НОВЫЙ СПОСОБ ПОЛУЧЕНИЯ ПРОИЗВОДНЫХ ТРИАЗИНА, ПИРИМИДИНА И ПИРИДИНА

FIELD: chemistry.SUBSTANCE: invention relates to a method of producing triazine, pyrimidine and pyridine derivatives of formula (I) by condensation of the corresponding halogen-triazine, pyrimidine or pyridine via a coupling reaction of Suzuki with pyridyl- or pyrimidinyl-borane, where the amino-functional group is protected in form of formamidine. Invention also relates to suitable intermediate compounds and methods of producing said intermediate compounds..EFFECT: technical result is a novel method of producing compounds of formula (I), which enables to obtain desired compounds with high output and purity.19 cl, 3 tbl, 17 ex, 1 dwg РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 688 665 C2 (51) МПК C07D 213/127 (2006.01) C07D 213/53 (2006.01) A61K 31/5377 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (52) СПК C07D 213/127 (2013.01); C07D 213/53 (2013.01); A61K 31/5377 (2013.01) (21)(22) Заявка: 2016138800, 20.04.2015 (24) Дата начала отсчета срока действия патента: Дата регистрации: (73) Патентообладатель(и): УНИВЕРСИТЕТ БАЗЕЛЬ (CH), ПИКУР ТЕРАПЬЮТИКС АГ (CH) 22.05.2019 (56) Список документов, цитированных в отчете о поиске: WO 2012109423 A1, 16.08.2012. 22.04.2014 EP 14165418.6 (43) Дата публикации заявки: 22.05.2018 Бюл. № 15 (45) Опубликовано: 22.05.2019 Бюл. № 15 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 22.11.2016 EP 2015/058493 (20.04.2015) C 2 C 2 (86) Заявка PCT: Gomez-Garcia, Omar et al, Tertiary formylated amines by microwave irradiation of N,Ndimethyl-N′-(2-pyridyl)formamidines with methyl vinyl ketone, Heterocycl. Commun., 20(1), 21-23, 2014. Gomez-Garcia, Omar, Reaction of Tosylmethyl Isocyanide with NHeteroaryl Formamidines: an Alternative Approach to the Synthesis of (см. прод.) (87) Публикация заявки PCT: 2 6 8 8 6 6 5 WO 2015/162084 (29.10.2015) R U 2 6 8 8 6 6 5 Приоритет(ы): (30) Конвенционный приоритет: R U 20.04.2015 (72) Автор(ы): ХЕБАЙСЕН Пауль (CH), БОФИС Флоран (FR), ...

Patent RU2017100520A3

7 ВУ“” 2017100520” АЗ Дата публикации: 09.11.2018 Форма № 18 ИЗИМ-2011 Федеральная служба по интеллектуальной собственности Федеральное государственное бюджетное учреждение 5 «Федеральный институт промышленной собственности» (ФИПС) ОТЧЕТ О ПОИСКЕ 1. . ИДЕНТИФИКАЦИЯ ЗАЯВКИ Регистрационный номер Дата подачи 2017100520/04(000849) 20.03.2015 РСТ/ОВ2015/050835 20.03.2015 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. 62/011,168 12.06.2014 05 Название изобретения (полезной модели): [Х] - как заявлено; [ ] - уточненное (см. Примечания) КОМПЛЕКСЫ Заявитель: ДЖОНСОН МЭТТИ ПАБЛИК ЛИМИТЕД КОМПАНИ, ОВ 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) С07Е 15/00 (2006.01) ВО1. 31/24 (2006.01) С07В 43/04 (2006.01) СО7Е 19/00 (2006.01) С07В 37/02 (2006.01) ВО1. 31/22 (2006.01) С07В 37/04 (2006.01) 5. ОБЛАСТЬ ПОИСКА 5.1 Проверенный минимум документации РСТ (указывается индексами МПК) СО7Е 15/00 СО7Е 19/00 ВО11 31/22 ВО11 31/24 СО7В 37/02 СО7В 37/04 СО7В 43/04 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): Езрасепе, Соозе, РабеагсВ, Кеахуз, эГМ ОпПпе 6. ДОКУМЕНТЫ, ОТНОСЯЩИЕСЯ К ПРЕДМЕТУ ПОИСКА ...

СИНТЕЗ ПОЛУСИНТЕТИЧЕСКИХ ПРОИЗВОДНЫХ ПРИРОДНЫХ ЛЮТЕИНА И АСТАКСАНТИНА

Изобретение относится к фармации, в частности к химико-фармацевтической отрасли, и касается способа получения новых полусинтетических производных лютеина и астаксантина и может использоваться для получения лекарственных препаратов на основе этих соединений. Описан синтез полусинтетических производных индивидуальных природных каротиноидов, в частности сложных эфиров лютеина и бензойной кислоты, лютеина и n-метилбензойной кислоты (n-толуиловой кислоты), лютеина и никотиновой кислоты, лютеина и миндальной кислоты, астаксантина и бензойной кислоты, астаксантина и n-метилбензойной кислоты (n-толуиловой кислоты), астаксантина и никотиновой кислоты, астаксантина и миндальной кислоты. Способ синтеза сложных эфиров лютеина и астаксантина проводят в присутствии биокатализатора Новозима 435. Синтез полусинтетических производных природных лютеина и астаксантина не требует сложного и дорогостоящего технического оснащения, позволяет получать сложные эфиры лютеина и астаксантина, которые в дальнейшем ...

СИНТЕЗ ПОЛУСИНТЕТИЧЕСКИХ СЛОЖНЫХ ЭФИРОВ ПРИРОДНОГО ЗЕАКСАНТИНА

Изобретение относится к фармации, в частности к химико-фармацевтической отрасли, и касается способа получения новых полусинтетических сложных эфиров зеаксантина и может использоваться для получения лекарственных препаратов на основе этих соединений. Описан синтез полусинтетических сложных эфиров природного зеаксантина и бензойной, n-метилбензойной, фенилгликолиевой, никотиновой, салициловой кислот, ибурофена и кетопрофена. Способ синтеза сложных эфиров зеаксантина позволяет проводить реакции этерификации с модельными кислотами (бензойной, фенилгликолиевой, n-метилбензойной) и лекарственными средствами (никотиновой и салициловой кислотами, ибупрофеном, кетопрофеном) в неводной среде, при температуре 40°С, что обусловлено применением биокатализатора Amano Lipase PS. Предлагаемый способ синтеза полусинтетических производных природного зеаксантина позволяет получать его сложные эфиры с модельными кислотами (бензойной, фенилгликолиевой, 4-метилбензойной) и лекарственными средствами (никотиновой ...

Catalyst for biaryl production

SYNTHESIS OF MORPHIN-6-GLUCURONID

Novel manufacturing process for triazine, pyrimidine and pyridine derivatives

The invention relates to a method of manufacturing triazine, pyrimidine and pyridine derivatives of formula (I), wherein U, V, W and Z are nitrogen or carbon atoms, whereby at least one of U, V and W is nitrogen, and the other substituents are defined as in the specification, by condensing a corresponding halo-triazine, pyrimidine or pyridine in a type of Suzuki coupling with a pyridyl- or pyrimidinyl-borane, wherein the amino function is protected as a formamidine. The invention further relates to suitable intermediates and methods of manufacturing of such intermediates. Furthermore the invention relates to pure 5-(4,6-dimorpholino-1,3,5- triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine in solid form.

MORPHINE-6-GLUCURONIDE SYNTHESIS

The invention provides a novel method for synthesising M6G, and intermediates therefor. In order to synthesise M6G the major problem to overcome is to obtain the glycoside linkage with very high .beta.-selectivity since prior methods produce the .alpha.-anomer. The invention provides a method for the preferential synthesis of the, .beta.-anomer of M6G which includes the step shown in Scheme 6: wherein use of DMAP is optional.

Synthesis process of 2.2 ' - bipyridine - and bimetallic nanoparticle catalysts by means of supported metal.

Die vorliegende Erfindung offenbart das Syntheseverfahren von 2,2´-Bipyridyl mit Hilfe von unterstützten Metall- oder Bimetall-Nanopartikel-Katalysatoren, gekennzeichnet durch: mit Hilfe von unterstützten Metall- oder Bimetall-Nanopartikel-Katalysatoren M 1 /AI 2 O 3 oder M 1 /M 2 /Al 2 O 3 wird Pyridin durch direkte Kupplung zu 2,2´-Bipyridyl synthetisiert. Bei den unterstützten Metall- oder Bimetall-Nanopartikel-Katalysatoren M 1 /AI 2 O 3 oder M 1 /M 2 /Al 2 O 3 dient Al 2 O 3 als Träger und die aktiven Bestandteile sind ein oder zwei unterschiedliche Metalle M 1 und M 2 . M 1 und M 2 sind jeweils unabhängig voneinander unter Edelmetallen Pd, Pt, Ru, Au, Ag, Rh oder Nichtedelmetallen Ni, Cu, Fe, Zn, Co gewählt. Mit dieser Erfindung wird ein unterstützter Metall- oder Bimetall-Nanopartikel-Katalysator in einer direkten Kupplungssynthese von 2,2´-Bipyridyl aus Pyridin verwendet. Die Produktionseffizienz ist hoch, die Produktion entspricht den Prinzipien der Atom-Ökonomie in der Chemieindustrie ...

Process for the synthesis of 2, 2' - bipyridine using a supported bimetallic nanoparticle catalyst.

Die vorliegende Erfindung offenbart das Syntheseverfahren von 2, 2´-Bipyridyl mithilfe eines unterstützten Bimetall-Nanopartikel-Katalysators, dadurch gekennzeichnet: mithilfe eines unterstützten Bimetall-Nanopartikel-Katalysators M 1 -M 2 @Al 2 O 3 wird Pyridin durch direkte Kupplung zu 2, 2´-Bipyridyl synthetisiert. Bei unterstütztem Bimetall-Nanopartikel-Katalysator M 1 -M 2 @Al 2 O 3 dient Al 2 O 3 als Träger und aktive Bestandteile sind zwei unterschiedliche Metalle M 1 und M 2 . M 1 und M 2 sind jeweils unabhängig voneinander unter Edelmetallen Pd, Pt, Ru, Au, Ag, Rh oder Nichtedelmetallen Ni, Cu, Fe, Zn, Co gewählt. Mit dieser Erfindung wird unterstützter Bimetall-Nanopartikel-Katalysator in direkte Kupplungssynthese von 2, 2´-Bipyridyl aus Pyridin verwendet. Die Produktionseffizienz ist hoch, die Produktion entspricht den Prinzipien der Atom-Ökonomie in Chemieindustrie und keine Umweltbelastungen entstehen. Das ist eine grüne Produktionstechnologie zur Herstellung von chemischen ...

Process For Production Of Bis-quaternary Ammonium Salt, And Novel Intermediate

Corrosion inhibitor for clean diverting acid, and preparation method thereof

COMPOUND COMPRISING PHENYL PYRIDINE UNITS

ELECTRON TRANSPORTING MATERIAL AND ORGANIC ELECTROLUMINESCENT DEVICE USING SAME

DRIER COMPOSITION AND USE THEREOF

Способ получения N-(4-хлорбензил)пиридин-2-амина

Изобретение относится способу получения N-(4-хлорбензил)пиридин-2-амина (I) из 4-хлорбензальдегида (II) и 2-аминопиридина (III) путем восстановительного аминирования, который осуществляют взаимодействием соединений (II) и (III) в присутствии кислотного катализатора, в качестве которого используют органическую или неорганическую кислоту, в кипящем азеотропообразующем растворителе, в качестве которого используют ароматический или алифатический углеводород, с одновременной азеотропной отгонкой воды до отделения ее теоретического количества, удаляют азеотропообразующий растворитель, полученный остаток растворяют в алифатическом спирте C-Cи восстанавливают борогидридом натрия при нагревании и выделяют целевой продукт (I) путем удаления из реакционной смеси алифатического спирта, обработки полученной массы водой, фильтрования осадка целевого продукта и его высушивания. Технический результат - однореакторный способ синтеза N-(4-хлорбензил)пиридин-2-амина из коммерчески доступных 4-хлорбензальдегида ...

Patent RU2016138800A3

`”ВУ“” 2016138800`” АЗ Дата публикации: 19.10.2018 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 2016138800/04(061850) 20.04.2015 РСТ/ЕР2015/058493 20.04.2015 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. 14165418.6 22.04.2014 ЕР Название изобретения (полезной модели): [Х] - как заявлено; [ ] - уточненное (см. Примечания) НОВЫЙ СПОСОБ ПОЛУЧЕНИЯ ПРОИЗВОДНЫХ ТРИАЗИНА, ПИРИМИДИНА И ПИРИДИНА Заявитель: УНИВЕРСИТЕТ БАЗЕЛЬ, СН, ПИКУР ТЕРАПЬЮТИКС АГ, СН 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) (070 213/127 (2006.01) (070 213/53 (2006.01) Аб/1К 31/5377 (2006.01) 5. ОБЛАСТЬ ПОИСКА 5.1 Проверенный минимум документации РСТ (указывается индексами МПК) С07О 213/127, СО7О 213/53, АбТК 31/5377 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): Езрасепев, Соозе, Соое эспо]аг, Раеагсп, Кеахуз 6 ДОКУМЕНТЫ, ОТНОСЯЩИЕСЯ К ПРЕДМЕТУ ПОИСКА Кате- Наименование документа с указанием (где ...

Method for preparing 2,2'-dipyridine and derivatives thereof

Disclosed is a method for preparing 2,2'-dipyridine and derivatives thereof. The method comprises: using pyridine represented by formula I or a derivative thereof as a raw material to generate 2,2'-dipyridine represented by formula II by performing dehydrogenative coupling under the action of a supported catalyst in the presence of additives, wherein R is H, C1-C2 alkyl, Cl, or Br. The method of the present invention features wide adaptability to raw materials, high atomic utilization rate, high catalyst activity, long service life, and fewer by-products.

