbon monoxide and hydrogen are used in quantities such that the molar ratio of CO to H2 is from 0.3:1 to 3:1. The catalyst system is made up of at least one noble metal or compound of a noble metal from Group VIIIB of the Periodic System of Elements, at least one organic nitrogen base and a co-catalyst combination of iron or copper oxidic or hydroxidic compound and a chloride compound. The product urethanes are useful in the production of isocyanates and pesticides.

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31-01-1989 дата публикации

PROCESS FOR THE PREPARATION OF N,O-SUBSTITUTED MONO- AND/OR POLYURETHANES

Номер: CA1249596A
Принадлежит: BASF AG, BASF AKTIENGESELLSCHAFT

PROCESS FOR THE PREPARATION OF N,o-SUBSTITUTED MONO- AND/OR POLYURETHANES The invention describes a process for the preparation of N,o-substituted mono- and/or polyurethanes of formula R1¢-NHCOOR2!n, in which R1 is an aliphatic, cycloaliphatic, aromatic, araliphatic, or heterocyclic radical, which may be substituted, R2 is an aliphatic, cycloaliphatic, or araliphatic radical which may be substituted with alkoxy or polyoxyalkylene groups, and n is a whole number from 1 to 5, through the reaction of N-substituted allophanates and/or polyallophanates with alcohols R2OH in the presence or absence of catalysts at temperatures of at least 160.degree.C, preferably from 165.degree. to 250.degree.C.

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03-08-2021 дата публикации

INTEGRATED PROCESS FOR CARBON CAPTURE AND ENERGY PRODUCTION

Номер: CA2970471C
Автор: NOVEK ETHAN, NOVEK, ETHAN
Принадлежит: NOVEK ETHAN, NOVEK, ETHAN

The present invention pertains to new methods for generating energy and useful nitrogen compounds from captured carbon dioxide. It involves employing an osmotic engine, draw solution, and feed solution. An osmotic gradient between the solutions assists in generating energy and a solution of ammonium carbonate, ammonium bicarbonate or mixture thereof. This solution may be decomposed to form ammonia, carbon dioxide, a precipitate, or a mixture thereof.

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01-03-2012 дата публикации

One-pot production of carbamates using solid catalysts

Номер: US20120053359A1

The invention relates to the production of carbamates in a single reactor (one-pot) using solid catalysts, involving the reaction between at least one nitro compound, an organic carbonate of formula (OR)(OR′)C═O, a gas selected from hydrogen gas and a mixture of gases containing hydrogen and hydrogen precursor compounds, and a catalyst that has at least one metallic oxide and can also contain an element of groups 8, 9, 10 and 11 of the periodical table. The carbonates obtained can be transformed into their corresponding isocyanates.

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15-08-2013 дата публикации

Process for preparing carboxamidine compounds

Номер: US20130211130A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

The present invention relates to a process of making a compound of formula (I): Wherein, R 1 , R 2 , R 4 and X are as defined herein.

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05-09-2013 дата публикации

PROCESS FOR THE PREPARATION OF 2-PHENYL-1,3-PROPANEDIOL

Номер: US20130231496A1
Принадлежит: Taro Pharmaceutical Industries Ltd.

The present invention is related to a novel synthetic procedure that provides a simple, safe and commercially valuable method for the preparation of 2-phenyl-1,3-propanediol. The process for the preparation of 2-phenyl-1,3-propanediol involves reducing diethyl phenylmalonate with sodium borohydride (NaBH) in the presence of an alkali metal dihydrogen phosphate buffer or the hydrate thereof. 1. A process for preparing 2-phenyl-1 ,3-propanediol comprising the steps of:(a) reacting diethyl phenylmalonate with sodium borohydride in the presence of an alkali metal dihydrogen phosphate or the hydrate thereof to yield 2-phenyl-1,3-propanediol;(b) quenching the reaction of step (a);(c) basifying the reaction mixture of step (b) and extracting the 2-phenyl-1,3-propanediol into an organic solvent to form an organic layer; and(d) isolating the 2-phenyl-1,3-propanediol from the organic layer of step (c).2. The process of claim 1 , wherein the alkali metal dihydrogen phosphate of step (a) is sodium dihydrogen phosphate or the hydrate thereof claim 1 , potassium dihydrogen phosphate or the hydrate thereof.3. The process of claim 2 , wherein the alkali metal dihydrogen phosphate of step (a) is sodium dihydrogen phosphate monohydrate or potassium dihydrogen phosphate monohydrate.4. The process of claim 1 , wherein the alkali metal dihydrogen phosphate maintains the pH of the reaction of step (a) within a range of between about 5.0 to about 6.0.5. The process of claim 1 , wherein the isolated 2-phenyl-1 claim 1 ,3-propanediol of step (d) comprises not more than about 1% of total impurities.6. The process of claim 1 , wherein the reaction of step (a) is performed in the presence of a polar solvent.7. The process of claim 6 , wherein the polar solvent is selected from the group consisting of dioxane claim 6 , tetrahydrofuran (THF) claim 6 , dimethoxyethane (Glyme) claim 6 , bis(2-methoxyethyl)ether (Diglyme) claim 6 , isopropyl alcohol and ethanol claim 6 , or any combination thereof. ...

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05-12-2013 дата публикации

PROCESSES AND REAGENTS FOR MAKING DIARYLIODONIUM SALTS

Номер: US20130324718A1
Автор: DiMagno Stephen
Принадлежит:

This invention relates to processes and reagents for making diaryliodonium salts, which are useful for the preparation of fluorinated and radiofluorinated aromatic compounds. 2. The process of claim 1 , wherein the process is carried out in the absence of added acid.3. The process of claim 1 , wherein the process utilizes (1-chloromethyl-4-fluoro-1 claim 1 ,4-diazoniabicyclo[2.2.2]octane)bis(tetrafluoroborate).4. The process of claim 1 , wherein the process utilizes (1-fluoro-4-methyl-1 claim 1 ,4-diazoniabicyclo[2.2.2]octane)bis(tetrafluoroborate).5. The process of claim 1 , wherein the process utilizes N-fluoro-2 claim 1 ,3 claim 1 ,4 claim 1 ,5 claim 1 ,6-pentachloropyridinium tetrafluoroborate.6. The process of claim 1 , wherein the process utilizes less than 2 equivalents of (1-chloromethyl-4-fluoro-1 claim 1 ,4-diazoniabicyclo[2.2.2]octane)bis(tetrafluoroborate) claim 1 , (1-fluoro-4-methyl-1 claim 1 ,4-diazoniabicyclo[2.2.2]octane)bis(tetrafluoroborate) claim 1 , or optionally substituted N-fluoropyridinium tetrafluoroborate for 1 equivalent of the compound of Formula II.7. The process of claim 1 , wherein the process utilizes less than 1.5 equivalents of (1-chloromethyl-4-fluoro-1 claim 1 ,4-diazoniabicyclo[2.2.2]octane)bis(tetrafluoroborate) claim 1 , (1-fluoro-4-methyl-1 claim 1 ,4-diazoniabicyclo[2.2.2]octane)bis(tetrafluoroborate) claim 1 , or optionally substituted N-fluoropyridinium tetrafluoroborate for 1 equivalent of the compound of Formula II.8. The process of claim 1 , wherein each X is claim 1 , independently claim 1 , a ligand that is a conjugate base of an acid HX claim 1 , wherein HX has a pKa of less than or equal to 5.9. The process of claim 1 , wherein each X is O(C═O)CH.10. The process of claim 1 , wherein the tetravalent silicon moiety is (R)Si—X claim 1 , wherein each Ris claim 1 , independently claim 1 , Calkyl or aryl.11. The process of claim 10 , wherein each Ris methyl.12. The process of claim 10 , wherein (R)Si—X is (CH)Si—X.13. The ...

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23-01-2020 дата публикации

INTEGRATED PROCESS FOR PRODUCTION OF GLYCEROL CARBONATE (4-HYDROXYMETHYL-2-OXO-1, 3-DIOXOLANE) AND UREA

Номер: US20200024227A1
Принадлежит:

Systems and methods for integrated glycerol carbonate and/or urea production. This disclosure pertains to development of a process for production of glycerol carbonate and/or urea from ammonia, carbon dioxide and glycerol. The process integrates glycerol carbonate production into a urea production process. The urea produced in the production facility may be used to produce glycerol carbonate by reacting urea with glycerol. The ammonia generated by glycerol carbonate production may be recycled back to urea production. Unreacted urea from the glycerol carbonate production may be separated and recycled to the urea product stream. The systems and methods can reduce the cost for urea production and increase product value of the excessive glycerol produced from other chemical plants. 1. A method of producing glycerol carbonate and/or urea , the method comprising steps as follows:(1) employing carbon dioxide and ammonia in synthesizing the urea;(2) reacting at least some of the urea with glycerol to form glycerol carbamate and ammonia;(3) decomposing the glycerol carbamate to form the glycerol carbonate and ammonia;(4) feeding at least some of the ammonia from step (2) and/or step (3) to step (1) for the synthesizing;(5) transferring any unreacted urea from step (2) to a urea product stream; and(6) flowing the glycerol carbonate from step (3) in a glycerol carbonate product stream.2. The method of claim 1 , wherein step (1) comprises:(a) reacting the ammonia with the carbon dioxide to form ammonium carbamate, and(b) decomposing the ammonium carbamate to form water and the urea.3. The method of claim 2 , wherein step (1) further comprises:(c) heating the urea, unreacted ammonia and ammonium carbamate from steps (a) and (b) to further decompose ammonium carbamate and form urea and water;(d) concentrating the urea from the water and urea from steps (b) and (c); and(e) granulating the concentrated urea from step (d) to form granulated urea.4. The method of any of claim 1 , ...

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01-05-2014 дата публикации

1,3-DI-OXO-INDENE DERIVATIVE, PHARMACEUTICALLY ACCEPTABLE SALT OR OPTICAL ISOMER THEREOF, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING SAME AS AN ANTIVIRAL, ACTIVE INGREDIENT

Номер: US20140121187A1
Принадлежит:

Disclosed are 1,3-Dioxoindene derivatives, pharmaceutically acceptable salts thereof or enantiomers, a preparation method thereof, and a pharmaceutical composition for the prevention or treatment of viral diseases, comprising the same as an active ingredient. The 1,3-Dioxoindene derivatives have excellent inhibitory activity against picornaviruses including coxsackie-, entero-, echo-, Polio-, and rhinoviruses, as well as exhibiting low cytotoxicity, so that they can be useful as an active ingredient of a pharmaceutical composition for the prevention or treatment of viral diseases including poliomyelitis, paralysis, acute hemorrhagic conjunctivitis, viral meningitis, hand-foot-and-mouth disease, vesicular disease, hepatitis A, myositis, myocarditis, pancreatitis, diabetes, epidemic myalgia, encephalitis, flu, herpangina, foot-and-mouth disease, asthma, chronic obstructive pulmonary disease, pneumonia, sinusitis or otitis media. 3. The 1 claim 1 ,3-Dioxoindene derivatives claim 1 , pharmaceutically-acceptable salt thereof or optical isomer thereof as set forth in claim 1 , wherein claim 1 , A claim 1 , A claim 1 , Aand Aare claim 1 , either independently or optionally claim 1 , any one selected from a group consisting of —H claim 1 , halogen and —NRR;{'sup': 1', '2', '1', '2, 'G is —OH, —NR(C═O)Ror —NR(C═O)OR;'}{'sup': 1', '2', '3', '4', '1', '2, 'sub': 1', '10, 'D, D, Dand Dare, either independently or optionally, any one selected from a group consisting of halogen, C˜Cstraight- or side-chain alkyl and —NR(C═O)R;'}{'sup': 1', '1', '1', '1', '2, 'E is —H, —OH, —OR, —O(C═O)R, —O(C═O)ORor —O(C═O)NRR;'}{'sup': 1', '2', '3, 'sub': 1', '8', '1', '4', '6', '10, 'R, Rand Rare, each independently, hydrogen, nonsubstituted or phenyl-substituted C˜Cstraight- or side-chain alkyl, nonsubstituted or phenyl-substituted C˜Cstraight- or side-chain alkenyl or C˜Caryl;'}X and Y are oxygen;{'sup': 1', '2', '3, 'Z, Zand Zare carbon;'}n is integer between 1˜3; and{'img': {'@id': 'CUSTOM- ...

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13-02-2020 дата публикации

HIGH WATER CONTENT OPHTHALMIC DEVICES

Номер: US20200049857A1
Принадлежит:

An ophthalmic device is disclosed which is a polymerization product of a monomeric mixture comprising: (a) a major amount of one or more first non-silicone-containing hydrophilic monomers; (b) one or more hydrophobic monomers; and (c) a crosslinking agent mixture comprising (i) one or more di-, tri- or tetra(meth)acrylate-containing crosslinking agents and (ii) one or more di-, tri- or tetracarbamate-containing crosslinking agents, wherein the ophthalmic device has an equilibrium water content of at least about 65 weight percent. 1. An ophthalmic device which is a polymerization product of a monomeric mixture comprising: (a) a major amount of one or more first non-silicone-containing hydrophilic monomers; (b) one or more hydrophobic monomers; and (c) a crosslinking agent mixture comprising (i) one or more di- , tri- or tetra(meth)acrylate-containing crosslinking agents and (ii) one or more di- , tri- or tetracarbamate-containing crosslinking agents , wherein the ophthalmic device has an equilibrium water content of at least about 65 weight percent.2. The ophthalmic device of claim 1 , wherein the major amount of the one or more first non-silicone-containing hydrophilic monomers present in the monomeric mixture is an amount greater than about 80 weight percent claim 1 , based on the total weight of the monomeric mixture.3. The ophthalmic device of claim 1 , wherein the one or more first non-silicone-containing hydrophilic monomers is a cyclic lactam.4. The ophthalmic device of claim 3 , wherein the cyclic lactam is selected from the group consisting of N-vinyl-2-pyrrolidone claim 3 , N-vinyl caprolactam claim 3 , N-vinyl-2-piperidone and mixtures thereof.5. The ophthalmic device of claim 1 , wherein the monomeric mixture further comprises a minor amount of one or more second non-silicone-containing hydrophilic monomers.6. The ophthalmic device of claim 5 , wherein the one or more second non-silicone-containing hydrophilic monomers is one or more non-silicone- ...

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03-03-2016 дата публикации

PHENOL DERIVATIVE AND PREPARATION METHOD AND USE IN MEDICINE THEREOF

Номер: US20160060197A1
Принадлежит: Sichuan Haisco Pharmaceutical Co., Ltd.