N ortho substituted nitrogen-containing heterocyclic compound and procss for preparing aminal iron (II) complexes thereof

Provided are a N ortho acyl substituted nitrogen-containing heterocyclic compound and a process for preparing aminal iron (II) complexes thereof, and use of the complexes obtained by the process in an olefin oligomerization catalyst. The N ortho acyl substituted nitrogen-containing heterocyclic compound in the present invention is for example a 2-acyl-1,10-phenanthroline or a 2,6-diacetyl pyridine as shown in the formula b; the N ortho acyl substituted nitrogen-containing heterocyclic compound in the present invention is produced by a reaction of a precursor thereof in a substituted or unsubstituted nitrobenzene. Preferably the precursor shown in formula I in the present invention is produced by reacting the 1,10-phenanthroline with a trialkyl aluminum, or a halogenoalkyl aluminum RnAlXm, or a substituted or unsubstituted benzyl lithium Ph'CH2Li, followed by hydrolysis. The preparation method provided in the present invention has few synthetic steps, an easy process, a low toxic effect, ...

N ortho substituted nitrogen-containing heterocyclic compound and procss for preparing aminal iron (II) complexes thereof

Catalyst for producing a substituted or unsubstituted pyridine

Process of manufacture of a compound for inhibiting the activity of shp2

The invention relates to a method for the manufacture of a compound of Formula I as mentioned above, or a pharmaceutically acceptable salt, acid co-crystal, hydrate or other solvate thereof, said method comprising reacting a compound of the formula II with a compound of the formula III according to the following reaction scheme: wherein A, LG, n and m are as defined in the Summary of the Invention.

Drier composition and use thereof

The invention relates to a drier composition for an autoxidizable alkyd based coating composition, comprising: a) at least one Fe complex comprising Fe and at least one nitrogen donor ligand, wherein said at least nitrogen donor ligand is selected from the group comprising tridentate, tetradentate, pentadentate and hexadentate nitrogen donor ligands; b) at least one metal salt of a carboxylic acid, wherein the metal is selected from the group comprising: Mn, Ce, V, and Cu, preferably Mn; and c) at least one ligand comprising at least one moiety selected from the group comprising 1,4,7-tri-azacyclononanyl, 2,2'-bipyridyl, 1,10-phenantrolinyl, imidazolyl, pyrazolyl, porphyrinyl, aliphatic, cycloaliphatic, and aromatic amines. The present invention also relates to coating composition comprising the drier composition, and the uses thereof.

MORPHINE-6-GLUCURONIDE SYNTHESIS

The invention provides a novel method for synthesising M6G, and intermediates therefor. In order to synthesise M6G the major problem to overcome is to obtain the glycoside linkage with very high .beta.-selectivity since prior methods produce the .alpha.-anomer. The invention provides a method for the preferential synthesis of the .beta.-anomer of M6G which includes the step shown in Scheme 6: wherein use of DMAP is optional.

비스 제4급 암모늄염의 제조법 및 신규 중간체

... 본 발명은 효율적으로 비스 제4급 암모늄염을 제조하는 방법 및 신규한 합성중간체를 제공하는 것이다. 본 발명은 일반식 [1] (식 중, 두 개의 R1및 T의 정의는 청구항 1 기재와 같다.)로 표시되는 디술폰산에스테르와 일반식 [2] (식 중, R3~R5의 정의는 청구항 1 기재와 같다.)로 표시되는 제3급 아민을 반응시키는 것을 특징으로 하는, 일반식 [3] 으로 표시되는 비스 제4급 암모늄염의 제조법, 및 일반식 [1'] (식 중, 두 개의 R16은 각각 독립하여, 할로겐원자 또는 탄소수 1~3의 플루오로알킬기를 나타내고, 두 개의 m은 1~5의 정수를 나타낸다.)로 표시되는 디술폰산에스테르의 발명이다.

A METHOD FOR MANUFACTURING ASYMMETRIC ANTHRACENE DERIVATIVES AND APPLICATION FOR OLED DEVICE USING THE SAME

본 발명은 비대칭성 안트라센 유도체의 신규 제조방법에 관한 것이다. 보다 구체적으로는 2번 탄소가 알킬기, 시클로알킬기, 헤테로시클로알킬기, 아릴기, 또는 헤테로 아릴기로 치환되어 있으면서, 9번 및 10번 탄소가 각각 아릴기 또는 헤테로 아릴기로 치환된 안트라센 유도체를 높은 수율로 제조할 수 있는 방법에 관한 것이다.

Organic electroluminescent device

The present invention relates to an organic electroluminescent device comprising an anode, a cathode and organic layers, the said organic layers are a hole injection layer, a hole transport layer, an electron injection layer, an electron transport layer, a light-emitting layer which comprises at least one or more layers of the light-emitting layer; The said light-emitting layer is a host-guest doping system consisting of host materials and guest materials, the emitting region of the said light-emitting layer is 490-750 nm, the said host materials are a compound having the structure of formula (I), the said organic electroluminescent device emits red light or green light, and it has advantages of good electroluminescent luminous efficiency, excellent color purity and a long service life. Formula (I).

СПОСОБ ПОЛУЧЕНИЯ 4-(ЦИКЛОПРОПИЛМЕТОКСИ)-N-(3,5-ДИХЛОР-1-ОКСИДО-4-ПИРИДИЛ)-5-МЕТОКСИПИРИДИН-2-КАРБОКСАМИДА

FIELD: pharmacology. SUBSTANCE: invention relates to a method for preparation of formula 4-(cyclopropylmethoxy)-N-(3,5-dichloro-1-oxide-4-pyridyl)-5-methoxypyridine-2 carboxamide compound in the basic or hydrated form, or in the form of pharmaceutically acceptable salts, as well as certain new synthetic intermediates useful in this production method. EFFECT: improved production method. 12 cl, 5 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 635 094 C2 (51) МПК C07D 213/89 (2006.01) C07D 213/127 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (21)(22) Заявка: 2015125472, 28.11.2013 (24) Дата начала отсчета срока действия патента: 28.11.2013 Дата регистрации: (72) Автор(ы): КАЗИМИР Жан-Поль (FR), РОССЕ Ги (FR), ВЕРЕ Кристиан (FR) Приоритет(ы): (30) Конвенционный приоритет: R U (73) Патентообладатель(и): САНОФИ (FR) 09.11.2017 (56) Список документов, цитированных в отчете о поиске: EA 15355 B1, 30.06.2011. 28.11.2012 FR 1261351 WO2004005258 A1, 15.01.2004. WO 1996031476 A1, 10.10.1996. WO 2002069905 A2, 12.09.2002. 2 6 3 5 0 9 4 (43) Дата публикации заявки: 11.01.2017 Бюл. № 2 (45) Опубликовано: 09.11.2017 Бюл. № 31 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 29.06.2015 (86) Заявка PCT: EP 2013/074970 (28.11.2013) (87) Публикация заявки PCT: Адрес для переписки: 129090, Москва, ул. Б. Спасская, 25, стр. 3, ООО "Юридическая фирма Городисский и Партнеры" (54) СПОСОБ ПОЛУЧЕНИЯ 4-(ЦИКЛОПРОПИЛМЕТОКСИ)-N-(3,5-ДИХЛОР-1-ОКСИДО-4ПИРИДИЛ)-5-МЕТОКСИПИРИДИН-2-КАРБОКСАМИДА (57) Реферат: Изобретение относится к способу получения соединения 4-(циклопропилметокси)-N-(3,5дихлор-1-оксидо-4-пиридил)-5-метоксипиридин2-карбоксамида формулы (1) R U 2 6 3 5 0 9 4 C 2 C 2 WO 2014/083106 (05.06.2014) , в основной или гидратной форме, или в форме фармацевтически приемлемых солей, а также некоторых новых синтетических промежуточных Стр.: 1 соединений, полезных в этом способе получения. 6 н. и 6 з.п. ф-лы, 5 пр. R U R U 2 6 3 5 0 ...

СПОСОБ ПОЛУЧЕНИЯ ПРЯМОГО ИНГИБИТОРА ФАКТОРА Ха

Изобретение относится к промышленному способу получения соединения формулы Iа,который включает стадии а) взаимодействия 5-метилантраниловой кислоты и 2-амино-5-хлорпиридина с получением 2-амино-N-(5-хлорпиридин-2-ил)-5-метилбензамида; б) взаимодействия 2-амино-N-(5-хлорпиридин-2-ил)-5-метилбензамида с 4-[(трет-бутоксикарбонил)-N-метил]аминобензойной кислотой; в) удаления трет-бутоксикарбонил-защитной группы у продукта реакции стадии (б) с получением N-(5-хлорпиридин-2-ил)-5-метил-2-(4-(метиламино)бензамидо)бензамида; г) взаимодействия N-(5-хлорпиридин-2-ил)-5-метил-2-(4-(метиламино)бензамидо)бензамида с хлорангидридом имидоуксусной кислоты с получением соединения формулы Iа. Полученные соединения могут быть использованы как эффективный и селективный ингибитор фактора Ха для контроля свертываемости крови у человека и других млекопитающих, а также для лечения заболеваний, связанных со свертываемостью крови. 5 з.п. ф-лы.

НОВЫЙ СПОСОБ ПОЛУЧЕНИЯ ПРОИЗВОДНЫХ ТРИАЗИНА, ПИРИМИДИНА И ПИРИДИНА

Соли (5-гидрокси-3,4-бис(гидроксиметил)-6-метилпиридин-2-ил)метансульфокислоты и способ их получения

Изобретение относится к солям (5-гидрокси-3,4-бис(гидроксиметил)-6-метилпиридин-2-ил)метансульфокислоты общей формулы I: и способу их получения. Заявленный способ получения (5-гидрокси-3,4-бис(гидроксиметил)-6-метилпиридин-2-ил)метансульфокислоты отличается от известных аналогов меньшим числом стадий, более высоким выходом, применением более дешевых и при этом менее токсичных реагентов и растворителей, меньшим количеством отходов и их меньшей токсичностью. Заявленный способ очистки позволяет получить высокочистую (5-гидрокси-3,4-бис(гидроксиметил)-6-метилпиридин-2-ил)метансульфокислоту с содержанием примесей менее 0,1%. Заявляемые соли I-2 – I-13 синтезируются из (5-гидрокси-3,4-бис(гидроксиметил)-6-метилпиридин-2-ил)метансульфокислоты в одну стадию путем простой реакции нейтрализации и обладают существенно лучшей растворимостью в воде по сравнению с исходной кислотой. 2 н.п. ф-лы, 4 ил., 57 пр.

Complexes

The invention relates to a palladium (II) complex of formula (2): wherein R18 and R19 are independently selected from Me, -Et, -nPr, -iPr, -nBu, -iBu, cyclohexyl or cycloheptyl; R12 is an organic group having 1-20 carbon atoms; R20, R21, R22, R23 and R24 are independently H or organic groups having 1-20 carbon atoms; or one or both of R20/R21 or R22/R23 may form a ring; m is 0, 1,2,3,4 or 5; X is a coordinating anionic ligand. Preferably, R18 and R19 are both cyclohexyl; R20 and R21 are both H; R22, R23 and R24 are all phenyl; X is chloro; m is 0. The invention also provides a process for the preparation of the complexes, and their use in carbon-carbon and carbon-heteroatom coupling reactions.

Catalyst for biaryl production

A method of producing a biaryl compound from an aromatic/heteroaromatic substrate using a coupling catalyst; wherein the catalyst comprises Ni on an alumina support; wherein the content of Ni is 10-30 wt% based on the total weight of catalyst; and wherein the catalyst comprises a promoter metal selected from (i) a Group 1 metal in an amount of 0.5-5.5 wt% based on the total weight of catalyst; or (ii) a Group 2 metal in an amount of 0.5-10 wt% based on the total weight of catalyst. In another aspect, the per se catalyst used in the method, wherein the catalyst is in the form of an extrudate and is free from a metal salt or metal oxide cocatalyst. In yet another aspect, a method of manufacturing said catalyst, comprising the steps of: (i) providing a solution comprising a nickel salt and a solution comprising a promoter metal salt; (ii) carrying out incipient wetness impregnation of an extruded alumina support with the solution(s) from step (i); (iii) drying the product of step (ii); (iv ...

Process for the preparation of ionic liquids based on the triflimide anion

Die Erfindung betrifft ein Verfahren zur Herstellung von ionischen Flüssigkeiten auf Basis des Bistriflimid-Anions, wobei in einer ersten Stufe ein primäres aliphatisches Amin R-NH2 mit Trifluormethansulfonsäureanhydrid Tf20 zum entsprechenden N-alky­ lierten Trifluormethansulfonsäureimid R-NTf2 umgesetzt wird, das in einer zweiten Stu­ fe mit einem Nukleophil Nu zu einer ionischen Flüssigkeit, bestehend aus dem ent­ sprechenden alkylierten Nukleophil R-Nu+ als Kation und dem Bistriflimid-Anion Tf2N­ weiter umgesetzt wird: Tf20 Nu ----3)11o R-NTf2 ------'3)11o R-Nu+ - NTf2 dadurch gekennzeichnet, dass a) in der ersten Stufe ein in einem organischen Lösungsmittel gelöstes Alkylamin mit zumindest 3 Kohlenstoffatomen eingesetzt wird; b) in der zweiten Stufe ein Stickstoff-Heterozyklus oder eine Phosphorverbindung als Nukleophil eingesetzt wird; und c) beide Stufen in einem kontinuierlichen Fluss durchgeführt werden.

Method of preparing benzy 4-amino-3-chloro-5-fluoro-6-(4-chloro-2-fluoro-3-methoxyphenyl)picolinate

A method of preparing benzyl 4-amino-3-chloro-5-fluoro-6-(4-chloro-2-fluoro-3-methoxyphenyl)picolinate (I) from benzyl 4,5-difluoro-6-(4-chloro-2-fluoro-3-methoxyphenyl)picolinate (II) is described. The method includes the use of amination and chlorination process steps to provide the compound of Formula I.

2-(2,4-DIFLUOROPHENYL)-1,1-DIFLUORO-1-(5-SUBSTITUTED-PYRIDIN-2-YL)-3-(1H-TETRAZOL-1-YL)PROPAN-2-OLS AND PROCESES FOR THEIR PREPARATION

Provided herein are 2-(2,4-difluorophenyl)-1,1-difluoro-1-(5-substituted-pyridin-2- yl)-3-(1H-tetrazol-1-yl)propan-2-ols and processes for their preparation.

PROCESS FOR PREPARING 4-(CYCLOPROPYLMETHOXY)-N-(3,5-DICHLORO-1-OXIDO-4-PYRIDYL)-5-METHOXYPYRIDINE-2-CARBOXAMIDE

The present invention relates to a novel process for preparing the compound 4-(cyclopropylmethoxy)-N-(3,5-dichloro-l-oxido-4-pyridyl)-5-methoxypyridine-2-carboxamide of formula (1), in base or hydrate form or in the form of pharmaceutically acceptable salts, and also to several novel synthetic intermediates that are useful in this preparation process.

PROCESS FOR PREPARING ATAZANAVIR BISULFATE AND NOVEL FORMS

A process is provided for preparing the HIV protease inhibitor atazanavir bisulfate wherein a solution of atazanavir free base is reacted with concentrated sulfuric acid in an amount to react with less than about 15% by weight of the free base, seeds of Form A crystals of atazanavir bisulfate are added to the reaction mixture, and as crystals of the bisulfate form, additional concentrated sulfuric acid is added in multiple stages at increasing rates according to a cubic equation, to effect formation of Form A crystals of atazanavir bisulfate. A process is also provided for preparing atazanavir bisulfate as Pattern C material. A novel form of atazanavir bisulfate is also provided which is Form E3 which is a highly crystalline triethanolate solvate of the bisulfate salt from ethanol.

Process for preparing nicotinic acid and catalyst used in the method

The present invention relates to a process for preparing nicotinic acid, which comprises directly subjecting a mixture of 3-methylpyridine, oxygen, and water to a gas-phase oxidation in the presence of a catalyst consisting of vanadium oxide (V2O5) and transition metal oxide both of which are supported on a supporter, to give the nicotinic acid, wherein crystal size of the catalyst on the surface of the carrier is controlled in a range of from 40 to 200 nm through use of transition metal oxide. The present invention further relates to a catalyst used in the gas-phase oxidation. In the method according to the present invention, the nicotinic acid can be obtained in a higher convertibility and a higher selectivity by using a lower content of vanadium oxide. Therefore, the manufacturing cost can be reduced.

COMPOUND COMPRISING PHENYL PYRIDINE UNITS

Organic compounds of formula I may be used in optoelectronic devices Fornula (I) wherein R 1 is, independently at each occurrence, a C 1 -C 20 aliphatic radical, a C 3 -C 20 aromatic radical, or a C 3 -C 20 cycloaliphatic radical; R 2 is, independently at each occurrence, a C 1 -C 20 aliphatic radical, a C 3 -C 20 aromatic radical, or a C 3 -C 20 cycloaliphatic radical; a is, independently at each occurrence, an integer ranging from 0-4; b is, independently at each occurrence, an integer ranging from 0-3; Ar 1 is a direct bond or heteroaryl, aryl, or alkyl or cycloalkyl; Ar 2 is heteroaryl, aryl, or alkyl or cycloalkyl; c is 0, 1 or 2; and n is an integer ranging from 2-4.

RUTHENIUM-BASED COMPLEX CATALYSTS

The present invention provides novel Ruthenium-based transition metal complex catalysts comprising specific ligands, their preparation and their use in hydrogenation processes. Such complex catalysts are inexpensive, thermally robust, and olefin selective.

PROCESS FOR MAKING ORGANIC COMPOUNDS AND THE ORGANIC COMPOUNDS MADE THEREFROM

An organic compound of formula (E) is made from a process comprising. reacting a compound of formula (A) and a compound of formula (B) to form a compound of formula (C); and reacting one of the compound of formula (C) and the compound of formula (D) with a first boron esterification reagent to generate a boronic acid or a boronic ester to react with another of the compound of formula (C) and the compound of formula (D) to form a compound of formula (E).

PROCESS FOR PREPARING CARBOXAMIDE PYRIDINE DERIVATIVES USED AS INTERMEDIATES IN THE SYNTHESIS OF NK-1 RECEPTOR ANTAGONISTS

COBALT COMPLEXES, PROCESS FOR PREPARATION AND USE THEREOF

КОМПЛЕКСЫ

FIELD: chemistry.SUBSTANCE: present invention relates to a complex of palladium (II) of formula (1) and a complex of palladium (II) of formula (2).,.Value of groups R, R, R, R, R, R, R, R, R, R, R, R, R, R, R, R, R, Rand R, m, E and X is given in the claim. Also disclosed are a method of producing a complex of formula (1) or complex of formula (2), a method of carrying out a carbon-carbon combination reaction and a carbon-heteroatom combination reaction using a complex of formula (1) or a complex of formula (2), use of a complex of formula (1) or a complex of formula (2) as a catalyst for reactions of combining carbon-carbon and carbon-heteroatom.EFFECT: disclosed complexes are highly active catalysts of carbon-carbon and carbon-heteroatom combination reactions.29 cl, 6 dwg, 9 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) (19) RU (51) МПК C07F 15/00 C07F 19/00 B01J 31/22 B01J 31/24 C07B 37/02 C07B 37/04 C07B 43/04 (11) (13) 2 682 680 C2 (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (52) СПК C07B 37/04 (2019.02); C07B 43/04 (2019.02); C07C 17/32 (2019.02); C07C 45/68 (2019.02); C07D 213/127 (2019.02); C07D 213/24 (2019.02); C07D 213/50 (2019.02); C07D 213/56 (2019.02); C07D 215/38 (2019.02); C07D 295/096 (2019.02); C07D 307/46 (2019.02); C07D 401/06 (2019.02); C07D 403/04 (2019.02); C07D 405/04 (2019.02); C07D 409/04 (2019.02); C07D 471/04 (2019.02); C07F 15/006 (2019.02) (24) Дата начала отсчета срока действия патента: 20.03.2015 Дата регистрации: 20.03.2019 Приоритет(ы): (30) Конвенционный приоритет: (43) Дата публикации заявки: 18.07.2018 Бюл. № 20 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 12.01.2017 (86) Заявка PCT: GB 2015/050835 (20.03.2015) (87) Публикация заявки PCT: WO 2015/189554 (17.12.2015) Адрес для переписки: 129090, Москва, ул. Б. Спасская, 25, стр. 3, ООО "Юридическая фирма Городисский и Партнеры" (54) КОМПЛЕКСЫ (57) Реферат: Настоящее ...

НОВЫЙ ПАЛЛАДИЕВЫЙ КАТАЛИЗАТОР, СПОСОБ ЕГО ПОЛУЧЕНИЯ И ЕГО ПРИМЕНЕНИЕ

... 1. Способ получения комплекса три-[3,5-бис(трифторметил)-фенил]-фосфина и палладия (0), характеризующийся тем, что осуществляют реакцию соли палладия (II) с три-[3,5-бис(трифторметил)-фенил]-фосфином, и палладий (II) восстанавливают до палладия (0) в полученной в результате комплексной соли.2. Способ по п.1, характеризующийся тем, что реакцию соли палладия (II) осуществляют по меньшей мере с четырехкратным молярным избытком три-[3,5-бис(трифторметил)-фенил]-фосфина.3. Способ по п.1, характеризующийся тем, что реакцию соли палладия (II) с три-[3,5-бис(трифторметил)-фенил]-фосфином и восстановление палладия (II) до палладия (0) осуществляют в одном реакционном сосуде без выделения промежуточных соединений.4. Способ по п.1, отличающийся тем, что в качестве соли палладия (II) применяют дихлорид палладия.5. Способ по п.1, отличающийся тем, что восстановление проводят гидразин-гидратом.6. Катализатор, представляющий собой комплекс три-[3,5-бис(трифторметил)-фенил]-фосфина и палладия (0), полученный ...

КОМПЛЕКСЫ

РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2017 100 520 A (51) МПК C07D 215/38 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2017100520, 20.03.2015 (71) Заявитель(и): ДЖОНСОН МЭТТИ ПАБЛИК ЛИМИТЕД КОМПАНИ (GB) Приоритет(ы): (30) Конвенционный приоритет: 12.06.2014 US 62/011,168 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 12.01.2017 R U (43) Дата публикации заявки: 18.07.2018 Бюл. № 20 (72) Автор(ы): КОЛАКОТ Томас (US), ЧОУ Жуйшань (US), ДЖОН ДИЭНДЖЕЛИС Эндрю (US) (86) Заявка PCT: (87) Публикация заявки PCT: WO 2015/189554 (17.12.2015) (54) КОМПЛЕКСЫ (57) Формула изобретения 1. Комплекс палладия (II) формулы (1): R U A 2 0 1 7 1 0 0 5 2 0 A Адрес для переписки: 129090, Москва, ул. Б. Спасская, 25, стр. 3, ООО "Юридическая фирма Городисский и Партнеры" 2 0 1 7 1 0 0 5 2 0 GB 2015/050835 (20.03.2015) в котором: R1 и R2 независимо представляют собой органические группы, имеющие 1-20 атомов углерода, или R1 и R2 соединены с образованием кольцевой структуры с Е; Стр.: 1 A 2 0 1 7 1 0 0 5 2 0 A R U 2 0 1 7 1 0 0 5 2 0 Стр.: 2 R U R3, R4, R5, R6, R7, R8, R9, R10 и R11 независимо представляют собой -Н или органические группы, имеющие 1-20 атомов углерода; или R1/R3 или R2/R3 образует кольцевую структуру с атомами, к которым они присоединены, и в этом случае R4/R5, R5/R6, R7/R8, R8/R9, R9/R10 или R10/R11 могут независимо образовывать кольцевую структуру с атомами углерода, к которым они присоединены, или R1, R2, R4, R5, R6, R7, R8, R9, R10 и R11 являются такими, как определено выше; R12 представляет собой органическую группу, имеющую 1-20 атомов углерода; m равно 0, 1, 2, 3, 4 или 5; Е представляет собой P или As; и Х представляет собой координирующий анионный лиганд; при условии, что палладиевый комплекс формулы (1) не представляет собой (πкротил)PdCl(дициклогексилфосфино-2-бифенил). 2. Комплекс палладия (II) по п.1, в котором Е представляет собой Р. 3. Комплекс палладия (II) по п.2, в котором R1 и ...

СПОСОБ ПОЛУЧЕНИЯ 4-(ЦИКЛОПРОПИЛМЕТОКСИ)-N-(3,5-ДИХЛОР-1-ОКСИДО-4-ПИРИДИЛ)-5-МЕТОКСИПИРИДИН-2-КАРБОКСАМИДА

РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2015 125 472 A (51) МПК C07D 401/12 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2015125472, 28.11.2013 (71) Заявитель(и): САНОФИ (FR) Приоритет(ы): (30) Конвенционный приоритет: 28.11.2012 FR 1261351 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 29.06.2015 R U (43) Дата публикации заявки: 11.01.2017 Бюл. № 02 (72) Автор(ы): КАЗИМИР Жан-Поль (FR), РОССЕ Ги (FR), ВЕРЕ Кристиан (FR) (86) Заявка PCT: (87) Публикация заявки PCT: WO 2014/083106 (05.06.2014) (54) СПОСОБ ПОЛУЧЕНИЯ 4-(ЦИКЛОПРОПИЛМЕТОКСИ)-N-(3,5-ДИХЛОР-1-ОКСИДО-4ПИРИДИЛ)-5-МЕТОКСИПИРИДИН-2-КАРБОКСАМИДА R U (57) Формула изобретения 1. Способ получения 4-(циклопропилметокси)-N-(3,5-дихлор-1-оксидо-4-пиридил)5-метоксипиридин-2-карбоксамида, в основной или гидратной форме, или в форме фармацевтически приемлемых солей, приведенной ниже формулы 1: Стр.: 1 A 2 0 1 5 1 2 5 4 7 2 A Адрес для переписки: 129090, Москва, ул. Б. Спасская, 25, стр. 3, ООО "Юридическая фирма Городисский и Партнеры" 2 0 1 5 1 2 5 4 7 2 EP 2013/074970 (28.11.2013) , R U 2 0 1 5 1 2 5 4 7 2 , R U стадию b): реакцию окисления соединения 4, полученного на стадии c), согласно приведенной ниже схеме: Стр.: 2 A 2 0 1 5 1 2 5 4 7 2 A отличающийся тем, что включает: стадию c): взаимодействие соединения 2-гидроксиметил-5-метокси-4-пирид-(1H)-она формулы 5 с метилциклопропановым производным и основанием в полярном апротонном растворителе, согласно приведенной ниже схеме: , R U стадию a) реакцию сочетания соединения 2, полученного на стадии b), с N-оксидом 3,5-дихлораминопиридина (соединение 3) или его N-Boc-производным, согласно приведенной ниже схеме: R U 2 0 1 5 1 2 5 4 7 2 A Стр.: 3 A 2. Способ получения 4-(циклопропилметокси)-N-(3,5-дихлор-1-оксидо-4-пиридил)5-метоксипиридин-2-карбоксамида по п. 1, отличающийся тем, что метилциклопропановое производное представляет собой бромид метилциклопропана, основание представляет собой ...