The present invention relates to a phenol derivative and the preparation method and use in medicine thereof, and particular to a phenol derivative represented by general formula (A) or a stereoisomer, a solvate, a metabolite, a prodrug, a pharmaceutically acceptable salt or a cocrystal thereof, a preparation method thereof, a pharmaceutical composition comprising the same, and use of the compound or composition of the present invention in the field of the central nervous system; wherein the definitions of substituents in general formula (A) are the same as those in the Description. 19. The compound according to claim 1 , or a stereoisomer claim 1 , a solvate claim 1 , a metabolite claim 1 , a prodrug claim 1 , a pharmaceutically acceptable salt claim 1 , or a cocrystal thereof claim 1 ,wherein the salt includes an ammonium salt, a potassium salt, a sodium salt, a calcium salt, a magnesium salt, a tetramethylammonium salt, a tetraethylammonium salt, a tetrapropylammonium salt, a tetrabutylammonium salt, a tetra(isopentyl)ammonium salt, an ethanolamine salt, a diethanolamine salt, a triethanolamine salt, trimethylamine salt, N-methylglucosamine salt, hydrochloride sulfate, phosphate, acetate, trifluoroacetate, fumarate, hemifumarate, maleate, malate, citrate, succinate, benzenesulfonate, or p-toluenesulfonate.22. A pharmaceutical composition claim 1 , comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'a compound according to , or a stereoisomer, a solvate, a metabolite, a pharmaceutically acceptable salt, a cocrystal, or a prodrug thereof; and'}one or more pharmaceutically acceptable vehicles and/or excipients.23. Use of the compound according to claim 1 , or a stereoisomer claim 1 , a solvate claim 1 , a metabolite claim 1 , a pharmaceutically acceptable salt claim 1 , a cocrystal claim 1 , or a prodrug thereof claim 1 , for the manufacture of a medicament forinducing and maintaining anesthesia in an animal or a human,facilitating sedation and hypnosis of ...

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22-03-2018 дата публикации

NOVEL CONFIGURATION AND ITS USE IN PROCESS FOR SYNTHESIS OF ALKYL CARBAMATES FROM ALKYL ALCOHOL AND UREA IN A TUBULAR REACTOR

Номер: US20180079714A1
Принадлежит:

The present invention discloses an improved catalyst free process for synthesis of alkyl carbamates in an integrated system comprising a tubular reactor and a striper. The process comprises reacting urea and an alcohol in said tubular reactor under autogeneous pressure; wherein said process provides >90% selectivity towards alkyl carbamate. The mixture of urea and alcohol is N fed to the tubular reactor at a particular feed rate. The tubular reactor is heated externally under autogeneous pressure to carry out a synthesis reaction producing alkyl carbamate and ammonia. The ammonia is removed from the tubular reactor by the striper. The tubular reactor and the stripper are arranged in series to reduce the equilibrium limitations of the reaction and drive the reaction in forward direction. 1. A catalyst free process for synthesis of alkyl carbamate within an integrated system of at least one tubular reactor and a stripper in series , comprising reacting urea and an alcohol in said tubular reactor under autogeneous pressure; wherein said process provides >90% selectivity towards alkyl carbamate.2. The catalyst free process according to claim 1 , wherein the alcohol is selected from methanol claim 1 , ethanol claim 1 , 1-propanol claim 1 , 2-propanol claim 1 , 1-butanol claim 1 , 2-butanol claim 1 , tert-butanol claim 1 , pentanol and its isomers claim 1 , hexanol and its isomers claim 1 , their higher homologues or their isomers.3. The catalyst free process according to claim 1 , wherein the temperature of the reaction mixture is in the range of 150-250 C.4. The catalyst free process according to claim 1 , wherein urea and alcohol in mole ratio 10 to 50 are fed in to the tubular reactor at a feed rate of 5-25 ml/min.5. The catalyst free process according to claim 1 , wherein said process can be carried out continuously claim 1 , semi continuously or batch wise.6. The catalyst free process according to claim 1 , wherein the process further comprises reacting said alkyl ...

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23-03-2017 дата публикации

PROPELLANE DERIVATES AND SYNTHESIS

Номер: US20170081295A1
Автор: Bunker Kevin Duane
Принадлежит:

Disclosed herein are compounds of the general Formula (I), and methods of synthesizing substituted bicyclo[1.1.1 jpentanes. The synthetic methods described herein use a [1.1.1]propellane, a Group VIII transition metal compound, a hydride source and a reagent that can contribute a substituent to form a substituted bicyclo[1.1.1]pentane, such as a compound of the general Formula (I). 1. A method for preparing a substituted bicyclo[1.1.1]pentane compound comprising:combining [1.1.1]propellane;a Group VIII transition metal compound;a hydride source; anda reagent capable of contributing all or a part of a substituent group such that bicyclo[1.1.1]pentane is substituted with the substituent group.3. The method of claim 2 , wherein Ris —N claim 2 , halogen claim 2 , —CN claim 2 , —OH claim 2 , —SCN claim 2 , —NCO claim 2 , —NO claim 2 , —C(═NOR)(CN) claim 2 , —CH(═NOR) or —COH.4. The method of claim 2 , wherein Ris an optionally substituted Calkyl claim 2 , an optionally substituted Calkenyl claim 2 , an optionally substituted Calkynyl claim 2 , an optionally substituted cycloalkyl claim 2 , an optionally substituted cycloalkenyl claim 2 , an optionally substituted cycloalkynyl claim 2 , an optionally substituted aryl claim 2 , an optionally substituted heteroaryl claim 2 , an optionally substituted heterocyclyl claim 2 , an optionally substituted aryl(Calkyl) claim 2 , an optionally substituted heteroaryl(Calkyl) claim 2 , an optionally substituted heterocyclyl(Calkyl) claim 2 , an optionally substituted alkoxy claim 2 , an optionally substituted acyl claim 2 , an optionally substituted amino claim 2 , an optionally substituted alkoxyalkyl claim 2 , an optionally substituted acylalkyl claim 2 , an optionally substituted aminoalkyl claim 2 , an optionally substituted hydroxyalkyl claim 2 , an optionally substituted haloalkyl claim 2 , an optionally substituted haloalkoxy claim 2 , an optionally substituted arylthio claim 2 , or an optionally substituted alkylthio.5. The ...

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03-07-2014 дата публикации

PREPARATION OF SITAGLIPTIN INTERMEDIATES

Номер: US20140187558A1
Автор: Casar Zdenko, Stavber Gaj
Принадлежит: Lek Pharmaceuticals D.D.

The invention relates to the preparation of chiral compounds, in particular to the preparation of chiral compounds which may be used as intermediates for the preparation of anti-diabetic agents, preferably sitagliptin. 2. The process of claim 1 , wherein in step (b) the solvent is selected from the group consisting of water claim 1 , methanol claim 1 , ethanol claim 1 , iso-propanol claim 1 , tort-butanol claim 1 , trifluoroethanol claim 1 , hexafluoro-2-propanol claim 1 , amyl alcohol and any combination thereof.3. The process of claim 1 , wherein step (b) is carried out without adding solvents.4. The process of claim 1 , wherein step (b) is carried out at a temperature of 20° C. to 100° C.6. The process of claim 1 , wherein step (b) is a non-catalyzed process.7. The process of wherein step (b) is a transition metal catalyzed process.8. The process of claim 7 , wherein in step (b) the transition metal compound is selected from the group consisting of copper compounds claim 7 , indium compounds claim 7 , zinc compounds claim 7 , iron compounds claim 7 , manganese compounds claim 7 , cerium compounds claim 7 , bismuth compounds claim 7 , scandium compounds claim 7 , ytterbium compounds claim 7 , yttrium compounds claim 7 , tin compounds and vanadium compounds.9. The process of claim 7 , wherein the transition metal catalyzed process is optionally carried out in the presence of a base claim 7 , wherein the base is selected from the group consisting of NatOBu claim 7 , KtOBu claim 7 , KCO claim 7 , NaCO claim 7 , KOAc claim 7 , NaOAc claim 7 , and any combination thereof.10. The process of claim 7 , wherein the transition metal catalyzed process is carried out in the absence of a base.11. The process of claim 1 , wherein step (b) is an acid catalyzed process.12. The process of claim 11 , wherein in step (b) the acid is a Lewis acid claim 11 , selected from the group consisting of copper(II) acetate claim 11 , copper(II) chloride claim 11 , copper(II) triflate claim 11 ...

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30-04-2015 дата публикации

(HETERO)ARYL CYCLOPROPYLAMINE COMPOUNDS AS LSD1 INHIBITORS

Номер: US20150119396A9
Принадлежит:

The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and theft use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection. 6. The compound of any of to for use as a medicament.9. A pharmaceutical composition comprising the compound of any of to and a pharmaceutically acceptable carrier.16. The compound of any of to or the compound for use as a medicament according to any of to or the pharmaceutical composition of any of to , wherein D is a cycloalkyl group having from 4 to 7 C atoms , wherein said cycloalkyl group has one or two substituents Rand is further optionally substituted with one or more R.17. The compound of any of to or the compound for use as a medicament according to any of to or the pharmaceutical composition of any of to , wherein D is a cycloalkyl group having from 4 to 7 C atoms , wherein said cycloalkyl group has one substituent Rand is further optionally substituted with one or more R.18. The compound of any of to or the compound for use as a medicament according to any of to or the pharmaceutical composition of any of to , wherein D is a cycloalkyl group having from 4 to 7 C atoms , wherein said cycloalkyl group has one substituent R.19181818. The compound of any of to or to or the compound for use as a medicament according to any of to or to or the pharmaceutical composition of any of to or to , wherein the cycloalkyl group having from 4 to 7 C atoms which forms part of D is a cyclohexyl group.222121. The compound of any of to or to or the compound for use as a medicament according to any of to or to or the pharmaceutical composition of any of to , wherein each Ris independently selected from —NRR , —NHOH , —NRCOR , —NRSOR , —NRCOOR , —NRCONRR , —NRSONRR , —CONRR , oxo , —Calkylene-NRR , —Calkylene-NHOH , —Calkyene-NRCOR , —Calkylene-NRSOR , —Calkylene-NRCOOR , —Calkylene- ...

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16-04-2020 дата публикации

DIFLUOROALKYLCYCLOPROPYL AMINO ACIDS AND ESTERS, AND SYNTHESES THEREOF

Номер: US20200115329A1
Принадлежит:

The invention provides methods of synthesizing compounds in an asymmetric or enantioenriched fashion, wherein the compounds are useful intermediates in the synthesis of viral protease inhibitors. 116-. (canceled)18. The method of claim 17 , wherein the first metal comprises TiCl claim 17 , TiOR claim 17 , CeCl claim 17 , Ce(SO) claim 17 , CaCl claim 17 , MgCl claim 17 , Ti(Oi-Pr)Cl or Ti(OEt)Cl.19. The method of claim 17 , wherein the first base is present; and the first base comprises (i-Pr)EtN claim 17 , triethylamine claim 17 , EtNH claim 17 , EtNH claim 17 , or (iPr)NH.20. The method of claim 19 , wherein the first base is triethylamine.21. The method of claim 17 , wherein the first metal is CeClor MgCl; and the first base is absent.22. The method of claim 17 , wherein the first metal is CeClor MgCl; and the first metal is present in a catalytic quantity.23. The method of claim 17 , wherein the first metal is TiCl claim 17 , TiOR claim 17 , Ti(Oi-Pr)Cl claim 17 , or Ti(OEt)Cl; and the first metal is present in a stoichiometric quantity.24. The method of claim 17 , wherein the first solvent comprises MeOH claim 17 , EtOH claim 17 , n-PrOH claim 17 , i-PrOH claim 17 , tetrahydrofuran (THF) claim 17 , methyl tert-butyl ether claim 17 , ethyl acetate claim 17 , dioxane claim 17 , DMF claim 17 , acetonitrile claim 17 , or DMSO.25. The method of claim 24 , wherein the first metal is TiCl claim 24 , TiOR claim 24 , Ti(Oi-Pr)Cl claim 24 , or Ti(OEt)Cl.26. The method of claim 24 , wherein the first metal is CeClor MgCl.27. The method of claim 17 , wherein the first temperature is from about −10° C. to about 15° C.28. The method of claim 17 , wherein the first period of time is from about 6 h to about 18 h.29. The method of claim 17 , further comprising heating the first product mixture at a second temperature.30. The method of claim 29 , wherein the first product mixture is maintained at the second temperature for a second period of time.31. The method of claim 17 , ...

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26-05-2016 дата публикации

Method for producing meta-xylylenediisocyanates

Номер: US20160145201A1
Принадлежит: Mitsui Chemicals Inc

A method for producing meta-xylylenediisocyanates includes a reaction step in which monohalogenated benzenes, formaldehydes, and an amide compound represented by general formula (1) below are allowed to react in the presence of an acidic liquid to produce a bisamide compound; a dehalogenation step in which in the bisamide compound, the halogen atom derived from the monohalogenated benzenes is replaced with a hydrogen atom; and a thermal decomposition step in which the bisamide compound from which the halogen atom is eliminated is subjected to thermal decomposition. In the reaction step, the acidic liquid contains inorganic acid, the equivalent ratio of the hydrogen atom of the inorganic acid relative to the monohalogenated benzenes is more than 14, the acidic liquid has an inorganic acid concentration of more than 90 mass %, and the reaction temperature is more than 10° C. General formula (1): wherein R 1 represents an alkoxy group or an amino group.

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28-05-2015 дата публикации

GAMMA AMINO ACID BUILDING BLOCKS

Номер: US20150148523A1
Принадлежит: WISCONSIN ALUMNI RESEARCH FOUNDATION

The invention provides compounds and methods, for example, to carry out organocatalytic Michael additions of aldehydes to cyclically constrained nitroethylene compounds catalyzed by a proline derivative to provide cyclically constrained α-substituted-γ-nitro-aldehydes. The reaction can be rendered enantioselective when a chiral pyrrolidine catalyst is used, allowing for Michael adducts in nearly optically pure form (e.g., 96 to >99% e.e.). 4. The compound of wherein Ris H or alkyl claim 3 , A-Aare each carbon claim 3 , Ris H or alkyl claim 3 , P is H claim 3 , methyl or acetyl claim 3 , and Y is nitro or protected amino.5. A method for preparing a compound of wherein Ris H comprising:contacting a cyclic compound of 5 or 6 ring atoms that includes a nitroethylene moiety within the ring and that optionally includes one or two nitrogen atoms in the ring, wherein the carbon atoms in the ring are optionally substituted and the optional nitrogen atom or atoms in the ring are optionally substituted by a nitrogen protecting group; andan aldehyde that has at least one α-hydrogen;{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'in the presence of an organic solvent, and a proline derivative, for a period of time sufficient to provide the compound of .'}6. The method of wherein the aldehyde has an α-methylene group or an α-methine group.7. The method of wherein the contacting is carried out in the presence of a carboxylic acid claim 5 , the proline derivative is a chiral pyrrolidine catalyst claim 5 , and the compound of is prepared in at least about 80% enantiomeric purity.8. The method of further comprising reducing an aldehyde moiety of the compound of to an alcohol claim 5 , oxidizing the resulting alcohol to a carboxylic acid claim 5 , reducing the nitro moiety of the compound of to an amine claim 5 , or a combination thereof.12. The method of wherein the contacting is carried out in the presence of a carboxylic acid claim 11 , the proline derivative is a chiral ...

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02-06-2016 дата публикации

PROCESS FOR THE PREPARATION OF URETHANES

Номер: US20160152559A1
Принадлежит:

Urethanes are prepared by oxidative carbonylation of at least one amino compound in the presence of carbon monoxide, oxygen and organic, at least one hydroxyl-group-carrying compound. The carbonylation is carried out in the absence of halogen-containing promoters. The carbonylation is also carried out in the presence of a metal complex catalyst which contains neutral bidentate N-chelate ligands of the (N˜N) type, two monoanionic N,O-chelate ligands of the general type (N˜O) or tetradentate dianionic chelate ligands (O˜N˜N˜O). 110-. (canceled)12. The process of claim 11 , wherein the metal complex catalyst is used in a concentration of from 0.1 to 10 mol % claim 11 , based on one mole of amino groups.13. The process of claim 11 , wherein the carbonylation is carried out in methanol claim 11 , ethanol claim 11 , n-butanol claim 11 , or 2 claim 11 ,2 claim 11 ,2-trifluoroethanol.14. The process of claim 11 , wherein ureas groups are formed during the carbonylation claim 11 , wherein these urea groups subsequently react further claim 11 , partially or completely claim 11 , with the organic hydroxyl-group-containing compound by alcoholysis to give the corresponding urethanes.15. The process of claim 11 , in which an aliphatic claim 11 , cycloaliphatic and/or aromatic mono- or di-amino compound is used.16. The process of claim 11 , in which the carbonylation is carried out in the absence of a halogenated solvent.17. A process for the preparation of isocyanates claim 11 , comprising:a) preparing a urethane by carbonylation by the process of 1, andb) thermally cleaving the urethane to obtain the isocyanate.18. The process of claim 17 , wherein the carbonylation and the thermal cleavage take place in one process step. The invention relates to a process for the preparation of urethanes and/or ureas by oxidative carbonylation of amino compounds in the presence of carbon monoxide and oxygen as oxidizing agents and, particularly in the case of the urethanes, in the presence of ...

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11-06-2015 дата публикации

METHOD OF MAKING 1-(ACYLOXY)-ALKYL CARBAMATE COMPOUNDS

Номер: US20150158809A9
Принадлежит: XenoPort, Inc.

Methods of preparing carbamate prodrugs of amine-containing drugs are provided. Carbonates useful in the synthesis of the carbamate prodrugs are also provided. 2. The method of claim 1 , wherein X is halo.3. The method of claim 1 , wherein X is Cl.4. The method of claim 1 , wherein reaction step (A) occurs in a solvent.5. The method of claim 4 , wherein the solvent is selected from the group consisting of heptane claim 4 , xylene claim 4 , toluene claim 4 , N-methylpyrrolidine claim 4 , N claim 4 ,N-diisopropylamine claim 4 , dimethyl formamide claim 4 , dimethyl sulfoxide claim 4 , diphenyl ether claim 4 , and combinations thereof.6. The method of claim 1 , wherein reaction step (A) occurs at a temperature from about 50° C. to about 120° C.7. The method of claim 1 , wherein reaction step (A) occurs in the presence of a metal oxide.8. The method of claim 1 , wherein the reaction step (A) occurs in the presence of a metal alkanoate or a metal salt of RCOH.9. The method of claim 1 , wherein reaction step (A) occurs in the presence of RC(O)—O—C(O)R.10. The method of claim 1 , wherein reaction step (A) occurs in the presence of a tetraalkylammonium salt.11. The method of claim 1 , wherein reaction step (A) occurs in the presence of an organic base.12. The method of claim 1 , wherein reaction step (B) occurs in a solvent selected from the group consisting of heptane claim 1 , xylene claim 1 , toluene claim 1 , dialkyl ether claim 1 , cyclic ethers claim 1 , dimethyl formamide claim 1 , dimethyl sulfoxide claim 1 , water claim 1 , acetonitrile claim 1 , ethyl acetate claim 1 , and combinations thereof.13. The method of claim 1 , wherein reaction step (B) occurs at a temperature from about 0° C. to about 50° C.14. The method of claim 1 , wherein reaction step (B) occurs in the presence of a base.15. The method of claim 1 , wherein Ris i-Pr; Ris Me or i-Pr; and Ris H.16. The method of claim 1 , wherein one or more of R claim 1 , R claim 1 , R claim 1 , R claim 1 , and Ris ...

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28-08-2014 дата публикации

METHOD OF MAKING 1-(ACYLOXY)-ALKYL CARBAMATE COMPOUNDS

Номер: US20140243544A1
Принадлежит: XenoPort, Inc.

Methods of preparing carbamate prodrugs of amine-containing drugs are provided. Carbonates useful in the synthesis of the carbamate prodrugs are also provided. 2. The method of claim 1 , wherein X is halo.3. The method of claim 1 , wherein X is Cl.4. The method of claim 1 , wherein reaction step (A) occurs in a solvent.5. The method of claim 4 , wherein the solvent is selected from the group consisting of heptane claim 4 , xylene claim 4 , toluene claim 4 , N-methylpyrrolidine claim 4 , N claim 4 ,N-diisopropylamine claim 4 , dimethyl formamide claim 4 , dimethyl sulfoxide claim 4 , diphenyl ether claim 4 , and combinations thereof.6. The method of claim 1 , wherein reaction step (A) occurs at a temperature from about 50° C. to about 120° C.7. The method of claim 1 , wherein reaction step (A) occurs in the presence of a metal oxide.8. The method of claim 1 , wherein the reaction step (A) occurs in the presence of a metal alkanoate or a metal salt of RCOH.9. The method of claim 1 , wherein reaction step (A) occurs in the presence of RC(O)—O—C(O)R.10. The method of claim 1 , wherein reaction step (A) occurs in the presence of a tetraalkylammonium salt.11. The method of claim 1 , wherein reaction step (A) occurs in the presence of an organic base.12. The method of claim 1 , wherein reaction step (B) occurs in a solvent selected from the group consisting of heptane claim 1 , xylene claim 1 , toluene claim 1 , dialkyl ether claim 1 , cyclic ethers claim 1 , dimethyl formamide claim 1 , dimethyl sulfoxide claim 1 , water claim 1 , acetonitrile claim 1 , ethyl acetate claim 1 , and combinations thereof.13. The method of claim 1 , wherein reaction step (B) occurs at a temperature from about 0° C. to about 50° C.14. The method of claim 1 , wherein reaction step (B) occurs in the presence of a base.15. The method of claim 1 , wherein Ris i-Pr; Ris Me or i-Pr; and Ris H.16. The method of claim 1 , wherein one or more of R claim 1 , R claim 1 , R claim 1 , R claim 1 , and Ris ...

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16-06-2016 дата публикации

INTEGRATED PROCESS FOR CARBON CAPTURE AND ENERGY PRODUCTION

Номер: US20160167974A1
Автор: Novek Ethan
Принадлежит:

The present invention pertains to new methods for generating energy and useful nitrogen compounds from captured carbon dioxide. It involves employing an osmotic engine, draw solution, and feed solution. An osmotic gradient between the solutions assists in generating energy and a solution of ammonium carbonate, ammonium bicarbonate or mixture thereof. This solution may be decomposed to form ammonia, carbon dioxide, a precipitate, or a mixture thereof. 2. The integrated process of which further comprises:employing an osmotic engine comprising: (1) the formed solution of ammonium carbonate, ammonium bicarbonate, ammonium carbamate or mixture thereof as a draw solution and (2) a feed solution having a lower osmotic pressure than said draw solution to generate a gradient; andusing the gradient to generate energy and a second solution of ammonium carbonate, ammonium bicarbonate, ammonium carbamate or mixture thereof wherein said second solution has a lower osmotic pressure than the draw solution and wherein at least a portion of said second solution is subjected to decomposing.3. The integrated process of wherein the engine is selected from the group consisting of pressure retarded osmosis system claim 2 , reverse electrodialysis claim 2 , and capacitive mixing power production.4. The integrated process of wherein the osmotic engine is a pressure retarded osmosis system wherein the transfer of water from the feed solution across one or more membranes is employed to generate electricity via a hydroelectric generator.5. The integrated process of wherein the draw solution is formed by capturing carbon dioxide with ammonia.6. The integrated process of wherein the captured carbon dioxide used to form the solution comprises carbon dioxide captured from combustion or oxidation of one or more hydrocarbons claim 1 , from steam reforming claim 1 , from gas shift reaction claim 1 , from catalytic reforming claim 1 , from natural gas purification claim 1 , from land fill gas claim 1 ...

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30-05-2019 дата публикации

METHOD FOR PRODUCING INDOLE COMPOUND

Номер: US20190161475A1
Принадлежит: JAPAN TOBACCO INC.

The present invention aims to provide a new method for producing an indole compound or a salt thereof, which has an ITK inhibitory action, and is useful for the prophylaxis or treatment of inflammatory disease. The present invention relates to a new method for producing an indole compound or a salt thereof, which is useful as an inducible T cell kinase (ITK) inhibitor, and an intermediate thereof.Patent Document 1 discloses a compound useful as an ITK inhibitor, and a method for producing the same.The present invention aims to provide a new method for producing an indole compound or a salt thereof, which is useful for the prophylaxis or treatment of inflammatory disease, and the like.Embodiments of the present invention are shown in the following (1) to (16).which comprises a step of removing the protecting group from N-[2-(6,6-dimethyl-1-(tetrahydropyran-2-yl)-4,5,6,7-tetrahydro-1H-indazol-3-yl)-1H-indol-6-yl]-N-methyl-(2S)-2-(morpholin-4-yl)propanamide (formula [III]to give a compound of the formula [I].which comprises a step of reacting N-[2-(6,6-dimethyl-4,5,6,7-tetrahydro-1H-indazol-3-yl)-1H-indol-6-yl]-N-methyl-(2S)-2-(morpholin-4-yl)propanamide (formula [I]with hydrogen chloride to give a compound of the formula [II].which comprises a step of removing the protecting group from N-[2-(6,6-dimethyl-1-(tetrahydropyran-2-yl)-4,5,6,7-tetrahydro-1H-indazol-3-yl)-1H-indol-6-yl]-N-methyl-(2S)-2-(morpholin-4-yl)propanamide (formula [III]to give N-[2-(6,6-dimethyl-4,5,6,7-tetrahydro-1H-indazol-3-yl)-1H-indol-6-yl]-N-methyl-(2S)-2-(morpholin-4-yl)propanamide (formula [I]andwith (2S)-2-(morpholin-4-yl)propanoic acid (formula [IV]or reactive derivative thereof or a salt thereof to give N-[2-(6,6-dimethyl-1-(tetrahydropyran-2-yl)-4,5,6,7-tetrahydro-1H-indazol-3-yl)-1H-indol-6-yl]-N-methyl-(2S)-2-(morpholin-4-yl)propanamide (formula [III]wherein Rand Rare each independently hydrogen, Calkyl or Calkoxy,wherein Ris as defined above,wherein Ris as defined above,wherein Rand ...

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11-09-2014 дата публикации

(HETERO)ARYL CYCLOPROPYLAMINE COMPOUNDS AS LSD1 INHIBITORS

Номер: US20140256729A1
Принадлежит:

The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and theft use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection.

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28-05-2020 дата публикации

Method for producing 3-arylpropionamide compound and 3-arylpropionic acid ester compound

Номер: US20200165209A1
Принадлежит: Sumitomo Chemical Co Ltd

(wherein X represents a chlorine atom or a bromine atom; and Y represents an alkyl group optionally substituted with fluorine atom(s), a hydrogen atom, a fluorine atom, a cyano group, an alkylcarbonyl group, a dialkylamino group, or the like) with acrylamide or an acrylic acid ester in the presence of a metal catalyst and a reducing agent.

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30-06-2016 дата публикации

A Process to Produce Polycarbamate, Polycarbamate Produced Thereby and a Coating Composition Comprising the Polycarbamate

Номер: US20160185713A1
Принадлежит: Dow Global Technologies LLC

A process to prepare polycarbamate comprising adding urea to a polyol in the presence of at least one catalyst selected from the group consisting of compounds having the following formula MZ; wherein M is a trivalent metal, and Z is an anionic functionality or a functionality capable of forming a covalent bond with M and wherein n times a valence number of Z equals X and m times three equals Y wherein the absolute value of X equals the absolute value of Y is provided. Also provided are a polycarbamate produced according to the process and a coating composition comprising the polycarbamate. 1. A process to prepare polycarbamate comprising:{'sub': m', 'n, 'adding urea to a polyol in the presence of at least one catalyst selected from the group consisting of compounds having the following formula MZ; wherein M is a trivalent metal selected from the group consisting of Bi(III), Al(III), Yb(III), Y(III), Fe(III), La(IIII), Sm(IIII), Ru(III), Ga(III), Sc(III) or Ce(III), and wherein Z is selected from the group consisting of 2-ethylhexanoate, benzoate, hexafluoroacetylacetonate, isopropoxide, acetyl acetonate, hydroxyl, phenoxide, stearate, tert-butoxide, neodecanoate, citrate, trifluoromethane sulfonate, n-butoxide, trifluoroacetate, 1,1,1-trifluoro-2,4-pentanedionate, 2,2,6,6,-tetramethyl-3,5-hexanedionate, cresylate, ethoxide, methoxide, triethanolaminato, 2-methyl-2-butoxide, oxo, fluoride, chloride, bromide, iodide, aryl or substituted aryl, mixtures thereof and chelates thereof, and wherein Z is an anionic functionality or a functionality capable of forming a covalent bond with M.'}2. The process according to claim 1 , wherein a second catalyst selected from the group consisting of carbamylation catalysts is present.3. The process according to claim 2 , wherein the second catalyst is dibutyltin oxide and/or dibutyltin acetate.4. (canceled)5. (canceled)4. The process according to claim 1 , wherein the catalyst is selected from the group consisting of: Bismuth(III) ...