Verfahren zur Herstellung von Vinyl-verbindungen der Pyridin- und Chinolinreihe

Verfahren zur Herstellung von aromatischer Verbindung

Verfahren zur Herstellung einer aromatischen Verbindung der folgenden Formel (3), umfassend Umsetzen einer Verbindung der folgenden Formel (1) mit einer Olefinverbindung der folgenden Formel (2) in der Gegenwart eines Übergangsmetallkomplexes: (wobei ein Ring Ar1 einen aromatischen Kohlenwasserstoffring oder aromatischen heterocyclischen Ring darstellt, ein Ring Ar2 einen heterocyclischen Ring, enthaltend Xi und N*, darstellt und das X1 ein Stickstoffatom oder Kohlenstoffatom darstellt und das N* ein Stickstoffatom darstellt, bindend über eine Doppelbindung zu einem von zwei benachbarten Atomen in dem Ring Ar2. Der Ring Ar1 und/oder der Ring Ar2 können gegebenenfalls einen Rest, ausgewählt aus einem Alkylrest mit 1 bis 10 Kohlenstoffatomen, einem Alkoxyrest mit 1 bis 10 Kohlenstoffatomen, einem Arylrest mit 6 bis 18 Kohlenstoffatomen und einem Aryloxyrest mit 6 bis 10 Kohlenstoffatomen, aufweisen. Der Ring Ar1 und der Ring Ar2 können ferner direkt oder über einen zweiwertigen Rest verbunden ...

Pi-allyl palladium complexes comprising coordinating anionic ligands and their use in coupling reactions

Process for dehydrating organic liquids and apparatus therefor

... Organic liquids are dehydrated by subjecting their vapours to the action of anhydrous calcium sulphate obtained by heating either plaster of Paris or mineral gypsum to 160-180 DEG C. or higher, the anhydrous sulphate being used in such quantity as to be converted into the semihydrate. The process is particularly applicable to liquids which have boiling points close to that of water, or form azeotropic mixtures with water, or decompose when heated with water. Examples of liquids are acetal, acetaldehyde, aldehyde - ammonia, formic acid, amylene hydrate, crotonaldehyde, acetic acid, isobutyl alcohol, propyl and iso-propyl alcohol, ethyl alcohol, piperidine, pyridine and its homologues, chloral, chlorhydrin, chloracetone, cyclohexanol. In one form of apparatus the sulphate is arranged in layers in a tower and is periodically regenerated without removal, air at 200 DEG C. being passed through alternately with the vapours of the pyridine to be dehydrated ...

MANUFACTURING PROCESS FOR CARBOXAMID PYRIDINDERIVATE ONES AS INTERMEDIATE PRODUCTS WITH THE SYNTHESIS OF NK-1-REZEPTOR-ANTAGONISTEN

Process for the preparation of ionic liquids based on the triflimide anion

Die Erfindung betrifft ein Verfahren zur Herstellung von ionischen Flüssigkeiten auf Basis des Bistriflimid-Anions, wobei in einer ersten Stufe ein primäres aliphatisches Amin R-NH2 mit Trifluormethansulfonsäureanhydrid Tf20 zum entsprechenden N-alkylierten Trifluormethansulfonsäureimid R-NTf2 umgesetzt wird, das in einer zweiten Stufe mit einem Nukleophil Nu zu einer ionischen Flüssigkeit, bestehend aus dem entsprechenden alkylierten Nukleophil R-Nu+ als Kation und dem Bistriflimid-Anion Tf2Nweiter umgesetzt wird: dadurch gekennzeichnet, dass a) in der ersten Stufe ein in einem organischen Lösungsmittel gelöstes Alkylamin mit zumindest 3 Kohlenstoffatomen eingesetzt wird; b) in der zweiten Stufe ein Stickstoff-Heterozyklus oder eine Phosphorverbindung als Nukleophil eingesetzt wird; und c) beide Stufen in einem kontinuierlichen Fluss durchgeführt werden.

PROCESS FOR PREPARING CARBOXAMIDE PYRIDINE DERIVATIVES USED AS INTERMEDIATES IN THE SYNTHESIS OF NK-1 RECEPTOR ANTAGONISTS

NOVEL MANUFACTURING PROCESS FOR TRIAZINE, PYRIMIDINE AND PYRIDINE DERIVATIVES

The invention relates to a method of manufacturing triazine, pyrimidine and pyridine derivatives of formula (I), wherein U, V, W and Z are nitrogen or carbon atoms, whereby at least one of U, V and W is nitrogen, and the other substituents are defined as in the specification, by condensing a corresponding halo-triazine, pyrimidine or pyridine in a type of Suzuki coupling with a pyridyl- or pyrimidinyl-borane, wherein the amino function is protected as a formamidine. The invention further relates to suitable intermediates and methods of manufacturing of such intermediates. Furthermore the invention relates to pure 5-(4,6-dimorpholino-1,3,5- triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine in solid form.

METAL OXIDE-SUPPORTED EARTH-ABUNDANT METAL CATALYSTS FOR HIGHLY EFFICIENT ORGANIC TRANSFORMATIONS

PROCESS FOR PRODUCTION OF BIS-QUATERNARY AMMONIUM SALT, AND NOVEL INTERMEDIATE

NOVEL MANUFACTURING PROCESS FOR TRIAZINE, PYRIMIDINE AND PYRIDINE DERIVATIVES

The invention relates to a method of manufacturing triazine, pyrimidine and pyridine derivatives of formula (I) 2. The method of claim 1 , wherein in the compound of formula (I){'sup': U', 'U, 'U is CRor N, wherein Ris hydrogen;'}{'sup': V', 'V, 'V is CRor N, wherein Ris hydrogen;'}{'sup': W', 'W, 'W is CRor N, wherein Ris hydrogen;'}{'sup': Z', 'Z, 'Z is CRor N, wherein Ris hydrogen;'}{'sup': '1', 'Ris morpholino;'}{'sup': '2', 'Ris trifluoromethyl;'}{'sup': '3', 'and Ris hydrogen.'}3. The method of claim 1 , wherein in the compound of formula (II){'sub': '2', 'YB represents a cyclic boronic ester;'}{'sup': '4', 'Ris hydrogen; and'}{'sup': 5', '6, 'Rand Rare methyl.'}4. The method of claim 1 , wherein the organic solvent is selected from the group consisting of tetrahydrofuran claim 1 , dioxane and toluene.5. The method of claim 1 , wherein the Pd phosphine catalyst is a mixture of triphenylphosphine and palladium(II) acetate or palladium dichloride.1115-. (canceled)16. The method of claim 1 , wherein{'sup': U', 'U, 'U is CRor N, wherein Ris hydrogen;'}{'sup': V', 'V, 'V is CRor N, wherein Ris hydrogen;'}{'sup': W', 'W, 'W is CRor N, wherein Ris hydrogen;'}{'sup': Z', 'Z, 'Z is CRor N, wherein Ris hydrogen;'}{'sup': '1', 'Ris halogen;'}{'sup': '2', 'Ris trifluoromethyl; and'}{'sup': '3', 'Ris hydrogen;'}and wherein further said resulting formamidine of formula s reacted morpholine prior to said its hydrolyzation.17. The method of claim 1 , wherein{'sup': U', 'U, 'U is CRor N, wherein Ris hydrogen;'}{'sup': V', 'V, 'V is CRor N, wherein Ris hydrogen;'}{'sup': W', 'W, 'W is CRor N, wherein Ris hydrogen;'}{'sup': Z', 'Z, 'Z is CRor N, wherein Ris hydrogen;'}{'sup': '1', 'Ris chlorine;'}{'sup': '2', 'Ris trifluoromethyl; and'}{'sup': '3', 'Ris hydrogen;'}and wherein further said resulting formamidine of formula s reacted with morpholine prior to said its hydrolyzation18. The method of claim 1 , wherein{'sup': Z', 'Z, 'U is N; V is N; W is N; Z is CR, wherein Ris ...

СПОСОБ ПОЛУЧЕНИЯ ПРЯМОГО ИНГИБИТОРА ФАКТОРА Ха

А 2016121496 ко РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) (11) = КО х (51) МПК С07О 213/00 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2016121496, 01.06.2016 (71) Заявитель(и): Закрытое акционерное общество "ФАРМА Приоритет(ы): " ВАМ" (КО) (22) Дата подачи заявки: 01.06.2016 , (72) Автор(ы): (43) Дата публикации заявки: 06.12.2017 Бюл. № 34 Балазовский Марк Борисович (ВП), Адрес для переписки: Игнатенко Олег Александрович (КП) 197101, Санкт-Петербург, а/я 128, "АРС- ПАТЕНТ", М.В. Хмара (54) СПОСОБ ПОЛУЧЕНИЯ ПРЯМОГО ИНГИБИТОРА ФАКТОРА Ха (57) Формула изобретения 1. Способ получения гидрохлорида М-(5-хлорпиридин-2-ил)-5-метил-2-(4-(М- метилацетимидамидо)бензамидо)бензамида формулы [Па С а при котором осуществляют: а) взаимодействие 5-метилантраниловой кислоты и 2-амино-5-хлорпиридина с получением 2-амино-М-(5-хлорпиридин-2-ил)-5-метилбензамида; 6) взаимодействие 2-амино-М-(5-хлорпиридин-2-ил)-5-метилбензамида с 4-[(трет- бутоксикарбонил)-М-метил|аминобензойной кислотой; Стр.: 1 па ЭбУгс+т9рОсС У А 2016121496 ко в) удаление трет-бутоксикарбонил-защитной группы у продукта реакции стадии (6) сполучением М-(5-хлорпиридин-2-ил)-5-метил-2-(4-(метиламино)бензамидо)бензамида: г) взаимодействие №-(5-хлорпиридин-2-ил)-5-метил-2-(4-(метиламино)бензамидо) бензамида с хлорангидридом имидоуксусной кислоты с получением соединения формулы Га. 2. Способ по п. 1, где удаление трет-бутоксикарбонил-защитной группы на стадии (в) осуществляют путем взаимодействия продукта реакции стадии (6) стрифторуксусной КИСЛОТОЙ. 3. Способ по п. 2, где на стадии (в) дополнительно проводят нейтрализацию трифторуксусной кислоты. 4. Способ по п. 3, где нейтрализацию проводят с использованием гидроксида калия или гидроксида натрия. 5. Способ по п. 4, где нейтрализацию проводят с использованием гидроксида натрия. 6. Способ по п. 1, где на стадии (г) применяют хлорангидрид имидоуксусной кислоты, который образуется ш зи из ацетонитрила, хлористого тионила и воды ...

Process for the preparation of vinyl-substituted pyridine and quinoline compounds

Vinyl-substituted pyridine and quinoline compounds are obtained by dehydrating corresponding pyridine and quinoline alcohols by introducing the alcohol with water into triethanolamine, glycerol or a polyglycol containing 0.1 to 5% by weight of a caustic alkali or acid-reacting compound, while heating to 180 DEG to 200 DEG C. to distil off the vinyl compound and water vapour. A solution of the alcohol in water may be poured into the solvent, injected below the surface of the solvent or sprayed on to the surface of the solvent, or the alcohol may be introduced simultaneously with steam into the solvent. In examples 2-vinylpyridine is obtained from 2-pyridine-ethanol, 4-vinylpyridine is obtained from 4-pyridine-ethanol, 2-methyl-6-vinylpyridine is obtained from 2-methyl-6-pyridine-ethanol, and 2-vinyl-quinoline is obtained from 2-quinoline-ethanol; the solvents used are triethanolamine containing sodium hydroxide, glycerol containing potassium bisulphate, glycerol containing monoammonium phosphate ...

Method for preparing 2,2'-dipyridine and derivatives thereof

Disclosed is a method for preparing 2,2'-dipyridine and derivatives thereof. The method comprises: using pyridine represented by formula I or a derivative thereof as a raw material to generate 2,2'-dipyridine represented by formula II by performing dehydrogenative coupling under the action of a supported catalyst in the presence of additives, wherein R is H, C1-C2 alkyl, Cl, or Br. The method of the present invention features wide adaptability to raw materials, high atomic utilization rate, high catalyst activity, long service life, and fewer by-products.

Morphine-6-glucuronide synthesis

PROCESS FOR FLUORINATING COMPOUNDS

Methods of preparing a fluorinated substrate by combining potassium fluoride, a quaternary ammonium salt, and a substrate substituted with at least one chloro, bromo, sulfonyl, or nitro group to thereby provide the fluorinated substrate are disclosed.

Preparation and application methods of flame retardant ionic liquid

Method for synthesizing cis-olefin by catalyzing decarboxylation coupling reaction of NHP ester and aryl-terminated alkyne with iridium

Condensed compound and organic light emitting diode comprising the same

novas aminopiridinas catiônicas, composição corantte compreendendo uma aminopiridina catiônica, processos para aquelas e suas utilizações.

N ORTHO ACYL SUBSTITUTED NITROGEN-CONTAINING HETEROCYCLIC COMPOUND AND PROCESS FOR PREPARING AMINAL IRON (II) COMPLEXES THEREOF

Provided are a N ortho acyl substituted nitrogen-containing heterocyclic compound and a process for preparing aminal iron (II) complexes thereof, and use of the complexes obtained by the process in an olefin oligomerization catalyst. The N ortho acyl substituted nitrogen-containing heterocyclic compound in the present invention is for example a 2-acyl-1,10-phenanthroline or a 2,6-diacetyl pyridine as shown in the formula b; the N ortho acyl substituted nitrogen-containing heterocyclic compound in the present invention is produced by a reaction of a precursor thereof in a substituted or unsubstituted nitrobenzene. Preferably the precursor shown in formula I in the present invention is produced by reacting the 1,10-phenanthroline with a trialkyl aluminum, or a halogenoalkyl aluminum RnAlXm, or a substituted or unsubstituted benzyl lithium Ph'CH2Li, followed by hydrolysis. The preparation method provided in the present invention has few synthetic steps, an easy process, a low toxic effect, ...

TRANSITION METAL-CATALYZED ALKYLATION OF C-H BONDS WITH ORGANOBORON REAGENTS

One aspect of the present invention relates to methods for functionalization of 2-arylpyridine and arylpyrazoles with organoboron reagents in the presence of a transition metal catalyst to furnish alkylated arylpyridines and arylpyrazoles via regioselective functionalization of sp2 -hybridized C-H bonds at a position ortho to the point of attachment of the pyridine or pyrazole ring to the aromatic nucleus, hi other embodiments, the present invention provides for alkylation of sp3-hybridized C-H bonds in alkylpyridines.

PROCESSES FOR PRODUCING AMINE COMPOUNDS

The present invention provides processes for producing amine-containing compounds such as diammonium salts and amino acid derivatives comprising the steps of subjecting a salt of an amine bearing an unsaturated group to a self-metathesis reaction with itself to produce a diammonium salt or to a cross-metathesis with a suitable α,β-unsaturated acid, ester or amide to form an amino acid salt or a derivative thereof. The salts produced by the metathesis reactions can then be subjected to hydrogenation to reduce the double bond which is formed in the metathesis reaction.

PROCESS FOR PRODUCTION OF AROMATIC COMPOUND

Disclosed is a process for production of an aromatic compound represented by the formula (3), wherein the process comprises reacting a compound represented by the formula (1) with an olefin compound represented by the formula (2) in the presence of a transition metal complex: (1) wherein the Ar1 ring represents an aromatic hydrocarbon ring or an aromatic heterocyclic ring; and the Ar2 ring represents a heterocyclic ring having X1 and N*, wherein X1 represents a nitrogen or carbon atom, and N* represents a nitrogen atom bound to one of two contiguous atoms in the Ar2 ring via a double bond; (2) wherein R1, R2, R3 and R4 independently represent a hydrogen atom, an alkyl group having 1 to 10 carbon atoms or an aryl group having 6 to 18 carbon atoms; and (3) wherein Ar1, Ar2, X1, N*, R1, R2 and R3 are as defined above.

Pi-allyl palladium complexes comprising coordinating anionic ligands, and their use in coupling reactions

Process for preparing atazanavir bisulfate and novel forms

A process for the palladium-catalyzed coupling of terminal alkynes with heteroaryl tosylates and heteroaryl benzenesulfonates

The present invention relates to a process for the regioselective synthesis of compounds of the formula (I), (I) wherein D, J and W have the meanings indicated in the claims. The present invention provides an efficient and general palladium-catalyzed coupling process of heteroaryl tosylates with terminal alkynes to a wide variety of substituted, multifunctional heteroaryl-1 -alkynes of the formula I useful for the production of pharmaceuticals, diagnostic agents, liquid crystals, polymers, herbicides, fungicidals, nematicidals, parasiticides, insecticides, acaricides and arthropodicides.

Morphine-6-glucuronide synthesis

Synthesis method of biaryl compounds

A N ortho-acyl substituted nitrogen-containing heterocyclic compound and its ketal amine gathers the iron method for preparing (II) complex

Process for preparing 4-(cyclopropylmethoxy)-N-(3,5-dichloro-1-oxido-4-pyridyl)-5-methoxypyridine-2-carboxamide

The present invention relates to a novel process for preparing the compound 4-(cyclopropylmethoxy)-N-(3,5-dichloro-l-oxido-4-pyridyl)-5-methoxypyridine-2-carboxamide of formula (1), in base or hydrate form or in the form of pharmaceutically acceptable salts, and also to several novel synthetic intermediates that are useful in this preparation process.

Method of preparing benzyl 4-amino-3-chloro-5-fluoro-6-(4-chloro-2-fluoro-3-methoxyphenyl)picolinate

A method of preparing benzyl 4-amino-3-chloro-5-fluoro-6-(4-chloro-2-fluoro-3-methoxyphenyl)picolinate (I) from benzyl 4,5-difluoro-6-(4-chloro-2-fluoro-3-methoxyphenyl)picolinate (II) is described. The method includes the use of amination and chlorination process steps to provide the compound of Formula I.

METHOD OF PREPARING BENZY 4-AMINO-3-CHLORO-5-FLUORO-6-(4-CHLORO-2-FLUORO-3-METHOXYPHENYL)PICOLINATE

A method of preparing benzyl 4-amino-3-chloro-5-fluoro-6-(4-chloro-2-fluoro-3-methoxyphenyl)picolinate (I) from benzyl 4,5-difluoro-6-(4-chloro-2-fluoro-3-methoxyphenyl)picolinate (II) is described. The method includes the use of amination and chlorination process steps to provide the compound of Formula I.

A PROCESS FOR PREPARATION OF E-ISOMER OF 1-(4-METHYLPHENYL)-1-(2-PYRIDYL)-3-PYRROLIDINO PROP-1-ENE AND ACID ADDITION SALTS THEREOF

A process for preparation of E-isomer of 1-(4-methylphenyl)-1-(2-pyridyl)-3-pyrrolidinoprop-1-ene of Formula-I, and acid addition salts thereof, said process comprising; dehydrating 1-(4-methylphenyl)-1-(2-pyridyl)-3-pyrrolidinopropan-1-ol of Formula III followed by adding a base solution to obtain a mixture of E and Z isomers of 1-(4-methylphenyl)-1-(2-pyridyl)-3-pyrrolidinoprop-1-ene, and washing said mixture of E and Z isomers of 1-(4-methylphenyl)-1-(2-pyridyl)-3-pyrrolidinoprop-1-ene with water to dissolve Z isomer and to obtain E-isomer of 1-(4-methylphenyl)-1-(2-pyridyl)-3-pyrrolidinoprop-1-ene of Formula I, which is substantially free from Z isomer.

Eutecticum of azilsartan and 4,4'-dipyridyl and preparation method of eutecticum

Electroluminescent device

Disclosed are electroluminescent devices that comprise organic layers that contain pyridine compounds. The pyridine compounds are suitable components of blue-emitting, durable, organo-electroluminescent layers. The electroluminescent devices may be employed for full color display panels in, for example, mobile phones, televisions and personal computer screens.

A ortho position alkylation method of organic compound containg pyridine

PREPARATION OF ASYMMETRIC ANTHRACENE DERIVATIVES AND ORGANIC ELECTROLUMINESCENT DEVICE USING SAME

The present invention relates to a novel method for preparing asymmetric anthracene derivatives. More particularly, the present invention relates to a method for preparing anthracene derivatives with a high yield rate in which number 2 carbon is substituted by an alkyl group, a cycloalkyl group, a heterocycloalkyl group, an aryl group or a heteroaryl group, and number 9 carbon and number 10 carbon are substituted by respective aryl groups or heteroaryl groups.

Compound for organic EL device and light-emitting device

A novel compound for an organic EL device is provided which has a structure represented by the general formula (1): ...

Process for preparing atazanavir bisulfate and novel forms

A novel form of atazanavir bisulfate is also provided which is Form E3 which is a highly crystalline triethanolate solvate of the bisulfate salt from ethanol.

A PROCESS FOR THE PALLADIUM-CATALYZED COUPLING OF TERMINAL ALKYNES WITH HETEROARYL TOSYLATES AND HETEROARYL BENZENESULFONATES

The present invention relates to a process for the regioselective synthesis of compounds of the formula (I), (I) wherein D, J and W have the meanings indicated in the claims. The present invention provides an efficient and general palladium-catalyzed coupling process of heteroaryl tosylates with terminal alkynes to a wide variety of substituted, multifunctional heteroaryl-1 -alkynes of the formula I useful for the production of pharmaceuticals, diagnostic agents, liquid crystals, polymers, herbicides, fungicidals, nematicidals, parasiticides, insecticides, acaricides and arthropodicides.

DRIER COMPOSITION AND USE THEREOF

The invention relates to a drier composition for an autoxidizable alkyd based coating composition, comprising: a) at least one Fe complex comprising Fe and at least one nitrogen donor ligand, wherein said at least nitrogen donor ligand is selected from the group comprising tridentate, tetradentate, pentadentate and hexadentate nitrogen donor ligands; b) at least one metal salt of a carboxylic acid, wherein the metal is selected from the group comprising: Mn, Ce, V, and Cu, preferably Mn; and c) at least one ligand comprising at least one moiety selected from the group comprising 1,4,7-tri-azacyclononanyl, 2,2'-bipyridyl, 1,10-phenantrolinyl, imidazolyl, pyrazolyl, porphyrinyl, aliphatic, cycloaliphatic, and aromatic amines. The present invention also relates to coating composition comprising the drier composition, and the uses thereof.

불균일 촉매작용에 의한 플루오로 알킬화 화합물의 제조방법

... 본 발명은 Cs2CO3 및 CsHCO3 의 존재 하에 알킬 할라이드 또는 플루오로, 클로로 및 플루오로클로로 알킬 할라이드에 의한 불균일 Pt/C-촉매작용 알킬화 또는 플루오로, 클로로 및 플루오로클로로 알킬화에 의하여, 알킬화 또는 플루오로, 클로로 및 플루오로클로로 알킬화 화합물을 제조하는 방법을 개시하고 있다.

Method for forming polyalkynyl-arenes

A method of coupling an aromatic compound having a two or more fluorosulfonate substituents to an alkyne is useful in the preparation of polyalkynyl-substituted arene compounds.

METHOD FOR PREPARATION OF ALKYLATED OR FLUORO, CHLORO AND FLUOROCHLORO ALKYLATED COMPOUNDS BY HETEROGENEOUS CATALYSIS

The invention discloses a method for preparation of alkylated or fluoro, chloro and fluorochloro alkylated compounds by a heterogeneous Pt/C-catalyzed alkylation or fluoro, chloro and fluorochloro alkylation with alkyl halides or with fluoro, chloro and fluorochloro alkyl halides in the presence of Cs2C03 or CsHC03.

Synthetic method of 4-methylpyridine quaternary ammonium salt

Compound having dual effects on 5-HT and application thereof in treatment of depression

Eutectic material with flexibility and optical driven shape change characteristic and preparation method thereof

NOVEL ORGANIC COMPOUND AND ORGANIC LIGHT-EMITTING DEVICE INCLUDING THE SAME

Ｎ ORTHO ACYL SUBSTITUTED NITROGEN-CONTAINING HETEROCYCLIC COMPOUND AND PROCESS FOR PREPARING AMINAL IRON （Ⅱ） COMPLEXES THEREOF

Novel cationic 4- aminoindoles, dye composition comprising a cationic 4-aminoindole, processes therefor and uses thereof

The present invention relates to a cationic aminopyridine of general formula (I), acid-addition salts thereof and solvates thereof: in which: R 1 is a linear or branched, saturated C 1 -C 20 alkyl radical, substituted and/or interrupted with a cationic radical. The present invention is also directed towards a process for synthesizing this cationic aminopyridine, compositions, uses, hair dyeing processes and devices using this cationic aminopyridine.

Highly Active Multidentate Catalysts for Efficient Alkyne Metathesis

The invention relates to highly active and selective catalysts for alkyne metathesis. In one aspect, the invention includes a multidentate organic ligand wherein one substrate-binding site of the metal center is blocked. In another aspect, the invention includes N-quaternized or silane-based multidentate organic ligands, capable of binding to metals. In yet another aspect, the invention includes N-quaternized or silane-based multidentate catalysts. The catalysts of the invention show high robustness, strong resistance to small alkyne polymerization and significantly enhanced catalytic activity compared to their corresponding non-quaternized or non-silane-based multidentate catalyst analogues. 2. The compound of claim 1 , wherein Ris N and each G is independently substituted with at least one electron-withdrawing substituent.3. The compound of claim 1 , where Ris selected from the group consisting of N claim 1 ,NH(A) claim 1 , NR(A) claim 1 , B claim 1 , P claim 1 , CH claim 1 , CR claim 1 , SiR and a 1 claim 1 ,3 claim 1 ,5-trivalent phenyl moiety claim 1 , wherein R is optionally substituted alkyl or aryl claim 1 , and A is an anion.8. The compound of claim 7 , wherein M is a transition metal.9. The compound of claim 8 , wherein M is selected from the group consisting of Mo claim 8 , W claim 8 , Re and Ta.10. The compound of claim 7 , wherein Ris N and each G is independently substituted with at least one electron-withdrawing substituent.11. The compound of claim 7 , where Ris selected from the group consisting of N claim 7 ,NH(A) claim 7 , NR(A) claim 7 , B claim 7 , P claim 7 , CH claim 7 , CR claim 7 , SiR and a 1 claim 7 ,3 claim 7 ,5-trivalent phenyl moiety claim 7 , wherein R is optionally substituted alkyl or aryl claim 7 , and A is an anion.12. The compound of claim 7 , wherein G is phenyl claim 7 , naphthyl or anthracenyl.14. The compound of claim 13 , wherein Ris NH(A) or N(R)(A) claim 13 , R is optionally substituted alkyl or aryl claim 13 , and A is an ...