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29-06-2017 дата публикации

METHOD USING ZIRCONIUM CATALYST FOR PRODUCING CARBAMATE-FUNCTIONAL MATERIALS

Номер: US20170183436A1
Автор: JADHAV Abhijit
Принадлежит: BASF COATINGS GMBH

A carbamate-functional material is prepared by reacting a carbamate compound with a hydroxy-functional material using zirconium acetylacetonates catalyst. 1: A method of preparing a carbamate-functional material , the method comprising:reacting a carbamate compound with a hydroxy-functional material in the presence of a zirconium acetylacetonate catalyst to form a carbamate-functional material.2: The method according to claim 1 , wherein the carbamate compound is an alkyl carbamate.3: The method according to claim 2 , wherein the carbamate compound is at least one selected from the group consisting of methyl carbamate claim 2 , ethyl carbamate claim 2 , n-propyl carbamate claim 2 , isopropyl carbamate claim 2 , n-butyl carbamate claim 2 , isobutyl carbamate claim 2 , tert-butyl carbamate claim 2 , n-hexyl carbamate claim 2 , 2-ethylhexyl carbamate claim 2 , cyclohexyl carbamate claim 2 , and phenyl carbamate claim 2 , and combinations thereof.4: The method according to claim 1 , wherein the hydroxy-functional material is a monomeric compound comprising having from 1 to 160 carbon atoms.5: The method according to claim 1 , wherein the hydroxy-functional material comprises from 12 to 72 carbon atoms and at least two hydroxyl groups.6: The method according to claim 1 , wherein the hydroxy-functional material is obtained by a reduction of an addition product of unsaturated fatty acids.7: The method according to claim 1 , wherein the hydroxy-functional material is a hyperbranched polyol.8: The method according to claim 7 , wherein the reacting is performed during a final step of obtaining the hyperbranched polyol.9: The method according to claim 1 , wherein the hydroxy-functional material is at least one selected from the group consisting of polyester polyols claim 1 , polyether polyols claim 1 , polyhydroxy polycarbonates claim 1 , polyurethane polyols claim 1 , polyvinyl polymer polyols claim 1 , polyhydroxy polyesteramides claim 1 , polysiloxane polyols claim 1 , and ...

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09-08-2018 дата публикации

Synthesis of Methyl Carbamate and Dimethyl Carbonate (DMC) in Presence of Stripping with Inert Gas or Superheated Vapours and a Reactor for the Same

Номер: US20180222852A1
Принадлежит:

The invention relates to synthesis of methyl carbamate (MC) and dimethyl carbonate (DMC) in presence of stripping inert gas or superheated methanol vapors using packed column reactor and bubble column reactor. 1. A horizontal sectionalized bubble column reactor for synthesis of methyl carbamate and dimethyl carbonate (DMC) comprising:a. a cylindrical bubble column reactor with single or multiple compartments to receive liquid reactant feed comprising of urea and methanol or methyl carbamate and methanol through inlet ports for a reaction to occur;b. a gas distributor chamber located within the cylindrical bubble column reactor comprising a plate intersecting a cylinder of the cylindrical bubble column reactor with or without an angle to an axis of the cylinder;c. single or multiple inlet ports fitted to the gas distributor chamber for distributing gas;d. single or multiple inlet ports fitted with a constant pressure regulator, single or multiple gas/vapor outlet ports fitted with a back pressure regulator for gaseous phase, wherein, a pressure difference of 10 psi is maintained to ensure positive flow of inert gas into the cylindrical bubble column reactor;e. single or multiple liquid outlet ports with an in-line filter fitted to the cylindrical bubble column reactor for liquid phase withdrawal;f. a heat transfer device fitted to the cylindrical bubble column reactor for maintaining temperature of the reaction;g. a condenser and a gas-liquid separator fitted to the outlet port(s) wherein a product in vapor form is condensed and separated from liquid components;h. an outlet for condensate and an outlet for non-condensate connected to the gas-liquid separator.2. The horizontal sectionalized bubble column reactor as claimed in claim 1 , wherein the cylindrical bubble column reactor further comprises an expanded slurry bed of solid catalyst particles suspended in a suspension liquid or in a packed bed of solid catalyst.3. The horizontal sectionalized bubble column ...

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27-08-2015 дата публикации

PROCESS FOR THE PREPARATION OF (1S,4S,5S)-4-BROMO-6-OXABICYCLO[3.2.1]OCTAN-7-ONE

Номер: US20150239909A1
Принадлежит: Daiichi Sankyo Company, Limited

The present invention relates to an improved and industrially advantageous process for the preparation of (1S, 4S, 5S)-4-bromo-6-oxabicyclo[3.2.1]octan-7-one represented by the following formula (1) 2. The production process according to claim 1 , wherein the brominating agent is N-bromosuccinimide. The present invention relates to an improved and industrially advantageous process for the preparation of (1S,4S,5S)-4-bromo-6-oxabicyclo[3.2.1]octan-7-one of formula (I):which is a key intermediate in the synthesis of edoxaban, a compound that exhibits an inhibitory effect on activated blood coagulation factor X (also referred to as activated factor X or FXa), and is useful as a preventive and/or therapeutic drug for thrombotic diseases.Chemically, edoxaban is N-(5-chloropyridin-2-yl)-N-((1S,2R,4S)-4-[(dimethylamino)carbonyl]-2-{[(5-methyl-4,5, 6,7-tetrahydrothiazolo[5,4-c]pyridin-2-yl)carbonyl]amino}cyclohexyl) ethanediamide, represented by the following formula (A):The p-toluenesulfonic acid monohydrate salt of compound A is represented by the following formula (B):Edoxaban is known as a compound that exhibits an inhibitory effect on activated blood coagulation factor X (also referred to as activated factor X or FXa), and is useful as a preventive and/or therapeutic drug for thrombotic diseases.Several processes are known in the literature for preparing edoxaban for example, U.S. Pat. No. 7,365,205; U.S. Publication No. 20090105491.U.S. Pat. No. 7,365,205 provides a process for the preparation of edoxaban, wherein the process involves the use of (1S,4S,5S)-4-iodo-6-oxabicyclo[3.2.1]octan-7-one, represented by the following formula (C):as an intermediate.The present inventors have identified that (1S,4S,5S)-4-bromo-6-oxabicyclo[3.2.1]octan-7-one, represented by the following formula (I):could also be used as an intermediate for the preparation of FXa inhibitory compounds like edoxaban. The present inventors have found that replacement of (1S,4S,5S)-4-iodo-6-oxabicyclo[ ...

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23-08-2018 дата публикации

3-PHENYLISOSERINE DERIVATIVE PRODUCTION METHOD

Номер: US20180237384A1
Принадлежит:

A method produces a 3-phenylisoserine derivative by protecting an amino group of a compound represented by General Formula (1) (wherein Rrepresents a phenyl group, or a phenyl group having a substituent; Rrepresents an alkali metal, alkaline earth metal, or nitrogen base; and Rrepresents a hydrogen atom, methyl group, benzyl group, p-methoxybenzyl group, tert-butyl group, methoxymethyl group, 2-tetrahydropyranyl group, ethoxyethyl group, acetyl group, pivaloyl group, benzoyl group, trimethylsilyl group, triethylsilyl group, or tert-butyldimethylsilyl group) in water or a mixed solvent containing water to obtain a particular compound; extracting with a Cether-based solvent; replacing at least part of the Cether-based solvent with a C-Caliphatic alcohol while removing the Cether-based solvent and water to perform esterification reaction; and isolating at 0 to 30° C. to obtain a 3-phenylisoserine derivative represented by General Formula (2). 14.-. (canceled)6. The method according to claim 5 , wherein the Cether-based solvent is tetrahydrofuran or 1 claim 5 ,2-dimethoxyethane.7. The method according to claim 5 , wherein the C-Caliphatic alcohol is methanol or ethanol.8. The method according to claim 5 , wherein Ris a benzoyl group or tert-butoxycarbonyl group.9. The method according to claim 6 , wherein the C-Caliphatic alcohol is methanol or ethanol.10. The method according to claim 6 , wherein Ris a benzoyl group or tert-butoxycarbonyl group.11. The method according to claim 7 , wherein Ris a benzoyl group or tert-butoxycarbonyl group. This disclosure relates to a method of producing a 3-phenylisoserine derivative, which is important as, for example, an intermediate material for pharmaceuticals.Compounds having a β-amino acid site such as 3-phenylisoserine derivatives are known to be compounds that are industrially useful for pharmaceuticals and the like. Known examples of methods of producing a 3-phenylisoserine derivative include the following:(1) a method in ...

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24-09-2015 дата публикации

FLEXIBLE TO RIGID NANOPOROUS POLYURETHANE-ACRYLATE (PUAC) TYPE MATERIALS FOR STRUCTURAL AND THERMAL INSULATION APPLICATIONS

Номер: US20150266983A1

Novel urethane-acrylate (UAC) Star monomers and polyurethane-acrylate (PUAC) aerogel polymers derived therefrom are described herein, along with other novel, related monomers and polymers. Also described herein are processes for preparing the UAC Star monomers, the PUAC aerogel polymers, and the other related monomers and polymers. The PUAC and related polymers herein are useful in various applications including in structural and thermal insulation. 2. The urethane-acrylate star monomer of wherein the nitrogen atoms of the urethane moieties are attached to their respective aryl rings at the 4-positions of the aryl rings.3. The urethane-acrylate star monomer of wherein W═X═Y═CHCH.4. The urethane-acrylate star monomer of wherein each of R1-R9 is a hydrogen.5. The urethane-acrylate star monomer of wherein the nitrogen atoms of the urethane moieties are attached to their respective aryl rings at the 4-positions of the aryl rings; wherein W═X═Y═CHCH; and wherein each of R1-R9 is a hydrogen.6. A polyurethane-acrylate polymer formed by the polymerization of the urethane-acrylate star monomer of in the presence of a polymerization catalyst.7. The polyurethane-acrylate polymer of claim 6 , wherein the polymerization catalyst is a free radical initiator.8. The polyurethane-acrylate polymer of claim 7 , wherein the free radical initiator is 2 claim 7 ,2′-azobisisobutyronitrile.9. A polyurethane-acrylate polymer formed by the copolymerization of the urethane-acrylate star monomer of with a polymerization chain extender claim 1 , in the presence of a polymerization catalyst.10. The polyurethane-acrylate polymer of claim 9 , wherein the polymerization chain extender is a compound comprising from 2 to 4 acrylate groups or from 2 to 4 methacrylate groups claim 9 , or a combination thereof.11. The polyurethane-acrylate polymer of claim 10 , wherein the chain extender is a compound comprising 2 acrylate groups.15. The polyurethane-acrylate polymer of wherein the nitrogen atoms of the ...

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15-09-2016 дата публикации

NALPHA, NALPHA, NALPHA-TRIALKYL HISTIDINE DERIVATIVES USEFUL FOR THE PREPARATION OF ERGOTHIONEINE COMPOUNDS

Номер: US20160264530A1
Принадлежит:

Provided herein are N,N,N-trialkyl histidine derivative compounds and methods of their preparation. Also provided are methods of their use for preparing useful compounds such as ergothioneine. 235-. (canceled)38. The method of claim 1 , wherein each (C)alkyl is unsubstituted.39. The method of claim 1 , wherein each Ris methyl.40. The method of claim 1 , wherein step (a) is conducted in one or more solvent(s) selected from the group consisting of water claim 1 , ethyl acetate claim 1 , tetrahydrofuran (THF) claim 1 , 2-methyltetrahydrofuran claim 1 , dioxane claim 1 , methyl ethyl ketone claim 1 , acetone claim 1 , dimethylformamide claim 1 , dimethylsulfoxide claim 1 , diglyme claim 1 , (bis)-methoxymethyl ether claim 1 , (bis)-2-ethoxyethyl ether claim 1 , and diethyl ether.41. The method of claim 1 , wherein step (a) is conducted with a base selected from the group consisting of sodium bicarbonate claim 1 , sodium carbonate claim 1 , potassium acetate claim 1 , sodium hydroxide claim 1 , sodium acetate claim 1 , and potassium hydrogen carbonate.42. The method of claim 1 , wherein step (a) is conducted at a temperature ranging from about 0° C. to about 30° C.43. The method of claim 1 , wherein step (a) is conducted for about 1 to 48 hours.44. The method of claim 1 , wherein compound 3 is isolated after step (a).46. The method of claim 36 , wherein step (b) is conducted in a solvent selected from the group consisting of water claim 36 , 1% (w/v) HCl claim 36 , methanol claim 36 , ethanol claim 36 , and 10% to 38% (w/v) HCl.47. The method of claim 46 , wherein step (b) is conducted in the presence of a catalyst claim 46 , and the catalyst is selected from the group consisting of Pd/C claim 46 , Pd/C sulfided claim 46 , Pd/CaSO claim 46 , Pd/CaCO claim 46 , Pd/CaCO/Pb and Raney Nickel.48. The method of claim 47 , wherein step (b) is conducted in the presence of a reagent selected from the group consisting of hydrogen gas claim 47 , formic acid claim 47 , and ammonium ...

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21-09-2017 дата публикации

Integrated process for capturing carbon dioxide

Номер: US20170267538A1
Автор: Ethan NOVEK
Принадлежит: Individual

The invention pertains to an integrated process for capturing CO 2 . The process involves desorbing gaseous CO 2 from a CO 2 containing aqueous solution comprising carbonate, bicarbonate, sesquicarbonate, carbamate, or a mixture thereof. The desorbing of gaseous CO 2 is conducted in the presence of a suitable water soluble substance. If desired, the process may also at least partially recover the soluble substance using a membrane, distillation, or another technique.

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21-09-2017 дата публикации

INTEGRATED PROCESS FOR CARBON CAPTURE AND ENERGY PRODUCTION

Номер: US20170267539A1
Автор: Novek Ethan
Принадлежит:

The present invention pertains to new methods for generating energy and useful nitrogen compounds from captured carbon dioxide. It involves employing an osmotic engine, draw solution, and feed solution. An osmotic gradient between the solutions assists in generating energy and a solution of ammonium carbonate, ammonium bicarbonate or mixture thereof. This solution may be decomposed to form ammonia, carbon dioxide, a precipitate, or a mixture thereof.