N ortho acyl substituted nitrogen-containing heterocyclic compound and process for preparing aminal iron (ii) complexes thereof

Provided are a process for preparing an N ortho acyl substituted nitrogen-containing heterocyclic compound and an aminal iron (II) complex thereof, and the use of the complexes obtained by the process in an olefin oligomerization catalyst. The N ortho acyl substituted nitrogen-containing heterocyclic compound in the present invention is for example 2-acyl-1,10-phenanthroline or 2,6-diacetyl pyridine as shown in formula b, and the N ortho acyl substituted nitrogen-containing heterocyclic compound in the present invention is produced by a reaction of a precursor thereof in a substituted or unsubstituted nitrobenzene. Preferably the precursor shown in formula I in the present invention is produced by 1,10-phenanthroline reacting with trialkyl aluminum, or a halogenoalkyl aluminum R n AlX m , or a substituted or unsubstituted benzyl lithium 2 Li, followed by hydrolysis. The preparation method provided in the present invention has a few synthetic steps, an easy process, a low toxic effect, and reduces the preparation costs of the catalyst, and has a promising outlook in the industrial application.

PALLADIUM CATALYST, METHOD FOR ITS PREPARATION AND ITS USE

The invention relates to palladium(0)-tris{tri-[3,5-bis(trifluoromethyl)-phenyl]-phosphine} complex of formula (I), as well as to its preparation and use. 2. The composition of in a solid form.3. The composition of having a melting point of 220° C. as determined by DSC in inert atmosphere.4. The composition of claim 1 , having a decomposition point of 169.5° C. as determined by DSC in air under atmospheric pressure.5. A palladium(0) complex comprising three fluorinated phosphine compounds.6. The palladium(0) complex of exhibiting a stability characterized by no measurable decomposition on the basis of P claim 5 , F claim 5 , C and H NMR spectra following 4 months of storage in air at a temperature of 25° C.7. The palladium(0) complex of exhibiting a stability characterized by no measurable decomposition on the basis of P claim 5 , F claim 5 , C and H NMR spectra following 20 months of storage in air at room temperature.8. The palladium(0) complex of having a melting point in inert atmosphere of 220° C.9. The palladium(0) complex of exhibiting stability at any temperature below its melting point.10. The palladium(0) complex of exhibiting insolubility in water at industrially relevant temperatures and stability when stored in water.11. The palladium(0) complex of comprising a yellow solid.12. The palladium(0) complex of that dissolves at around 90° C. in aqueous alcohols.13. The palladium(0) complex of having catalytic activity in cross coupling reactions at a concentration of from 0.1 to 0.3 mole % of the substrate.14. A method for catalysing a C—C claim 5 , C-heteroatom claim 5 , or hydrogenation reaction comprising carrying out the C—C claim 5 , C-heteroatom or hydrogenation reaction in the presence of the palladium(0) complex of .15. The method of claim 14 , wherein the reaction is a C—C cross-coupling reaction.16. The method of claim 14 , wherein the C—C cross-coupling reaction is selected from the group consisting of: Suzuki coupling claim 14 , Heck coupling and ...

New palladium catalyst, method for its preparation and its use

The invention relates to palladium(0) tris{tri-[3,5-bis(trifluoromethyl)-phenyl]-phosphine} complex of formula (I), as well as to its preparation and use. This compound is outstandingly stable, and can be used as catalyst with excellent results.

METHODS FOR THE SYNTHESIS OF DEUTERATED VINYL PYRIDINE MONOMERS

Methods for synthesizing deuterated vinylpyridine compounds of the Formula (1), wherein the method includes: (i) deuterating an acyl pyridine of the Formula (2) in the presence of a metal catalyst and DO, wherein the metal catalyst is active for hydrogen exchange in water, to produce a deuterated acyl compound of Formula (3); (ii) reducing the compound of Formula (3) with a deuterated reducing agent to convert the acyl group to an alcohol group, and (iii) dehydrating the compound produced in step (ii) with a dehydrating agent to afford the vinylpyridine compound of Formula (1). The resulting deuterated vinylpyridine compounds are also described. 2. The method of claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , R claim 1 , and Rare deuterium atoms claim 1 , and R claim 1 , R claim 1 , and Rare hydrogen atoms.3. The method of claim 1 , wherein the metal of said metal catalyst in step (i) is selected from Pd claim 1 , Pt claim 1 , Ni claim 1 , Ru claim 1 , Rh claim 1 , Ir claim 1 , and combinations thereof.4. The method of claim 1 , wherein the metal of said metal catalyst in step (i) is selected from Pd claim 1 , Pt claim 1 , and mixtures thereof.5. The method of claim 1 , wherein said metal catalyst in step (i) is comprised of a catalytically active metal on a carbon support.6. The method of claim 1 , wherein step (i) is conducted at a temperature of at least 50° C. and below the critical temperature of water.7. The method of claim 1 , wherein step (i) is conducted at a temperature above 100° C. and below the critical temperature of water.8. The method of claim 1 , wherein step (i) is conducted at a temperature above 150° C. and below the critical temperature of water.9. The method of claim 1 , wherein step (i) is conducted at a pressure above 1 atm and below the critical pressure of water.10. The method of claim 1 , wherein said deuterated reducing agent is selected from aluminum deteurides and borodeuterides.11. The method of claim 1 , wherein said dehydrating ...

Anthracene compound and organic light emitting diode including the same

An anthracene compound and organic light emitting diode including the same are disclosed. The organic light emitting diode includes, at least two stacks formed between a first electrode and a second electrode and a charge generation layer (CGL) including an N-type CGL and a P-type CGL formed between the stacks, wherein the N-type CGL is formed of the anthracene compound.

Aromatic compounds

The present invention relates to aromatic compounds suitable for preparation of asymmetric polydentate ligands. The present invention further describes a process for preparing asymmetric polydentate ligands and metal complexes comprising these ligands which are suitable for use as emitters in organic electroluminescent devices.

MODULATORS OF TMEM16A FOR TREATING RESPIRATORY DISEASE

Compounds of general formula (I): 126.-. (canceled)30. The compound according to claim 27 , wherein Y is —CH—.31. The compound according to claim 27 , wherein:{'sup': '4', 'claim-ref': {'@idref': 'CLM-00027', '#text': 'claim 27'}, '#text': 'Ris a 6- to 11-membered aryl group selected from phenyl, naphthyl, indanyl, 1,2,3,4-tetrahydronaphthyl and benzocycloheptanyl, any of which is unsubstituted or substituted as defined in ; or'}{'sup': '4', 'claim-ref': {'@idref': 'CLM-00027', '#text': 'claim 27'}, '#text': 'Ris a 5- to 10-membered heteroaryl group selected from pyridyl, quinolinyl, quinoxalinyl, indazolyl, indolyl, benzoxazolyl, dihydrobenzofuranyl, furyl and thienyl, any of which is unsubstituted or substituted as defined in ; or'}{'sup': '4', 'claim-ref': {'@idref': 'CLM-00027', '#text': 'claim 27'}, '#text': 'Ris a carbocyclyl group selected from cyclohexyl and adamantyl, any of which is unsubstituted or substituted as defined in .'}34. The compound according to claim 32 , wherein:{'sup': ['11a', '11b'], 'sub': ['1-4', '1-4'], '#text': 'the compound is a compound of formula (Iai), (Ibi), (Ici), (Idi), (Iei), (Ifi) or (Igi) and either Ris H, halo, Calkyl or C(O)O(Calkyl) and Ris H; or'}{'sup': ['11a', '11b'], '#text': 'both Rand Rare halo; or'}{'sup': '11a', '#text': 'the compound is a compound of formula (Iaii), (Ibii), (Icii), (Idii), (Ieii), (Ifii) or (Igii) and Ris H; and'}{'sup': '11b', 'sub': ['1-4', '1-4', '1-4'], '#text': 'Ris Calkyl, Calkyl substituted with OH or Chaloalkyl; and'}{'sup': '11c', '#text': 'Ris H, halo, methyl or ethyl.'}36. A pharmaceutical composition comprising a compound according to and a pharmaceutically acceptable excipient.37. A method for the treatment or prophylaxis of diseases and conditions affected by modulation of TMEM16A claim 27 , the method comprising administering to a patient in need of such treatment an effective amount of a compound according to .38. The method of claim 37 , wherein the diseases and conditions affected ...

FLUOROELASTOMER COMPOSITION

The invention pertains to a fluoroelastomer composition comprising a vinylidene-fluoride based fluoroelastomer, a polyhydroxylated compound, a basic compound, a pyridinium-type salt having an aromatic ring-quaternized nitrogen atom, and comprising at least two groups having a central carbon atom which bears acidic hydrogen atoms; and an accelerant, which possesses an improved molding behaviour, leading to shaped parts possessing less blisters and surface defects.

Complexes

The present invention provides a palladium(II) complex of formula (1) or a palladium(II) complex of formula (2). 2. The process of claim 1 , wherein E is P.3. The process of claim 2 , wherein Rand Rare less sterically bulky than a cyclohexyl group when R claim 2 , R claim 2 , R claim 2 , Rand/or Rare more sterically bulky than a cyclohexyl group.4. The process of claim 1 , wherein R claim 1 , R claim 1 , Rand Rare —H.5. The process of claim 1 , wherein two of R claim 1 , R claim 1 , Rand Rare —H claim 1 , and the other two of R claim 1 , R claim 1 , Rand Rare claim 1 , independently claim 1 , unsubstituted straight-chain alkyl claim 1 , unsubstituted branched-chain alkyl claim 1 , unsubstituted cycloalkyl claim 1 , or unsubstituted alkoxy.6. The process of claim 1 , wherein three of R claim 1 , R claim 1 , R claim 1 , Rand Rare —H claim 1 , and the other two of R claim 1 , R claim 1 , R claim 1 , Rand Rare claim 1 , independently claim 1 , unsubstituted straight-chain alkyl claim 1 , unsubstituted branched-chain alkyl claim 1 , unsubstituted cycloalkyl claim 1 , unsubstituted alkoxy claim 1 , unsubstituted —N(alkyl) claim 1 , wherein the alkyl groups are independently straight-chain or branched-chain groups claim 1 , or unsubstituted —N(aryl) claim 1 , wherein the aryl groups are the same or different; or{'sub': 7', '8', '9', '10', '11', '7', '8', '9', '10', '11', '2', '2, 'wherein two of R, R, R, Rand Rare —H, and the other three of R, R, R, Rand Rare, independently, unsubstituted straight-chain alkyl, unsubstituted branched-chain alkyl, unsubstituted cycloalkyl, unsubstituted alkoxy, unsubstituted —N(alkyl), wherein the alkyl groups are independently straight-chain or branched-chain groups, or unsubstituted —N(aryl), wherein the aryl groups are the same or different.'}8. The process according to claim 1 , wherein X is a halo group or a trifluoroacetate group.11. The process of claim 10 , wherein E is P.12. The process of claim 11 , wherein Rand Rare less ...

Complexes

The present invention provides a palladium(II) complex of formula (1). 2. A palladium(II) complex according to claim 1 , wherein Ris selected from the group consisting of substituted and unsubstituted straight-chain alkyl claim 1 , substituted and unsubstituted branched-chain alkyl claim 1 , substituted and unsubstituted cycloalkyl claim 1 , substituted and unsubstituted aryl claim 1 , and substituted and unsubstituted heteroaryl wherein the heteroatoms are independently selected from sulfur claim 1 , nitrogen and oxygen.3. A palladium(II) complex according to claim 1 , wherein X is a halo group or a trifluoroacetate group.6. A process for carrying out a carbon-carbon coupling reaction or a carbon-heteroatom coupling reaction in the presence of a catalyst claim 1 , the process comprising the use of a complex of formula (1) as defined in .7. The process of claim 6 , wherein the carbon-carbon coupling reaction is (a) a Heck reaction; (b) a Suzuki reaction; (c) a Sonogashira reaction; or (d) a Negishi reaction and the carbon-heteroatom coupling reaction is a Buchwald-Hartwig amination reaction. This application is a divisional of U.S. patent application Ser. No. 16/686,960, filed Nov. 18, 2019, which is a divisional of U.S. patent application Ser. No. 16/284,841, filed Feb. 25, 2019, now U.S. Pat. No. 10,858,382, which is a divisional of U.S. patent application Ser. No. 15/318,106, filed Dec. 12, 2016, now U.S. Pat. No. 10,253,056, which is a US national stage of International patent Application No. PCT/GB2015/050835, filed Mar. 20, 2015, which claims priority to U.S. Provisional Patent Application No. 62/011,168, filed Jun. 12, 2014, all applications of which are incorporated by reference herein.The present invention relates to optionally substituted π-allyl palladium complexes and their use thereof in coupling reactions.WO2011/161451 (to Johnson Matthey PLC) describes π-allyl complexes, such as π-allyl palladium complexes and π-allyl nickel complexes.Faller et al ( ...

Method For Preparation of Alkylated or Fluoro, Chloro and Fluorochloro Alkylated Compounds By Heterogeneous Catalysis

The invention discloses a method for preparation of alkylated or fluoro, chloro and fluorochloro alkylated compounds by a heterogeneous Pt/C-catalyzed alkylation or fluoro, chloro and fluorochloro alkylation with alkyl halides or with fluoro, chloro and fluorochloro alkyl halides in the presence of CsC0or CsHC0. 116-. (canceled)19. The method according to claim 17 , whereinm, n and q are identical or different and independently from each other 0, 1, 2, 3 or 4.21. The method according to claim 17 , whereinX is Br or I.22. The method according to claim 17 , whereinX is I.23. The method according to claim 17 , wherein{'sub': 2', '2, 'compound FCLALKYLHADLIDE is a perfluoroalkyl halide, FHC—Cl or FHC—Br.'}24. The method according to claim 17 , whereinX is Cl, Br or I, and{'sub': '1-20', 'R3 is perfluoro Calkyl; or'}{'sub': 2', '2, 'FCLALKYLHADLIDE is FHC—Cl or FHC—Br.'}25. The method according to claim 17 , wherein{'sub': 21', '10', '17', '8', '13', '6', '9', '4', '3', '3', '3', '2', '2, 'FCLALKYLHALIDE is selected from the group consisting of FC—I, FC—I, FC—I, FC—I, FC—I, FC—Br, FC—Cl, FHC—Cl and FHC—Br.'}26. The method according to claim 17 , whereinthe reaction is done in the presence of a compound COMPSALT;wherein COMPSALT is selected from the group consisting of NaI, KI, CsI and N(R30)(R31)(R32)R33I; and{'sub': '1-10', 'R30, R31, R32 and R33 are identical or different and independently from each other selected from the group consisting of H and Calkyl.'}27. The method according to claim 26 , wherein{'sub': '2-6', 'R30, R31, R32 and R33 are identical or different and independently from each other selected from the group consisting of H and Calkyl.'}28. The method according to claim 26 , wherein{'sub': '4', 'COMPSALT is selected from the group consisting of NaI and (n-Bu)NI.'}29. The method according to claim 17 , whereinthe amount of Pt in CAT is from 0.1 to 20%, the % are % by weight and are based on the combined weight of Pt and C in CAT.30. The method according ...

Method of preparing benzyl 4-amino-3-chloro-5-fluoro-6-(4-chloro-2-fluoro-3-methoxyphenyl)picolinate

A method of preparing benzyl 4-amino-3-chloro-5-fluoro-6-(4-chloro-2-fluoro-3-methoxyphenyl)picolinate (I) from benzyl 4,5-difluoro-6-(4-chloro-2-fluoro-3-methoxyphenyl)picolinate (II) is described. The method includes the use of amination and chlorination process steps to provide the compound of Formula I.

Complexes

The present invention provides a palladium(II) complex of formula (1) or a palladium(II) complex of formula (2). 137-. (canceled)39. The palladium(II) complex of claim 38 , wherein Rand Rare the same and are cyclohexyl.40. The palladium(II) complex of claim 38 , wherein Rand Rare claim 38 , independently claim 38 , —H claim 38 , substituted or unsubstituted straight-chain alkyl claim 38 , substituted or unsubstituted branched-chain alkyl claim 38 , substituted or unsubstituted cycloalkyl claim 38 , substituted or unsubstituted alkoxy claim 38 , substituted or unsubstituted aryl claim 38 , substituted or unsubstituted heteroaryl claim 38 , substituted or unsubstituted —N(alkyl)(wherein the alkyl groups are the same or different and are claim 38 , independently claim 38 , a straight-chain or branched-chain group) claim 38 , substituted or unsubstituted —N(cycloalkyl)(wherein the cycloalkyl groups are the same or different) claim 38 , substituted or unsubstituted —N(aryl)(wherein the aryl groups are the same or different) claim 38 , substituted or unsubstituted —N(heteroaryl)(wherein the heteroaryl groups are the same or different) or substituted or unsubstituted heterocycloalkyl.41. The palladium(II) complex of claim 40 , wherein both of Rand Rare —H.42. The palladium(II) complex of claim 38 , wherein Rand Rare claim 38 , independently claim 38 , —H claim 38 , substituted or unsubstituted straight-chain alkyl claim 38 , substituted or unsubstituted branched-chain alkyl claim 38 , substituted or unsubstituted cycloalkyl claim 38 , substituted or unsubstituted alkoxy claim 38 , substituted or unsubstituted -thioalkyl claim 38 , substituted or unsubstituted aryl claim 38 , substituted or unsubstituted heteroaryl claim 38 , substituted or unsubstituted —N(alkyl)(wherein the alkyl groups are the same or different and are claim 38 , independently claim 38 , straight-chain or branched-chain group) claim 38 , substituted or unsubstituted —N(cycloalkyl)(wherein the cycloalkyl ...

Highly active multidentate catalysts for efficient alkyne metathesis

The invention relates to highly active and selective catalysts for alkyne metathesis. In one aspect, the invention includes a multidentate organic ligand wherein one substrate-binding site of the metal center is blocked. In another aspect, the invention includes N-quaternized or silane-based multidentate organic ligands, capable of binding to metals. In yet another aspect, the invention includes N-quaternized or silane-based multidentate catalysts. The catalysts of the invention show high robustness, strong resistance to small alkyne polymerization and significantly enhanced catalytic activity compared to their corresponding non-quaternized or non-silane-based multidentate catalyst analogues.

Drier Composition and Use Thereof

The invention relates to a drier composition for an autoxidizable alkyd based coating composition, comprising: 1. A drier composition for an autoxidizable alkyd based coating composition , comprising:a) at least one Fe complex comprising Fe and at least one nitrogen donor ligand, wherein said at least nitrogen donor ligand is selected from tridentate, tetradentate, pentadentate and hexadentate nitrogen donor ligands;b) at least one metal salt of a carboxylic acid, wherein the metal is selected from Mn, Ce, V, and Cu;c) at least one ligand comprising at least one moiety selected from 1,4,7-tri-azacyclononanyl, 2,2′-bipyridyl, 1,10-phenantrolinyl, imidazolyl, pyrazolyl, porphyrinyl, aliphatic, cycloaliphatic, and aromatic amines; andd) a K salt of a carboxylic acid.4. The drier composition according to claim 1 , wherein the metal in b) is selected from Mn and Ce.5. The drier composition according to claim 1 , wherein the carboxylic acid is selected from branched-chain or straight-chain saturated and unsaturated aliphatic claim 1 , aromatic and alicyclic monocarboxylic acids having 5 to 22 carbon atoms claim 1 , cycloaliphatic monocarboxylic acids having 5 to 10 carbon atoms claim 1 , or mixtures of these acids claim 1 , and wherein the carboxylic acid is selected from 2-ethylbutanoic acid claim 1 , 2 claim 1 ,2-dimethylpentanoic acid claim 1 , 2-ethylpentanoic acid claim 1 , 2-ethyl-4-methylpentanoic acid claim 1 , 2-ethylhexanoic acid claim 1 , isooctanoic acid claim 1 , isononanoic acid claim 1 , neononanoic acid claim 1 , nonanoic acid claim 1 , isodecanoic acid claim 1 , neodecanoic acid claim 1 , 2-ethyldecanoic acid claim 1 , isotridecanoic acid claim 1 , isotetradecanoic acid claim 1 , n-hexanoic acid claim 1 , n-octanoic acid claim 1 , n-decanoic acid claim 1 , n-dodecanoic acid claim 1 , cyclopentanoic acid claim 1 , methylcyclopentanoic acid claim 1 , cyclohexanoic acid claim 1 , methylcyclohexanoic acid claim 1 , 1 claim 1 ,2-dimethylcyclohexanoic acid ...

METHOD FOR SYNTHESIZING BIPYRIDINE COMPOUND AND METHOD FOR MANUFACTURING PYRIDINE COMPOUND

A target bipyridine compound is synthesized with high purity and a high yield in a simple and safe manner in a short period of time. A method for synthesizing a di-tert-butyl-2,2′-bipyridine compound is provided, and the method includes a step of reacting, in a reaction solvent, a tert-butylpyridine compound with a dispersion product obtained by dispersing an alkali metal in a dispersion solvent. A method for synthesizing a bipyridine compound having no substituents is also provided, and the method includes a step of reacting, in a reaction solvent, pyridine with a dispersion product obtained by dispersing an alkali metal in a dispersion solvent. 2. The method for synthesizing a bipyridine compound according to claim 1 , wherein a hydrogen donor is added to a reaction product produced through the reaction of the tert-butylpyridine compound with the dispersion product obtained by dispersing an alkali metal in a dispersion solvent.3. The method for synthesizing a bipyridine compound according to claim 1 , wherein the reaction solvent contains a hydrogen donor.4. The method for synthesizing a bipyridine compound according to claim 1 , wherein the tert-butylpyridine compound is 4-tert-butylpyridine claim 1 , and 4 claim 1 ,4′-di-tert-butyl-2 claim 1 ,2′-bipyridine is synthesized.5. The method for synthesizing a bipyridine compound according to claim 1 , wherein when a ratio of tetrahydrofuran serving as the reaction solvent with respect to 1 mmol of the tert-butylpyridine compound is set to 2 ml or more and 8 ml or less claim 1 , the alkali metal is used in an amount of 1 mol equivalent or more and 2.5 mol equivalents or less with respect to the tert-butylpyridine compound.7. The method for synthesizing a bipyridine compound according to claim 6 , wherein a hydrogen donor is added to a reaction product produced through the reaction of the pyridine with the dispersion product obtained by dispersing an alkali metal in a dispersion solvent.8. The method for synthesizing a ...

METHOD FOR COUPLING HALOGENATED PYRIDINE COMPOUND WITH HALOGENATED AROMATIC COMPOUND

There is a demand for the development of a technique according to which a reaction for coupling a halogenated pyridine compound with a halogenated aromatic compound can be performed in a simple manner through a small number of steps without using expensive agents such as a palladium catalyst. A method for coupling a halogenated pyridine compound with a halogenated aromatic compound includes a step of coupling a halogenated pyridine compound with a halogenated aromatic compound to obtain a pyridine compound by reacting, in a reaction solvent, the halogenated pyridine compound and the halogenated aromatic compound with a solution containing an alkali metal. 2. The method for coupling a halogenated pyridine compound with a halogenated aromatic compound according to claim 1 , wherein the X1 and the X2 represent a chlorine atom claim 1 , the R1 and the R2 represent a hydrogen atom claim 1 , the Y represents a nitrogen atom claim 1 , and the X′ represents a hydrogen atom or a chlorine atom.3. The method for coupling a halogenated pyridine compound with a halogenated aromatic compound according to claim 2 , wherein the reaction solvent includes chlorobenzene.4. The method for coupling a halogenated pyridine compound with a halogenated aromatic compound according to claim 1 , wherein the X1 represents a chlorine atom claim 1 , the X2 represents a bromine atom claim 1 , the R1 and the R2 represent a hydrogen atom claim 1 , the Y represents a carbon atom claim 1 , and the X′ represents a hydrogen atom.5. The method for coupling a halogenated pyridine compound with a halogenated aromatic compound according to claim 1 , wherein the X1 and the X2 represent a chlorine atom claim 1 , the R1 and the R2 represent a methyl group claim 1 , the Y represents a nitrogen atom claim 1 , and the X′ represents a hydrogen atom or a chlorine atom.6. The method for coupling a halogenated pyridine compound with a halogenated aromatic compound according to claim 1 , wherein the reaction solvent ...

PALLADIUM (II)-CATALYZED gammaC(SP)-H ALKYNYLATION OF AMINE2

The present invention relates to a Palladium (II)-catalyzed C(sp)—H alkynylation of amines using picolinamide as directing group. The developed alkynylation strategy is simple, efficient, and tolerant of various ring size including five to eight member cyclic, quaternary amines, and N-heterocyclic motifs. 2. The process as claimed in claim 1 , wherein said amide is selected from the group consisting of N-cyclohexylpicolinamide claim 1 , N-(4-methylcyclohexyl)picolinamide claim 1 , N-(4-butylcyclohexyl)picolinamide claim 1 , N-cyclopentylpicolinamide claim 1 , N-cycloheptylpicolinamide claim 1 , N-cyclooctylpicolinamide methyl 1-(picolinamido)cyclopentanecarboxylate claim 1 , ethyl 1-(picolinamido)cyclopentanecarboxylate claim 1 , tert-butyl 3-(picolinamido)piperidine-1-carboxylate claim 1 , N-(5-methylhexan-2-yl)picolinamide claim 1 , N-(octan-2-yl)picolinamide claim 1 , N-cyclohexyl-6-methylpicolinamide claim 1 , N-cyclohexyl-3-methylpicolinamide claim 1 , N-cyclohexylpyrazine-2-carboxamide claim 1 , N-cyclohexyl-5-methylpyrazine-2-carboxamide claim 1 , N-cyclohexylquinoline-2-carboxamide claim 1 , N-cyclohexylisoquinoline-1-carboxamide claim 1 , and N-cyclohexyl-1-methyl-1H-indazole-3-carboxamide.3. The process as claimed in claim 1 , wherein said amine is selected from the group consisting of Cyclohexanamine claim 1 , 4-methylcyclohexanamine claim 1 , 4-butylcyclohexanamine claim 1 , cyclopentanamine claim 1 , cycloheptanamine claim 1 , cyclooctanamine claim 1 , methyl 1-aminocyclopentanecarboxylate claim 1 , ethyl 1-aminocyclopentanecarboxylate claim 1 , 5-methylhexan-2-amine claim 1 , and nonan-2-amine.4. The process as claimed in claim 1 , wherein said haloalkyne is selected from the group consisting of (bromoethynyl)triisopropylsilane claim 1 , (bromoethynyl)dimethyl(phenyl)silane claim 1 , (bromoethynyl)(tert-butyl)dimethylsilane claim 1 , (bromoethynyl)(ethyl)dimethylsilane claim 1 , tert-butyl(iodoethynyl)dimethylsilane claim 1 , and (bromoethynyl) ...