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20-09-2018 дата публикации

Process to produce polycarbamate, polycarbamate produced thereby and a coating composition comprising the polycarbamate

Номер: US20180265458A1
Принадлежит: Dow Global Technologies LLC

A process to prepare polycarbamate comprising adding urea to a polyol in the presence of at least one catalyst selected from the group consisting of compounds having the following formula MmZn; wherein M is a trivalent metal, and Z is an anionic functionality or a functionality capable of forming a covalent bond with M and wherein n times a valence number of Z equals X and m times three equals Y wherein the absolute value of X equals the absolute value of Y is provided. Also provided are a polycarbamate produced according to the process and a coating composition comprising the polycarbamate.

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12-10-2017 дата публикации

SUBSTITUTED 5-HYDROXY-2-PHENYL-3-HETEROARYL PENTANENITRILE DERIVATES, METHOD FOR THE PRODUCTION THEREOF AND USE THEREOF AS HERBICIDES AND/OR PLANT GROWH REGULATORS

Номер: US20170290330A1
Принадлежит:

Primarily, the present invention relates to compounds of the formula (I) defined below and to their use as herbicides, in particular for controlling broad-leaved weeds and/or weed grasses in crops of useful plants and/or as plant growth regulators for influencing the growth of crops of useful plants. The present invention also relates to herbicidal or plant growth-regulating compositions comprising one or more compounds of the formula (I). Moreover, the present invention relates to processes for preparing the compounds of the formula (I). 2. The compound of the formula (I) and/or salt thereof according to claim 1 , whereinQ represents a mono- or bicyclic heteroaromatic radical having in total 2 to 9 carbon ring atoms, where the heteroaromatic radical Q contains 1, 2, 3 or 4 heteroatoms in the heteroaromatic ring and the heteroatom or the heteroatoms are selected from the group consisting of N, O, and S.3. The compound of the formula (I) and/or salt thereof as claimed in claim 1 , whereinQ represents a mono- or bicyclic heteroaromatic radical selected from the group consisting of pyrimidinyl, pyridinyl, pyridazinyl, pyrazinyl, thienyl, furyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, triazinyl, quinolyl, isoquinolyl, cinnolinyl-, quinazolinyl, quinoxalinyl, pteridinyl, indolyl and phthalazinyl.5. The compound of the formula (I) and/or salt thereof as claimed in claim 1 , wherein{'sup': '1', 'Rrepresents hydrogen or a hydrolyzable radical having in total up to 30 carbon atoms, with preference a hydrolyzable radical having in total 1 to 24 carbon atoms, preferably optionally having in total 1 to 20 carbon atoms.'}6. The compound of the formula (I) and/or salt thereof as claimed in claim 1 , wherein{'sup': 1', '1, 'claim-text': represents an optionally substituted hydrocarbon radical or an optionally substituted heterocyclyl radical, or', {'sup': a', 'b', 'c', 'a', 'b, 'represents a radical of the formula SiRRR, or —NRR,'}], 'Rrepresents hydrogen or a hydrolyzable ...

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13-10-2016 дата публикации

REAGENTS AND METHODS FOR ESTERIFICATION

Номер: US20160297752A1
Принадлежит:

Methods and reagents for esterification of biological molecules including proteins, polypeptides and peptides. Diazo compounds of formula I: 2. The compound of claim 1 , wherein Ris an alkyl claim 1 , alkenyl claim 1 , alkynyl or aryl group.3. The compound of claim 1 , wherein Ris a label claim 1 , a cell penetrating group claim 1 , a cell targeting group claim 1 , or a reactive group or latent reactive4. The compound of claim 1 , wherein the cell targeting group is an antibody or functional fragment thereof.5. The compound of claim 1 ,wherein:{'sub': A', 'P', 'P', 'M1, 'Rrepresents hydrogens at each phenyl ring position, or represents 1 to 3 non-hydrogen substituents on the phenyl ring, wherein the non-hydrogen substituents are selected from the group consisting of alkyl, cycloalkyl, alkoxy, cycloalkoxy, aryl, arylalkyl, halogen, haloalkyl, haloalkoxy, heterocyclyl and R-CO—NH—, where the alkyl, cycloalkyl, alkoxy, cycloalkoxy, aryl, arylalkyl and heterocyclyl groups are optionally substituted with 1-3 non-hydrogen substituents selected from alkyl, alkoxy, halogen, haloalkyl or haloalkoxy groups and Ris hydrogen, an alkyl group or R; and'}{'sub': M', 'M1, 'Ror Rare independently an optionally substituted organic group M or Ml, respectively, having from 1 to 100 carbon atoms and optionally nitrogen, oxygen or sulfur atoms, or -L-M, or -L1-M1, respectively, where -L- and -L1- are independently a divalent linker moiety having from 1-30 carbon atoms and optionally nitrogen, oxygen or sulfur atoms; or'}{'sub': M', 'M1, 'Ror Ris or comprises a polymer, where the polymer is directly bonded into the compound or is bonded via a linker.'}6. The compound of claim 1 , wherein Ror Ris or comprises a cargo molecule.7. The compound of claim 1 , wherein Ror Ris or comprises a hydrophilic polymer.8. The compound of claim 1 , wherein Rrepresents ring substitution having at least one non-hydrogen group at the para ring or meta ring position.9. The compound of claim 1 , wherein Ris a ...

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18-10-2018 дата публикации

PROCESS FOR PREPARATION OF N-BOC BIPHENYL ALANINOL

Номер: US20180297941A1
Принадлежит:

A process is provided for preparation of (R)—N-Boc biphenyl alaninol. It provides a preparation process for a compound outlined as compound 4, which includes these operations: in one of the alcohol solvents, asymmetric hydrogenation of 5 in the presence of [Rh(Duanphos)(X)]Y and hydrogen to provide compound 4. Here “Duanphos” is (Rc,Sp)-Duanphos or (Sc,Rp)-Duanphos; X is NBD or/and COD; Y is one or more of BF4, PF6, SbF6. This process has a lot of advantages, such as low cost, safe operation, less pollution and high yield. The product was obtained in >99% purity and ee which is suitable to scale up in industrial scale. 2. The process defined as claim 1 , wherein the pressure of hydrogen is in the range of 0.1-0.5 MPa;and/or in the process for preparing compound 4, the alcohol solvent is methanol;and/or in the process for preparing compound 4, the ratio of the volume of the alcohol solvent to the mole of compound 5 is in the range of 1-10 L/mol;and/or in the process for preparing compound 4, the mole ratio of [Rh(Duanphos)(X)]Y to compound 5 is in the range of 0.00001-0.01;and/or in the process for preparing compound 4, the hydrogenation temperature is in the range of 0-60° C.;and/or in the process for preparing compound 4, the reaction time for hydrogenation is 1-20 h.3. The process defined as claim 2 , wherein the pressure of hydrogen is in the range of 0.5-3.0 MPa;and/or in the process for preparing compound 4, the ratio of the volume of the alcohol solvent to the mole of compound 4 is in the range of 1.5-3 L/mol;and/or in the process for preparing compound 4, the mole ratio of [Rh(Duanphos)(X)]Y to compound 5 is in the range of 0.0001-0.0003;and/or in the process for preparing compound 4, the hydrogenation temperature is in the range of 20−30° C.;and/or in the process for preparing compound 4, the reaction time for hydrogenation is 4-8 h.4. The process defined as claim 3 , wherein the pressure of hydrogen is in the range of 1.5-2.0 MPa;and/or in the process for ...

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05-11-2015 дата публикации

Synthesis of methyl carbamate and dimethyl carbonate (dmc) in presence of stripping with inert gas or superheated vapours and a reactor for the same

Номер: US20150315134A1

The invention relates to synthesis of methyl carbamate (MC) and dimethyl carabonate (DMC) in presence of stripping inert gas or superheated methanol vapors using packed column reactor and bubble column reactor.

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12-11-2015 дата публикации

METHOD USING ZIRCONIUM CATALYST FOR PRODUCING CARBAMATE-FUNCTIONAL MATERIALS

Номер: US20150321998A1
Автор: Jadhav Abhijit V.
Принадлежит: BASF COATINGS GMBH

A carbamate-functional material is prepared by reacting a carbamate compound with a hydroxy-functional material using zirconium acetylacetonate as catalyst. 1. A method of preparing a carbamate-functional material , comprising reacting a carbamate compound with a hydroxy-functional material using zirconium acetylacetonate as catalyst.2. A method according to claim 1 , wherein the carbamate compound is an alkyl carbamate.3. A method according to claim 2 , wherein the carbamate compound is selected from the group consisting of methyl carbamate claim 2 , ethyl carbamate claim 2 , n-propyl carbamate claim 2 , isopropyl carbamate claim 2 , n-butyl carbamate claim 2 , isobutyl carbamate claim 2 , tert-butyl carbamate claim 2 , n-hexyl carbamate claim 2 , 2-ethylhexyl carbamate claim 2 , cyclohexyl carbamate claim 2 , phenyl carbamate claim 2 , and combinations thereof.4. A method according to claim 1 , wherein the hydroxy-functional material is a monomeric compound having from 1 to 160 carbon atoms.5. A method according to claim 1 , wherein the hydroxy-functional material has from 12 to 72 carbon atoms and at least two hydroxyl groups.6. A method according to claim 1 , wherein the hydroxy-functional material comprises a reduction of an addition product of unsaturated fatty acids.7. A method according to claim 1 , wherein the hydroxy-functional material is a hyperbranched polyol.8. A method according to claim 7 , wherein reaction is carried out during a final step of making the hyperbranched polyol.9. A method according to claim 1 , wherein the hydroxy-functional material is a member selected from the group consisting of polyester polyols claim 1 , polyether polyols claim 1 , polyhydroxy polycarbonates claim 1 , polyurethane polyols claim 1 , polyvinyl polymer polyols claim 1 , polyhydroxy polyesteramides claim 1 , polysiloxane polyols claim 1 , and polyhydroxy polythioethers.10. A method according to claim 9 , wherein the hydroxy-functional material is an acrylic polymer ...

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12-11-2015 дата публикации

Method using titanium catalyst for producing carbamate-functional materials

Номер: US20150321999A1
Автор: Abhijit V. Jadhav
Принадлежит: BASF COATINGS GMBH

A carbamate-functional material is prepared by reacting a carbamate compound with a hydroxy-functional material using titanium (IV) alkoxide as catalyst.

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10-12-2015 дата публикации

Process for preparing the anti-tumor agent 6-(7-((1-aminocyclopropyl)methoxy)-6-methoxyquinolin-4-yloxy)-N-methyl-1-naphthamide and its crystalline

Номер: US20150353496A1
Автор: Chen Guoqing Paul
Принадлежит:

The present invention relates a new process to synthesize 6-(7-((1-aminocyclo-propyl)-methoxy)-6-methoxyquinolin-4-yloxy)-N-methyl-1-naphthamide (AL3810) by deprotection of substituted benzyl 1-((6-methoxy-4-(5-(methylcarbamoyl)naphthalen-2-yloxy)quinolin-7-yloxy)-methyl)cyc-lopropylcarbamate (Formula I) under a diluted or weak acidic condition. A stable crystalline form of 6-(7-((1-aminocyclo-propyl)-methoxy)-6-methoxyquinolin-4-yloxy)-N-methyl-1-naphthamide has also been prepared. 8. A method of preparing a compound having Formula II of comprising to react formula 17 with 4-methoxybenzylalcohol in a refluxing toluene condition.15. A crystalline form of 6-(7-((1-aminocyclopropyl)methoxy)-6-methoxyquinolin-4-yloxy)-N-methyl-1-naphthamide exhibiting at least one ofa melting point at 185° C.-205° C.;a no observable endotherm DSC from about 40° C. to about 185° C.;an observable endotherm DSC from about 185° C. to about 210° C.;a TGA themogram that doesn't exhibit significant weight loss until at 210° C. to 250° C.;a XRPD graph having 20-40 characteristic peaks.18. A crystalline form of 6-(7-((1-aminocyclopropyl)methoxy)-6-methoxyquinolin-4-yloxy)-N-methyl-1-naphthamide according is recrystallized from isopropanol. This application claims the benefit of U.S. Provisional Applications 61/754,516 filed on Jan. 18, 2013The present invention relates a new process to synthesize 6-(7-((1-aminocyclo-propyl)-methoxy)-6-methoxyquinolin-4-yloxy)-N-methyl-1-naphthamide (AL3810) by deprotection of substituted benzyl 1-((6-methoxy-4-(5-(methylcarbamoyl)naphthalen-2-yloxy)quinolin-7-yloxy)-methyl)cyclopropylcarbamate (Formula I) under a diluted or weak acidic condition. A stable crystalline form of 6-(7-((1-aminocyclo-propyl)-methoxy)-6-methoxyquinolin-4-yloxy)-N-methyl-1-naphthamide has also been prepared.6-(7-((1-Aminocyclopropyl)-methoxy)-6-methoxyquinolin-4-yloxy)-N-methyl-1-naphthamide (AL3810), or a pharmaceutically acceptable salt (such as hydrochloride salt) thereof, has been ...

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22-12-2016 дата публикации

(HETERO)ARYL CYCLOPROPYLAMINE COMPOUNDS AS LSD1 INHIBITORS

Номер: US20160368857A1
Принадлежит:

The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection. 6. The compound of any of to for use as a medicament.9. A pharmaceutical composition comprising the compound of any of to and a pharmaceutically acceptable carrier.16. The compound of any of to or the compound for use as a medicament according to any of to or the pharmaceutical composition of any of to , wherein D is a cycloalkyl group having from 4 to 7 C atoms , wherein said cycloalkyl group has one or two substituents Rand is further optionally substituted with one or more R.17. The compound of any of to or the compound for use as a medicament according to any of to or the pharmaceutical composition of any of to , wherein D is a cycloalkyl group having from 4 to 7 C atoms , wherein said cycloalkyl group has one substituent Rand is further optionally substituted with one or more R.18. The compound of any of to or the compound for use as a medicament according to any of to or the pharmaceutical composition of any of to , wherein D is a cycloalkyl group having from 4 to 7 C atoms , wherein said cycloalkyl group has one substituent R.19. The compound of any of to or to or the compound for use as a medicament according to any of to or to or the pharmaceutical composition of any of to or to , wherein the cycloalkyl group having from 4 to 7 C atoms which forms part of D is a cyclohexyl group.22. The compound of any of to or to or the compound for use as a medicament according to any of to or to or the pharmaceutical composition of any of to , wherein each Ris independently selected from —NRR , —NHOH , —NRCOR , —NRSOR , —NRCOOR , —NRCONRR , —NRSONRR , —CONRR , oxo , —Calkylene-NRR , —Calkylene-NHOH , —Calkyene-NRCOR , —Calkylene-NRSOR , —Calkylene-NRCOOR , —Calkylene-NRCONRR , — ...

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26-12-2019 дата публикации

PRODUCTION OF N-SUBSTITUTED AROMATIC HYDROXYLAMINE

Номер: US20190389808A1
Автор: Steiner Heinz
Принадлежит:

An economic, one-step method for the production of N-substituted aromatic hydroxylamines of formula (I) 2. Method according to claim 1 , characterised in that the group R comprises aromatic hydrocarbons or heteroaromatics claim 1 , or condensed or linked ring systems claim 1 , and the group R is unsubstituted or substituted.3. (canceled)4. Method according to claim 1 , characterised in that Rstands for linear or branched C-C-alkyl claim 1 , C-C-cycloalkyl claim 1 , benzyl or phenyl.5. (canceled)6. Method according to claim 1 , characterised in that the compounds of formula III are C-C-alkyl-O—CO—Cl.7. Method according to claim 1 , characterised in that the compounds of formula III are chloroformic acid methylester.8. Method according to claim 1 , characterised in that it is performed in the presence of an inert aprotic and apolar or polar solvent.9. Method according to claim 1 , characterised in that water is added to the reaction mixture.10. Method according to claim 1 , characterised in that the catalyst is a platinum catalyst.11. Method according to claim 1 , characterised in that the noble metal catalysts are used in quantities of 0.1 to 10% by weight relative to the substrate.12. Method according to claim 1 , characterised in that modifiers are added to the catalyst or to the reaction mixture.13. Method according to claim 12 , characterised in that tertiary amines claim 12 , phosphorus compounds or sulphur compounds or mixtures thereof are added as modifiers.14. Method according to claim 13 , characterised in that the phosphorus compounds are selected from the group of phosphines claim 13 , phosphine oxides and phosphoric acids.15. Method according to claim 14 , characterised in that the phosphorus compound is hypophosphoric acid HPO.16. Method according to claim 13 , characterised in that the sulphur compounds are selected from the group sulphides claim 13 , thiols claim 13 , thioethers claim 13 , sulphoxides claim 13 , thioureas and aromatic sulphur compounds ...

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02-09-2008 дата публикации

Use as catalyst for forming urethanes, of fluorinated and trivalent metal acid salts, composition containing same and methods using same

Номер: KR100855926B1
Принадлежит: 로디아 쉬미

본 발명은 우레탄을 형성하기 위한 신규한 촉매에 관한 것이다. 상기 촉매는 하기 화학식을 특징으로 한다: The present invention relates to novel catalysts for forming urethanes. The catalyst is characterized by the following formula: [화학식 I] [Formula I] MY 3-q [Z] q MY 3-q [Z] q [식 중, Z 는 초강산의 음이온에 상응하는 라디칼이며, 이의 햄맷 상수는 13 이상, 유리하게는 13 초과이다; [Wherein Z is a radical corresponding to the anion of the superacid, the Hammock constant thereof being at least 13, advantageously greater than 13; M 은 3가 금속, 바람직하게는 루이스 산을 형성하는 것으로 공지된 것을 나타낸다; M represents a trivalent metal, preferably known to form a Lewis acid; Y 는 음이온 또는 1가 음이온성 관능기이다; Y is an anion or monovalent anionic functional group; q 는 1 내지 3 (경계 포함)에서 유리하게 선택된 정수이다]. q is an integer advantageously selected from 1 to 3, inclusive. 본 발명은 페인트에 적용가능하다. The present invention is applicable to paints.

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22-12-2021 дата публикации

Method for preparing 18f-bpa and intermediate

Номер: EP3838890A4
Принадлежит: Neuboron Medtech Ltd

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14-10-2010 дата публикации

ハロゲン置換テレフタル酸ジアミド化合物、その製造方法及び該化合物を用いたハロゲン置換ベンゼンジメタノールの製造方法

Номер: JP2010229128A
Принадлежит: Sumitomo Chemical Co Ltd

【課題】ハロゲン置換ベンゼンジメタノールの新規な製造方法を提供する。 【解決手段】ハロゲン置換ベンゼンジカルボキサミド化合物とピロカルボン酸ジアルキルを反応させて、N,N,N’,N’−テトラキス(アルコキシカルボニル)ベンゼンジカルボキサミド化合物を得る第1工程と、該N,N,N’,N’−テトラキス(アルコキシカルボニル)ベンゼンジカルボキサミド化合物を水素化ホウ素化合物で還元して、下式(4)で示されるハロゲン置換ベンゼンジメタノールを得る第2工程とを含むことを特徴とするハロゲン置換ベンゼンジメタノール(4)の製造方法。 (式中、X 1 、X 2 、X 3 およびX 4 は、水素原子またはハロゲン原子を表す。) 【選択図】なし

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21-01-2010 дата публикации

Catalyst for the synthesis of alkyl carbamates, the method for preparing the same and the use thereof

Номер: WO2009106237A3
Принадлежит: BAYER MATERIALSCIENCE AG

The present invention pertains to a catalyst for the synthesis of organic alkyl carbamates, the method for preparing the same and the use thereof. The catalyst comprises a catalytically active component and a catalyst support, and the catalytically active component being carried by the catalyst support, wherein the catalytically active component comprises a transition metal oxide, and the general formula of the transition metal oxide is EOx, wherein E is selected from transition metal element and x is in the range of 0.5-4.

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26-09-2001 дата публикации

在苯环上有取代基的o-氨基甲酰基-苯丙氨醇,它的药用盐及其制备方法

Номер: CN1071741C
Принадлежит: SK Holdings Co Ltd

本发明涉及以结构式(1)代表的在苯环上有取代基的O-氨基甲酰基-苯丙氨醇及其药用盐,它可用来预防和治疗包括抑郁和焦虑的CNS疾病;其中R是含1-8个碳原子的低级烷基;诸如F、Cl和I的卤素;含1-3个碳原子的烷氧基;含1-3个碳原子的硫代烷氧基;硝基,羟基或三氟化碳,x是1-3整数,条件是x为2或3时,R是相同的或不同的。

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25-02-2020 дата публикации

Intermediate, preparation method and application

Номер: CN110835310A
Автор: 何静, 李世红, 蔡飞, 闫恒
Принадлежит: Neuboron Medtech Ltd

本发明提供了一种中间体、及制备方法及应用。通过所述中间体可以得到高纯度的 18 F‑BPA,简化了在 18 F标记之后的合成步骤,操作简单、效率高。

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30-03-2016 дата публикации

Method for synthesizing rivastigmine hydrogen tartrate

Номер: CN105439906A

一种重酒石酸卡巴拉汀的制备方法,其步骤如下:⑴将Ⅱ化合物与Ⅲ在无催化剂或有催化剂的适宜溶剂中缩合为Ⅰ,Ⅰ在适宜溶剂中与L-(+)酒石酸成盐得酒石酸卡巴拉汀。 其中,R 1 为H、K、Na,R为Cl、Br、I,CN或SCN。本发明方法具有工艺路线短,反应温和,所用试剂易于回收,收率高等优点,适合工业化生产。

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05-04-2006 дата публикации

Method For Carbamoylating Alcohols

Номер: KR100567706B1
Принадлежит: 워너-램버트 캄파니 엘엘씨

본 발명은 메탄술폰산의 존재하에 알코올을 시안산나트륨을 사용하여 카르바모일화하는 방법에 관한 것이다. 반응을 무수의 조건하에서 수행할 수 있다. 본 방법은 알코올 잔기 및 염기성 잔기를 모두 포함하는 분자 및(또는) 항바이러스제 카프라비린의 술페닐 알코올 전구체와 같은 알코올 잔기 및 술페닐 잔기를 모두 포함하는 분자를 카르바모일화하는데 적합하다. The present invention relates to a process for carbamoylating an alcohol using sodium cyanate in the presence of methanesulfonic acid. The reaction can be carried out under anhydrous conditions. The method is suitable for carbamoylating molecules comprising both alcohol residues and basic residues and / or alcohol residues such as sulfenyl alcohol precursors of the antiviral agent capravirin and sulfenyl residues.

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01-11-2017 дата публикации

Propellane derivates and synthesis

Номер: EP3114107A4
Автор: Kevin Duane Bunker
Принадлежит: Kalyra Pharmaceuticals Inc

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23-09-2022 дата публикации

Method for preparing isocyanate by pipeline phosgene method

Номер: CN115093348A
Принадлежит: Mojia Shanghai Biotechnology Co ltd

本申请涉及一种制备异氰酸酯的方法。具体地,本申请提供了一种通过管道光气化法制备异氰酸酯的方法。

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15-12-2015 дата публикации

Methods and devices for using isoperillyl alcohol

Номер: US9211269B2
Принадлежит: Neonc Technologies Inc

The present invention provides for a method of treating a disease such as cancer, comprising the step of administering to a patient a therapeutically effective amount of an isomer or analog of monoterpene or sesquiterpene (or its derivative), such as an isoperillyl alcohol. The present invention also provides for a method of treating a disease comprising the step of administering to a patient a therapeutically effective amount of a derivative of an isomer or analog of monoterpene or sesquiterpene, such as an isoperillyl alcohol carbamate. The derivative may be an isoperillyl alcohol conjugated with a therapeutic agent such as a chemotherapeutic agent. The route of administration may vary, including inhalation, intranasal, oral, transdermal, intravenous, subcutaneous or intramuscular injection.

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08-03-2017 дата публикации

(miscellaneous) aryl cyclopropyl amines as LSD1 inhibitor

Номер: CN103958474B
Принадлежит: Oryzon Genomics SA

本发明涉及(杂)芳基环丙基胺化合物,特别包括如本文所述和所定义的式I的化合物,且本发明涉及它们在疗法中的用途,包括例如在治疗或预防癌症、神经系统疾病或病症或病毒感染中的用途。

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18-02-2022 дата публикации

Catalyst for coproduction of oxamide and methyl carbamate and preparation method thereof

Номер: CN112915993B

本发明公开了一种联产草酰胺和氨基甲酸甲酯的催化剂及制备方法。所述催化剂的化学式表示为:Zn a In b Zr (1‑a‑b) O‑M;催化剂的活性组分包括Zn、In、Zr的氧化物或复合氧化物,所述a的取值范围是0.01~0.7;b的取值范围是0.01~0.5;为提升催化剂的整体性能,催化剂中还添加了Mo、Al、Ce等助剂。该催化剂的特点是表面同时含有强酸性中心和强碱性中心。这两种具有相反性质的活性中心在特殊的催化剂结构下可以稳定存在,并且协同加速了氨基和酯基的交换速率,使反应可以在较低的温度下发生,从而平衡了尿素醇解和草酸二甲酯氨解两个反应的热力学区间,可提高草酸酯和氨基甲酸甲酯的收率,降低甲醇、氨气和碳酸酯等副产物的生成量。

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07-10-2014 дата публикации

Biocatalysts and methods for the synthesis of (S)-3-(1-aminoethyl)-phenol

Номер: US8852900B2
Принадлежит: Codexis Inc

The present disclosure provides engineered transaminase polypeptides having improved properties as compared to naturally occurring transaminases including the ability of converting the substrate, 3′-hydroxyacetophenone to (S)-3-(1-aminoethyl)-phenol in enantiomeric excess and high percentage conversion. Also provided are polynucleotides encoding the engineered transaminases, host cells capable of expressing the engineered transaminases, and methods of using the engineered transaminases to synthesize (S)-3-(1-aminoethyl)-phenol and related compounds useful in the production of active pharmaceutical ingredients.

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13-01-2015 дата публикации

Biocatalysts and methods for the synthesis of (S)-3-(1-aminoethyl)-phenol

Номер: US8932838B2
Принадлежит: Codexis Inc

The present disclosure provides engineered transaminase polypeptides having improved properties as compared to naturally occurring transaminases including the ability of converting the substrate, 3′-hydroxyacetophenone to (S)-3-(1-aminoethyl)-phenol in enantiomeric excess and high percentage conversion. Also provided are polynucleotides encoding the engineered transaminases, host cells capable of expressing the engineered transaminases, and methods of using the engineered transaminases to synthesize (S)-3-(1-aminoethyl)-phenol and related compounds useful in the production of active pharmaceutical ingredients.

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02-09-2009 дата публикации

Catalyst used for synthesizing alkyl carbamate and preparing method and application thereof

Номер: CN101518729A

本发明涉及一种氨基甲酸烷基酯合成的催化剂、该催化剂的制备及其在氨基甲酸烷基酯合成中的应用。本发明所提供的催化剂包括一种催化剂活性成分和一种催化剂载体,所述催化剂活性成分搭载于所述催化剂载体上,所述催化剂活性成分包括一种过渡金属氧化物,所述过渡金属元素氧化物具有通式EOx,其中E表示一种过渡金属元素,x的取值范围为0.5-4。

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13-05-2022 дата публикации

Production method and production device of phenyl isocyanate

Номер: CN114478320A
Принадлежит: Upchem China Co ltd

本发明公开了一种苯基异氰酸酯的生产方法,将苯胺与溶剂配成苯胺溶液待用;在反应釜中加入固体光气和溶剂;60~130℃下,滴加苯胺溶液,滴加时长为0.5~1.5h,回流保温0.5~1.5h;反应过程通过DCS控制系统监控;得到反应混合液;采用连续化蒸馏方式提纯,将产物苯基异氰酸酯与副产物分离,收率达94%,产品含量≥99.5%。生产装置包括混配釜、反应釜、蒸馏器、冷凝器、产物储罐;蒸馏器的顶部、中部、底部分别设有低沸点副产物出口、产物出口和高沸点副产物出口。本发明采用绿色工艺制备苯基异氰酸酯,采用低毒化学品固体光气、溶剂,从物料的计量、输送及操作参数均采用DCS控制;采用一步法合成,反应稳定,副反应少;采用连续化蒸馏提纯,产品质量及收率高。

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13-09-2013 дата публикации

A novel method of making Endoxifen

Номер: KR101308258B1
Принадлежит: 씨제이제일제당 (주)

본 발명은 4,4-히드록시벤조페논을 출발물질로 사용하여 프로피오페논과 커플링시켜서 엔독시펜을 제조하는 방법에 관한 것으로, 종래의 엔독시펜 제조방법에 비해 높은 수율로 E/Z 형태의 엔독시펜 혼합물을 수득하고, 혼합물 중 약효를 나타내는 Z form을 99% 이상의 순도로 제공할 수 있다. The present invention relates to a method for preparing endoxifen by coupling with propiophenone using 4,4-hydroxybenzophenone as a starting material, and in an E / Z form at a higher yield than a conventional method for preparing endoxifen. To obtain an endoxifene mixture of, Z form showing the efficacy in the mixture can be provided with a purity of 99% or more.

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10-02-2021 дата публикации

Method for preparing intermediate compound for synthesis of medicinal agent

Номер: RU2742765C1
Принадлежит: ЭлДжи КЕМ, ЛТД.

FIELD: chemistry. SUBSTANCE: invention relates to a method of producing a compound of chemical formula 2, which is an intermediate compound used for synthesis of antidiabetic agents inhibiting the enzyme dipeptidyl peptidase IV. Method includes 1) a step of introducing a protective group P 1 into an amine group of a compound of chemical formula 6 to obtain a compound of chemical formula 5, in which the amine group is protected, 2) a step for producing a compound of chemical formula 4 by cyclisation through a condensation reaction of a compound of chemical formula 5 obtained in step 1), with paraformaldehyde and an acid catalyst, 3) a step for introducing a protective group P 2 into a carboxylic acid group of a compound of chemical formula 4 obtained in step 2), and converting a carboxylic acid group to an ester group to obtain a compound of chemical formula 3 and 4) a step for reacting ammonia as a nitrogen source with a compound of chemical formula 3 obtained at step 3), to obtain an amide compound of chemical formula 2 through decyclization of oxazolidinone. In compounds of chemical formulas 2−5 P 1 is Boc (butyloxycarbonyl), Cbz (benzyloxycarbonyl) or Fmoc (9-fluorenylmethyloxycarbonyl) as an amine protecting group, and P 2 is a protective carboxylic acid group. [Chemical formula 6] [Chemical formula 5] [Chemical formula 4] [Chemical formula 3] [Chemical formula 2] EFFECT: technical result is higher yield of compound of chemical formula 2. 14 cl, 4 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 742 765 C1 (51) МПК C07D 263/06 (2006.01) C07C 231/10 (2006.01) C07C 237/06 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (52) СПК C07D 263/06 (2020.05); C07C 231/10 (2020.05); C07C 237/06 (2020.05) (21)(22) Заявка: 2020114741, 28.09.2018 (24) Дата начала отсчета срока действия патента: Дата регистрации: 10.02.2021 28.09.2017 KR 10-2017-0126119; 28.09.2018 KR 10-2018-0115838 (45) Опубликовано: 10.02.2021 Бюл. № 4 (85) Дата ...

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19-05-2020 дата публикации

Lefamulin intermediate compound and application thereof in preparation of Lefamulin

Номер: CN111170893A
Автор: 张俊杰, 白晓光

本发明公开了一种Lefamulin的中间体化合物及其在Lefamulin制备中的应用,以期解决现有技术中Lefamulin制备成本高、收率低的技术问题。本发明提供一种中间体化合物 及其制备方法,并将上述中间体化合物在制备Lefamulin或Lefamulin相关的医药中间体中的应用。本发明克服了现有技术的生产过程中碰到的手性氧化缺乏手性诱导,造成目标化合物转化率非常低、成本非常高、工业化生产困难的缺陷;工业化应用时能够有效降低生产成本,且可以有效控制三废的产生,具有显著的经济效益和社会效益。

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19-11-1996 дата публикации

O-carbamoyl-phenylalanine having a substituent in phenyl, a pharmaceutically useful salt thereof, and a method for preparing the same

Номер: KR960037649A
Принадлежит: 조규향, 주식회사 유 공

본 발명은 하기 일반식(Ⅳ)로 표시되는 페닐에 치환체가 있는 O-카바모일-페닐알라닌을 화합물과 그의 약제적으로 유용한 염 및 이들의 제조방법에 관한 것이다. 상기 식중에서, R은 1∼8의 탄소원자를 갖는 저급알킬이거나, F, Cl, I 등의 할로겐, 1∼3의 탄소원자를 갖는 알콕시, 1∼3의 탄소원자를 갖는 티오알콕시, NO 2 , OH 또는 CF 3 이며, x는 1∼3의 범위를 갖고 x가 2 혹은 3일 경우 R은 동일하거나 다를 수 있다.

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20-07-2005 дата публикации

Method for carbamoylation of alcohols

Номер: RU2256657C2

FIELD: organic chemistry, chemical technology. SUBSTANCE: invention relates to a method for carbamoylation reaction of alcohol having both alcoholic moiety and basic moiety and/or sulfenyl moiety. Method involves mixing cyanate with indicated alcohol in inert solvent in anhydrous conditions, cooling formed reaction mixture to temperature from about -25°C to about 40°C, addition of acid to the cooled reaction mixture at the rate maintaining temperature lower 0°C, stirring the acid-containing reaction mixture at temperature from about -10°C to about 0°C for about 8-10 h and treatment of the reaction mixture with water. Method can be used for carbamoylation reaction of capravirine sulfenyl alcohol. Method provides enhancing conversion of alcohol and yield of carbamate. EFFECT: improved method for carbamoylation reaction. 11 cl, 3 ex ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß (19) RU (51) ÌÏÊ 7 (11) 2 256 657 (13) C2 C 07 D 401/06, C 07 C 269/02 ÔÅÄÅÐÀËÜÍÀß ÑËÓÆÁÀ ÏÎ ÈÍÒÅËËÅÊÒÓÀËÜÍÎÉ ÑÎÁÑÒÂÅÍÍÎÑÒÈ, ÏÀÒÅÍÒÀÌ È ÒÎÂÀÐÍÛÌ ÇÍÀÊÀÌ (12) ÎÏÈÑÀÍÈÅ ÈÇÎÁÐÅÒÅÍÈß Ê ÏÀÒÅÍÒÓ (21), (22) Çà âêà: 2003123791/04, 11.01.2002 (72) Àâòîð(û): ÝËËÈÑ Äæåéìñ Ýäâàðä (US) (24) Äàòà íà÷àëà äåéñòâè ïàòåíòà: 11.01.2002 (30) Ïðèîðèòåò: 31.01.2001 (ïï.1-11) US 60/265,502 (73) Ïàòåíòîîáëàäàòåëü(ëè): ÓÎÐÍÅÐ-ËÀÌÁÅÐÒ ÊÎÌÏÀÍÈ ËËÑ (US) R U (43) Äàòà ïóáëèêàöèè çà âêè: 27.02.2005 (45) Îïóáëèêîâàíî: 20.07.2005 Áþë. ¹ 20 2 2 5 6 6 5 7 (56) Ñïèñîê äîêóìåíòîâ, öèòèðîâàííûõ â îò÷åòå î ïîèñêå: LOEV B., KORMENDY M. Journal of Organic Chemistry. 1963, 28(12), p. 34213426. DE 2611695 A, 29.09.1977. SU 882403 A, 15.11.82. (85) Äàòà ïåðåâîäà çà âêè PCT íà íàöèîíàëüíóþ ôàçó: 30.07.2003 2 2 5 6 6 5 7 R U (87) Ïóáëèêàöè PCT: WO 02/060893 (08.08.2002) C 2 C 2 (86) Çà âêà PCT: IB 02/00082 (11.01.2002) Àäðåñ äë ïåðåïèñêè: 129010, Ìîñêâà, óë. Á.Ñïàññêà , 25, ñòð.3, ÎÎÎ "Þðèäè÷åñêà ôèðìà Ãîðîäèññêèé è Ïàðòíåðû", ïàò.ïîâ. Å.Å.Íàçèíîé (54) ÑÏÎÑÎÁ ÊÀÐÁÀÌÎÈËÈÐÎÂÀÍÈß ÑÏÈÐÒΠ(57) Ðåôåðàò: Èçîáðåòåíèå îòíîñèòñ ê ñïîñîáó êàðáàìîèëèðîâàíè ñïèðòà, ñîäåðæàùåãî ...

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28-02-1996 дата публикации

Process for the preparation of optically active 4-amino-3-hydroxycarboxylic acids

Номер: EP0529483B1
Принадлежит: Lonza AG

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24-07-2014 дата публикации

Process for preparing the anti-tumor agent 6-(7-((1-aminocyclopropyl) methoxy)-6-methoxyquinolin-4-yloxy)-n-methyl-1-naphthamide and its crystalline

Номер: WO2014113616A1
Автор: Guoqing Paul Chen
Принадлежит: Advenchen Pharmaceuticals, LLC

The present invention relates a new process to synthesize 6-(7-((l-aminocyclo-propyl)- methoxy)-6-methoxyquinolin-4-yloxy)-N-methyl- l -naphthamide (AL3810) by deprotection of substituted benzyl 1 -((6-methoxy-4-(5-(methylcarbamoyl)naphthalen-2-yloxy)quinolin-7-yloxy)- methyl)cyc-lopropylcarbamate (Formula I) under a diluted or weak acidic condition. A stable crystalline form of 6-(7-((l-aminocyclo-propyl)-methoxy)-6-methoxyquinolin-4-yloxy)-N- methyl- 1 -naphthamide has also been prepared.

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31-05-2019 дата публикации

Method of using titanium catalyst for producing materials containing carbamate functional groups

Номер: RU2690164C2
Принадлежит: БАСФ Коатингс ГмбХ

FIELD: manufacturing technology.SUBSTANCE: invention relates to a method of producing a material, to a material obtained using such a method, which can be used to produce thermosetting coatings, to a coating composition, as well as to a method of applying a coating composition. Method of producing the material involves reaction of a carbamate compound with a material containing hydroxyl functional groups using titanium (IV) alkoxide as a catalyst. Alkoxide of titanium (IV) is used in amount of 0.13 to 1.58 wt%, based on total weight of material with hydroxyl functional groups and carbamate compounds. Carbamate compound used is alkyl carbamate. Material containing hydroxyl functional groups used is polyol having 12 to 72 carbon atoms and at least two hydroxyl groups. Coating composition includes said material containing carbamate functional groups and one or more conventional coating additives. Coating composition application method involves application of said coating composition by any known method onto surface.EFFECT: invention enables to obtain a colorless material which does not contain tin, and also obtain a coating which has high resistance to scratching, good resistance to acids, good resistance to atmospheric conditions.10 cl, 1 tbl, 7 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 690 164 C2 (51) МПК C07C 269/06 (2006.01) C08G 71/04 (2006.01) C08F 8/30 (2006.01) C09D 175/04 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (52) СПК C07C 269/06 (2019.02); C08G 71/04 (2019.02); C08F 8/30 (2019.02); C09D 175/04 (2019.02) (21)(22) Заявка: 2016147986, 13.04.2015 (24) Дата начала отсчета срока действия патента: (73) Патентообладатель(и): БАСФ КОАТИНГС ГМБХ (DE) Дата регистрации: 31.05.2019 R U 13.04.2015 (72) Автор(ы): ЯДХАВ Абхийит (IN) (56) Список документов, цитированных в отчете о поиске: Shapiro G., Marzi M. Facile and 08.05.2014 US 14/272,597 (43) Дата публикации заявки: 08.06.2018 Бюл. № 16 selective O-alkyl ...

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22-11-2019 дата публикации

The production for the aromatic hydroxyamines that N- replaces

Номер: CN110494417A
Автор: H·斯坦纳
Принадлежит: Solvias AG

一种用氢气生产式(I)的N‑取代芳族羟胺的经济的一步法:R‑N(OH)‑C(=O)‑(O)R 1 (I),该方法中,在非质子溶剂中和在卤代甲酸酯存在下,在某些情况下在碱存在下,用可能改性的水合催化剂催化水合来生产式(I)的N‑取代芳族羟胺。

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23-10-2019 дата публикации

Method for producing 3-phenylisoserine derivative

Номер: JP6593328B2
Автор: 健 西川, 悠文 平賀
Принадлежит: Toray Fine Chemicals Co Ltd

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01-07-2014 дата публикации

(hetero)arylcyclopropylamine compounds as lsd1 inhibitors

Номер: KR20140081883A
Принадлежит: 오리존 지노믹스 에스.에이.

본 발명은 (헤테로)아릴 사이클로프로필아민 화합물, 특히 본원에 개시되고 정의된 바와 같은 하기 화학식 I의 화합물, 및 예를 들어 암, 신경학적 질병 또는 상태, 또는 바이러스 감염의 치료 또는 예방을 포함한 요법에서의 그의 용도에 관한 것이다. 화학식 I

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22-06-2016 дата публикации

Method for preparing arene beta-amino alcohol of optical voidness

Номер: CN105693555A
Принадлежит: Zhongshan Haihong Medicine Co Ltd

本发明公开了一种光学纯的芳烃β-氨基醇的制备方法,其特征在于包括以下步骤:D或L-氨基酸起始物料与氯甲酸苄酯CBz-Cl或BOC酐酸反应得化合物I-1;将化合物I-1用多聚甲醛在溶剂A中回流脱水得到化合物I-2;将化合物I-2于格氏试剂反应,稀盐酸处理得到化合物I-3;化合物I-3用异丙醇铝催化还原即可。本发明的目的是克服现有技术所述的缺点,提供一种物料廉价易得有利于降低成、制备工艺简单,所得中间体结构稳定的医药中间体的制备方法。

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05-07-2022 дата публикации

Anthranilic acid amide compound based on entinostat skeleton and preparation and application thereof

Номер: CN113185454B
Принадлежит: University of South China

本发明提供了一种基于恩替诺特骨架的邻氨基苯甲酰胺类化合物及其制备与应用。本发明所制备的基于恩替诺特骨架的邻氨基苯甲酰胺类化合物的结构式为 其中,R为甲氨基、二甲氨基、羟基、NH 2 或

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01-12-2020 дата публикации

Method for producing carbamate and method for producing isocyanate

Номер: CN112020493A
Принадлежит: Asahi Kasei Corp

本发明提供一种包括下述工序(1)和工序(2)的氨基甲酸酯的制造方法等。(1)使用一分子中具有至少1个伯氨基的有机伯胺与二氧化碳和碳酸衍生物中的至少任一种,在低于脲键的热解离温度的温度下,制造具有脲键的化合物(A)的工序;(2)使上述化合物(A)与碳酸酯反应来制造氨基甲酸酯的工序。

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16-02-1983 дата публикации

Process for preparing urethanes

Номер: EP0071835A1
Принадлежит: Bayer AG

1. Process for the preparation of urethanes by reacting a) unsubstituted or substituted ureas which do however still contain at least one hydrogen atom attached to a urea nitrogen atom, with b) organic compounds containing at least one hydroxyl group and c) carbon monoxide in the presence of d) molecular oxygen and e) a catalyst system containing at least one noble metal and/or noble metal compound of the eighth sub-group of the periodic system of elements, characterised in that the reaction is carried out in the presence of catalyst systems e) which contain as a further component at least one quinoid compound having oxidizing action and/or at least one compound which can be converted, under the reaction conditions, into a quinoid compound having oxidizing action.

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02-12-2022 дата публикации

Synthesis method of o-amino aryl ketone derivative

Номер: CN115417796A
Автор: 商铭洲, 董训青, 陆红健
Принадлежит: NANJING UNIVERSITY

本发明一种邻氨基芳基酮衍生物的合成方法,以银盐为催化剂,2,2,2‑三氯乙氧基羰基(Troc)叠氮化物为胺化试剂,实现芳烃的羰基定向单C‑H胺化,该方法提供了在温和条件下直接制备邻氨基芳基酮衍生物的方法,实现了多种芳基羰基化合物的胺化反应,包括烷基和乙烯基芳基酮、仲和叔芳基酰胺以及乙酰基吲哚。该方法可以利用所得邻位‑TrocNH芳基羰基化合物转化为相应的游离芳基胺、芳基氨基甲酸酯、芳基脲以及芳基稠合的N‑杂环。

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02-09-2008 дата публикации

Process for preparing aryl-iminomethyl-carbamino acid esters

Номер: CA2399598C

The invention relates to a method for producing compounds of formula (I) wherein the radicals R1 and R2 have the meanings given in the description and in the claims, which can be used on a large scale.

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17-08-2018 дата публикации

Aromatic rings allylamine compound, its pharmaceutically acceptable salt, Its Preparation Method And Use

Номер: CN105924362B

本发明涉及一种结构如通式(I)所示的芳香环丙基胺类化合物及其药学上可接受的盐,及其该类化合物的制备方法和该类化合物在制备预防或治疗耳聋的药物中的用途。其中,本发明所涉及的通式(I)中的R 1 、R 2 、R 3 、R 4 和R 5 如说明书和权利要求中所定义。

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20-09-2014 дата публикации

Method of producing n-substituted carbamic acid ester and method of producing isocyanate using n-substituted carbamic acid ester

Номер: RU2528423C2

FIELD: chemistry. SUBSTANCE: invention relates to a method of producing at least one N-substituted carbamic acid-O-aryl ester (where said ester denotes an N-substituted carbamic acid ester in which oxygen atoms of the carbamic acid group (-NHCOO-) are bonded to an aromatic ring) from a compound of formula (1), having a ureido group, and aromatic hydroxy-compound of formula (2) or an aromatic hydroxy composition containing at least one type of aromatic hydroxy compound of formula (2). The method includes a step for esterification or esterification and re-esterification of a compound of formula (1) and an aromatic hydroxy compound or an aromatic hydroxy composition of formula (2). In formula (1), R 1 is an organic group containing a whole number of carbon atoms ranging from 1 to 85, which is substituted a times by ureido group(s), a is an integer from 1 to 10. In formula (2), the ring A is an aromatic group selected from a benzene or naphthalene ring which is substituted b times with OH groups, and can be substituted with at least one substitute selected from groups of substitutes (i)-(v), which retain aromatic properties of ring A, ring A and at least one substitute contain a whole number of carbon atoms ranging from 6 to 50, b is an integer from 1 to 2. The groups of substitutes (i)-(v) denote (i) a hydrogen atom; (ii) a group consisting of carbon and hydrogen atoms which can also form a ring structure by binding with ring A; (iii) a group consisting of carbon, hydrogen and oxygen atoms; (iv) a halogen atom; (v) a group consisting of atoms selected from carbon, hydrogen, oxygen, nitrogen, sulphur and halogen atoms, except groups containing a carbonyl, ester, carboxyl, terminal methine and alcohol OH groups, NH 2 -, NH-, NOH-, SH-, SO 3 H- and SOH- groups. EFFECT: method enables to prevent formation of byproducts and reuse of starting substances; the invention also relates to different versions of the disclosed method, a composition for transportation and storage of ...

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12-08-1977 дата публикации

Patent FR2202057B1

Номер: FR2202057B1
Автор: [UNK]
Принадлежит: American Cyanamid Co

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03-03-2017 дата публикации

METHOD FOR PRODUCING ANTITUMOR AGENT 6- (7 - ((1-AMINOCYCLOPROPYL) METHOXY) -6-METOXYCHINOLIN-4-ILOXY) -N-METHYL-1-NAPHTHAMIDE AND ITS CRYSTAL STRUCTURE

Номер: RU2015127211A

РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2015 127 211 A (51) МПК C07D 215/22 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2015127211, 17.01.2014 (71) Заявитель(и): АДВЕНЧЕН ФАРМАСЬЮТИКАЛС, ЛЛС (US) Приоритет(ы): (30) Конвенционный приоритет: 18.01.2013 US 61/754,516 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 18.08.2015 R U (43) Дата публикации заявки: 03.03.2017 Бюл. № 07 (72) Автор(ы): ЧЭН Гоцин Пол (US) (86) Заявка PCT: (87) Публикация заявки PCT: WO 2014/113616 (24.07.2014) (54) СПОСОБ ПОЛУЧЕНИЯ ПРОТИВООПУХОЛЕВОГО АГЕНТА 6-(7-((1-АМИНОЦИКЛОПРОПИЛ) МЕТОКСИ)-6-МЕТОКСИХИНОЛИН-4-ИЛОКСИ)-N-МЕТИЛ-1-НАФТАМИДА И ЕГО КРИСТАЛЛИЧЕСКОЙ СТРУКТУРЫ R U (57) Формула изобретения 1. Способ получения 6-(7-((1-аминоциклопропил)-метокси)-6-метоксихинолин-4илокси)-N-метил-1-нафтамида (AL3810) или его фармацевтически приемлемой соли путем удаления защитной группы замещенного бензил-1-((6-метокси-4-(5(метилкарбамоил)-нафталин-2-илокси)-хинолин-7-илокси)-метил)циклопропилкарбамата формулы I при разбавленной или слабокислой среде согласно следующей химической схеме: где Стр.: 1 A 2 0 1 5 1 2 7 2 1 1 A Адрес для переписки: 190000, Санкт-Петербург, BOX 1125, "ПАТЕНТИКА" 2 0 1 5 1 2 7 2 1 1 US 2014/011948 (17.01.2014) R1 выбран из H, галогена, галоген-C1-C6алкила, C1-C6алкила, C1-C6алкокси, циано или нитро, предпочтительно из H, C1-C6алкокси или нитро; R2 выбран из C1-C6алкокси или нитро, предпочтительно представляет собой метокси, разбавленная или слабокислая среда выбрана из 5-50% ТФУ в CH2Cl2 или CH3CN, 10% HCl в этаноле, 4н. HCl в диоксане, HCOOH в CH3CN или моногидрата птолуолсульфоновой кислоты в CH3CN. 2. Способ по п. 1 получения 6-(7-((1-аминоциклопропил)-метокси)-6-метоксихинолин4-илокси)-N-метил-1-нафтамида (AL3810) или его фармацевтически приемлемой соли, путем удаления защитной группы 4-метоксибензил-1-((6-метокси-4-(5-(метилкарбамоил) -нафталин-2-илокси)-хинолин-7-илокси)-метил)-циклопропилкарбамата ...

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26-10-2021 дата публикации

Unnatural amino acid, application thereof, recombinant protein containing unnatural amino acid and recombinant protein conjugate

Номер: CN113548984A
Принадлежит: Zhejiang New Code Biomedical Co ltd

本发明提供了一种非天然氨基酸,为具有如式(Ⅰ)所示结构的化合物或其对映异构体。本发明还提供了所述非天然氨基酸的应用。进一步地,本发明还提供了一种包含所述非天然氨基酸的重组蛋白以及由所述重组蛋白制得的蛋白偶联物。本发明提供的非天然氨基酸制备简便,安全性好,插入蛋白时不易失活,与偶联部分的结合率高,所得偶联物的稳定性较好,本发明提供的非天然氨基酸可应用于众多领域,尤其是在制备重组蛋白或重组蛋白偶联物中,

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29-08-2018 дата публикации

Method using zirconium catalyst for producing carbamate-functional materials

Номер: EP3140341B1
Автор: Abhijit JADHAV
Принадлежит: BASF COATINGS GMBH

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15-10-2020 дата публикации

Preparation and use of an ammonium salt

Номер: WO2020207129A1
Автор: 罗梅
Принадлежит: 合肥祥晨化工有限公司

一种铵盐,其结构式如式(I),其合成方法,用8mol%氯化锌做催化剂,1-苯基-1,3-丁二酮5mmol,苯甲胺1.2g,用40mL氯苯做溶剂,回流反应2天后,有晶体化合物铵盐析出。该铵盐晶体I的用途,作为催化剂苯甲醛的腈硅化反应及苯甲醛与苯甲酰胺的反应中显示了良好的催化性能,其转化率分别达39.7%,62%。

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20-07-1983 дата публикации

Process for the preparation of carbamates

Номер: EP0083764A2
Принадлежит: BASF SE

1. A process for the preparation of a carbamate of the formula see diagramm : EP0083764,P5,F1 where R**1 is an aliphatic, cycloaliphatic or araliphatic radical or R**3-(OR**2)n -, R**2 is an aliphatic radical of not less than 2 carbon atoms, R**3 is an aliphatic, cycloaliphatic or araliphatic radical, and n is an integer, by reacting urea with an alcohol, wherein urea is reacted with an alcohol of the formula R**1-OH where R**1 has the above meaning, at not less than 140 degrees C and under not less than 2 bar, an inert gas being passed through the reaction mixture and the pressure during the reaction being so set that the reaction mixture boils.

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23-04-2014 дата публикации

1,3-di-oxo-indene derivative, pharmaceutically acceptable salt or optical isomer thereof, preparation method thereof, and pharmaceutical composition containing same as an antiviral, active ingredient

Номер: CN103748060A

本发明公开一种1,3-二氧代茚衍生物、其药学上可接受的盐或对映体,其制备方法以及包含其作为活性成分用于预防或治疗病毒性疾病的药物组合物。所述1,3-二氧代茚衍生物具有优异的对抗包括柯萨奇病毒、肠病毒、艾柯病毒、脊髓灰质炎病毒和鼻病毒的小核糖核酸病毒的抑制活性,以及表现出低细胞毒性,这使得它们可以用作用于预防或治疗病毒性疾病的药物组合物的活性成分,所述病毒性疾病包括脊髓灰质炎、麻痹、急性出血性结膜炎、病毒性脑膜炎、手足口病、水疱病、甲型肝炎、肌炎、心肌炎、胰腺炎、糖尿病、流行性肌痛、脑炎、流感、疱疹性咽峡炎、口蹄疫、哮喘、慢性阻塞性肺病、肺炎、鼻窦炎或中耳炎。

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01-10-2018 дата публикации

Patent RU2016147985A3

Номер: RU2016147985A3
Автор: [UNK]
Принадлежит: [UNK]

`”ВУ“” 2016147985” АЗ Дата публикации: 01.10.2018 Форма № 18 ИЗ,ПМ-2011 Федеральная служба по интеллектуальной собственности Федеральное государственное бюджетное учреждение ж Я «Федеральный институт промышленной собственности» (ФИПС) ОТЧЕТ О ПОИСКЕ 1. . ИДЕНТИФИКАЦИЯ ЗАЯВКИ Регистрационный номер Дата подачи 2016147985/04(077104) 14.04.2015 РСТ/ЕР2015/058077 14.04.2015 Приоритет установлен по дате: [ ] подачи заявки [ ] поступления дополнительных материалов от к ранее поданной заявке № [ ] приоритета по первоначальной заявке № из которой данная заявка выделена [ ] подачи первоначальной заявки № из которой данная заявка выделена [ ] подачи ранее поданной заявки № [Х] подачи первой(ых) заявки(ок) в государстве-участнике Парижской конвенции (31) Номер первой(ых) заявки(ок) (32) Дата подачи первой(ых) заявки(ок) (33) Код страны 1. 14/272593 08.05.2014 05 Название изобретения (полезной модели): [Х] - как заявлено; [ ] - уточненное (см. Примечания) СПОСОБ ПРИМЕНЕНИЯ ЦИРКОНИЕВОГО КАТАЛИЗАТОРА ДЛЯ ПОЛУЧЕНИЯ МАТЕРИАЛОВ, СОДЕРЖАЩИХ КАРБАМАТНЫЕ ФУНКЦИОНАЛЬНЫЕ ГРУППЫ Заявитель: БАСФ КОАТИНГС ГМБХ, РЕ 2. ЕДИНСТВО ИЗОБРЕТЕНИЯ [Х] соблюдено [ ] не соблюдено. Пояснения: см. Примечания 3. ФОРМУЛА ИЗОБРЕТЕНИЯ: [Х] приняты во внимание все пункты (см. п см. Примечания [ ] приняты во внимание следующие пункты: р [ ] принята во внимание измененная формула изобретения (см. Примечания) 4. КЛАССИФИКАЦИЯ ОБЪЕКТА ИЗОБРЕТЕНИЯ (ПОЛЕЗНОЙ МОДЕЛИ) (Указываются индексы МПК и индикатор текущей версии) СОЗЕ 220/36 (2006.01) С07С 269/06 (2006.01) С08С 71/04 (2006.01) (090 175/12 (2006.01) В05О 7/14 (2006.01) 5. ОБЛАСТЬ ПОИСКА 5.1 Проверенный минимум документации РСТ (указывается индексами МПК) С08Е220/36, С07С269/06, С08Е4/64, С0807 1/04, С090175/12, В9507/14 5.2 Другая проверенная документация в той мере, в какой она включена в поисковые подборки: 5.3 Электронные базы данных, использованные при поиске (название базы, и если, возможно, поисковые термины): СТРО, РЕРАТБпе, ЕАРАТГУ, Езрасепек, ]-Р1а Ра, ...

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