Isoxazole Derivatives as FXR Agonists and Methods of Use Thereof

The present invention provides compounds of Formula I: 8. A method for preventing or treating an FXR-mediated disease or condition in a subject in need thereof claim 1 , comprising administering to the subject a therapeutically effective amount of a compound according to .9. The method according to claim 8 , wherein the FXR-mediated disease or condition is selected from the group consisting of chronic liver disease claim 8 , gastrointestinal disease claim 8 , renal disease claim 8 , cardiovascular disease claim 8 , and metabolic disease.10. The method according to claim 9 , wherein the chronic liver disease is selected from the group consisting of primary biliary cirrhosis (PBC) claim 9 , cerebrotendinous xanthomatosis (CTX) claim 9 , primary sclerosing cholangitis (PSC) claim 9 , drug induced cholestasis claim 9 , intrahepatic cholestasis of pregnancy claim 9 , parenteral nutrition associated cholestasis (PNAC) claim 9 , bacterial overgrowth or sepsis associated cholestasis claim 9 , autoimmune hepatitis claim 9 , chronic viral hepatitis claim 9 , alcoholic liver disease claim 9 , nonalcoholic fatty liver disease (NAFLD) claim 9 , nonalcoholic steatohepatitis (NASH) claim 9 , liver transplant associated graft versus host disease claim 9 , living donor transplant liver regeneration claim 9 , congenital hepatic fibrosis claim 9 , choledocholithiasis claim 9 , granulomatous liver disease claim 9 , intra- or extrahepatic malignancy claim 9 , Sjogren's syndrome claim 9 , Sarcoidosis claim 9 , Wilson's disease claim 9 , Gaucher's disease claim 9 , hemochromatosis claim 9 , and alpha 1-antitrypsin deficiency.11. The method according to claim 9 , wherein the renal disease is selected from the group consisting of diabetic nephropathy claim 9 , focal segmental glomerulosclerosis (FSGS) claim 9 , hypertensive nephrosclerosis claim 9 , chronic glomerulonephritis claim 9 , chronic transplant glomerulopathy claim 9 , chronic interstitial nephritis claim 9 , and polycystic kidney ...

Preparation method of 4-(4-amino-3-fluorophenoxy)-n-methylpyridine-2-formamide

The present invention relates to a preparation method of 4-(4-amino-3-fluorophenoxy)-N-methylpyridine-2-formamide capable of enabling 4-chlorine-N-methylpyridine-2-formamide to react with 4-amino-3-fluorophenol in the presence of an inorganic base. The present invention employs the inorganic base to replace potassium t-butoxide in the prior art, thus effectively solving the problem of a potential safety hazard of the potassium t-butoxide in industrial production. In addition, after the reaction is completed, the present invention employs a crystallization method for separation to obtain a reaction product; thus compared with the methods of extraction, concentration and column isolation and purification employed in the prior art, the present invention has a simpler operation and a lower cost, results in less environment pollution and a higher yield, and is very suitable for industrial production.

Method for preparing 2,2'-dipyridine and derivatives thereof

Disclosed is a method for preparing 2,2′-dipyridine and derivatives thereof. The method includes: using pyridine represented by formula I or a derivative thereof as a raw material to generate 2,2′-dipyridine represented by formula II by performing dehydrogenative coupling under the action of a supported catalyst in the presence of additives, where R is H, C1-C2 alkyl, Cl, or Br. The method of the present invention features wide adaptability to raw materials, high atomic utilization rate, high catalyst activity, long service life, and fewer by-products.

ANTHRACENE COMPOUND, METHOD FOR PREPARING THE SAME, USE THEREOF AND ORGANIC LIGHT EMITTING DEVICE

Provided are anthracene compound, method for preparing the same and use thereof, as well as organic electroluminescent device containing the same. The anthracene compound represented by a formula: 2. The anthracene compound according to claim 1 , wherein R is selected from C6-C50 phenyl claim 1 , biphenyl claim 1 , naphthyl claim 1 , quinolyl claim 1 , phenanthryl claim 1 , pyridyl claim 1 , phenalenyl claim 1 , 9 claim 1 ,9-dimethyl-fluorenyl claim 1 , terphenyl claim 1 , anthryl claim 1 , aromatic azyl claim 1 , carbazolyl claim 1 , benzothiazolyl claim 1 , thienyl claim 1 , substituted or unsubstituted heterocyclic aryl claim 1 , or anilino.4. A method for utilizing the anthracene compound according to in an organic electroluminescent device claim 1 , comprising: using the anthracene compound as a fluoresce host material claim 1 , a hole injection material or a hole transport material in the organic electroluminescent device.5. The method according to claim 4 , wherein the anthracene compound is used as a fluorescent green host material in the organic electroluminescent device.6. An organic electroluminescent device claim 4 , comprising:a first electrode;a second electrode; andone or more organic compound layers between the first electrode and the second electrode,{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'wherein at least one organic compound layer comprises the anthracene compound according to .'}10. The method according to claim 7 , wherein R-boric acid is selected from phenylboric acid claim 7 , 4-biphenylboric acid claim 7 , 2-naphthylboric acid claim 7 , 8-quinolylboric acid claim 7 , 9-phenanthrylboric acid claim 7 , 4-pyridylboric acid claim 7 , phenalenylboric acid claim 7 , 4-(4-pyridyl)-phenylboric acid claim 7 , 9 claim 7 ,9-dimethyl-fluorenylboric acid claim 7 , 3 claim 7 ,5-diphenyl-phenylboric acid claim 7 , 9-anthrylboric acid claim 7 , or 2-benzothiazolylboric acid.11. An organic electroluminescent device claim 7 , comprising:a first ...

Stabilization of active metal catalysts at metal-organic framework nodes for highly efficient organic transformations

Metal-organic framework (MOFs) compositions based on post¬synthetic metalation of secondary building unit (SBU) terminal or bridging OH or OH 2 groups with metal precursors or other post-synthetic manipulations are described. The MOFs provide a versatile family of recyclable and reusable single-site solid catalysts for catalyzing a variety of asymmetric organic transformations, including the regioselective boryiation and siiylation of benzyiic C—H bonds, the hydrogenation of aikenes, imines, carbonyls, nitroarenes, and heterocycles, hydroboration, hydrophosphination, and cyclization reactions. The solid catalysts can also be integrated into a flow reactor or a supercritical fluid reactor.

PROCESS FOR PREPARING 5-[[4-[2-[5-(1-HYDROXYETHYL)-2-PYRIDINYL]ETHOXY]PHENYL]METHYL]-2,4-THIAZOLIDINEDIONE AND SALTS THEREOF

The disclosure provides a process of making the compound of Formula I, and pharmaceutically acceptable salts thereof: and the process of making the intermediate of Formula III: wherein PG is as defined as set forth in the specification. 2. The process of claim 1 , wherein PG is a protecting group selected from the group consisting of a silyl protecting group claim 1 , tetrahydropyranyl claim 1 , methoxymethyl claim 1 , and benzyl.3. The process of or claim 1 , wherein the ethylene oxide claim 1 , alkyl lithium claim 1 , and copper(I)salt or the Lewis acid are added into the reaction mixture comprising the compound of Formula II while maintaining the temperature of the reaction mixture below −20° C.4. The process of any one of - claim 1 , wherein the ethylene oxide claim 1 , alkyl lithium claim 1 , and copper(I)salt or the Lewis acid are added while maintaining the temperature of the reaction mixture at about <−55° C.5. The process of any one of - claim 1 , wherein the ethylene oxide is added into the reaction mixture after first adding the alkyl lithium.6. The process of any one of - claim 1 , wherein the ethylene oxide is added into the reaction mixture after adding the alkyl lithium and the copper(I)salt or the Lewis acid.7. The process of any one of - claim 1 , wherein the reaction mixture is allowed to warm to room temperature after the addition of the reagents.8. The process of any one of - claim 1 , wherein the reaction is conducted in the presence of an alkyl lithium and copper(I)iodide.9. The process of claim 8 , wherein the alkyl lithium and copper(I)iodide are added while maintaining the reaction temperature at about <−55° C.10. The process of any one of - claim 8 , wherein the reaction is conducted in the presence of an alkyl lithium and a Lewis acid selected from the group consisting of BF.O(Et) claim 8 , BBrand BCl.12. The process of claim 11 , wherein the ethylene oxide is added into the reaction mixture after first adding the alkyl lithium.13. The ...

Hydrogen Bond Directed Photocatalytic Hydrodefluorination and Methods of Use Thereof

Methods of synthesizing compounds comprising fluorinated aryl groups are disclosed, wherein said methods utilize hydrogen bond directed photocatalytic hydrodefluorination.

Synthesis of aryl coupled bis phenoxides and their use in olefin polymerization catalyst systems with activator-supports

Disclosed herein are methods of making bis(phenol) ligand compounds and transition metal bis(phenolate) compounds. The transition metal bis(phenolate) compounds can be used as components in catalyst systems for the polymerization of olefins.

Synthesis of aryl coupled bis phenoxides and their use in olefin polymerization catalyst systems with activator-supports

Disclosed herein are methods of making bis(phenol) ligand compounds and transition metal bis(phenolate) compounds. The transition metal bis(phenolate) compounds can be used as components in catalyst systems for the polymerization of olefins.

Synthesis of aryl coupled bis phenoxides and their use in olefin polymerization catalyst systems with activator-supports

Disclosed herein are methods of making bis(phenol) ligand compounds and transition metal bis(phenolate) compounds. The transition metal bis(phenolate) compounds can be used as components in catalyst systems for the polymerization of olefins.

Improved process for preparing 1-(6-methylpyridin-3-yl)-2-[4-(methylsulfonyl)phenyl]ethanone, an intermediate of etoricoxib

The present invention relates to a process for preparing 1-(6-methylpyridin-3-yl)-2-[4-(methylsulfonyl)phenyl]ethanone, an intermediate of the synthesis of Etoricoxib. The synthesis of the intermediates useful for such preparation is also described.

Novel borate compound-containing composition

The purpose of the present invention is to provide: a borate compound-containing composition which is useful as a promoter for polymerization of olefins or dienes and which is soluble in a hydrocarbon solvent; and a manufacturing method therefor. The present invention pertains to a composition containing a base A or a compound having eight or more total carbon atoms and represented by formula (5), (Definitions of the symbols in the formula are as disclosed in the specification.) and a borate compound represented by formula (1). (Definitions of the symbols in the formula are as disclosed in the specification.) The present invention additionally pertains to a manufacturing method for the composition.

芳基连接的双酚盐的合成及其用于具有活化剂-载体的烯烃聚合催化剂系统

本文公开的是制备双酚配体化合物和过渡金属双酚盐化合物的方法。过渡金属双酚盐化合物可被用作用于聚合烯烃的催化剂系统中的组分。

一种吡啶化合物烯基化的方法

本发明公开了一种吡啶化合物烯基化的方法，属于有机合成技术领域。该方法包括以下步骤：将吡啶季铵盐、内炔烃、催化剂、配体、一价铜盐、碱以及溶剂的混合物进行加热反应，得到式Ⅰ的化合物。式Ⅰ： 式I中R包括R 1 以及可选的R 2 ，其中，R 1 位于吡啶环的2位，R 1 包括烷基或取代苯基；R 2 位于吡啶环的3位至5位中的任意位置，R 2 包括烷基、取代烷基或苯基，Ar包括烷基、苯基或具有取代基的苯基。该方法使用季铵活化策略来进行吡啶底物的烯基化反应，克服了过去合成这类物质条件苛刻以及反应步骤繁琐等缺点，底物范围广泛，反应选择性良好，并具有较高的产率。

팔라듐 촉매제와 그 제조 방법 및 그 이용

본 발명은 하기 NMR 스펙트라의 특성 데이터를 가지는 화합물에 관한 것으로, 상기 화합물은 팔라듐염(II)을 트리[3,5-비스(트리플루오르메틸)-페닐]포스핀과 반응시켜, 착물 염을 형성하고, 착물 염 상태의 팔라듐(II)을 팔라듐(0)으로 환원시켜 촉매 특성을 갖는 팔라듐(0) 착물을 제조하는 단계를 포함하여 제조한 것을 특징으로 하는 화합물이며, NMR 스펙트라의 특성 테이터는 하기와 같다. 1 H-NMR (300 MHz, THF-d8, d= 3.58 ppm) 8.17 (s, 12H), 7.84 (s, 24H); 13 C-NMR(75 MHz, THF-d8, d= 67.3 ppm) 138,1(C), 133.7(q, J=38.7 Hz, C),133.4(CH),126.3(CH),123.4(q, J=271.57 Hz, CF3); 31 P-NMR(300 MHz, THF-d8) 28.77; 19 F-NMR(300 MHz, THF-d8)- 62.94. 이와 같은 화합물은 대단히 안정되고, 우수한 결과를 갖는 촉매제로 이용될 수 있다.

Amide addition reaction

A method of making a compound of formula II comprising the reaction of a compound of formula RCONH 2 with a compound of formula III R being a moiety having between 1 and 15 carbon atoms and optionally from 1 to 5 heteroatoms independently selected from oxygen, nitrogen and sulfur, and X and Y being independently selected front the group consisting of H, methyl, ethyl, OMe, OEt, and mixtures thereof; the reaction being performed in a solvent in the presence of a base. The method is useful for the inexpensive manufacture of certain commercially-valuable compounds, including some that have desirable cooling properties.

一种高负载量镍基催化剂及其制备方法与应用

本发明公开了一种高负载量镍基催化剂，它是以氧化铝为载体，以金属镍为活性成分，以氧化铈、氧化镧、氧化锆、氧化镁的一种或多种为助剂；金属镍占镍基催化剂质量的10～80％；助剂占镍基催化剂质量的1～20％。本发明镍基催化剂是由镍盐前驱体、氧化铝、助剂前驱体混合球磨后经焙烧、打片、还原制得的。本发明还公开了高负载量镍基催化剂在吡啶脱氢偶联制备2,2‑联吡啶中的应用，具有转化率高、稳定性好的优点，联吡啶的时空收率优于同等反应条件下的雷尼镍与负载镍的催化效果，可高达0.41g/gCat./h，催化剂寿命远超过同等反应条件下的雷尼镍与负载镍，寿命最长可以超过1500h。

Synthesis of aryl coupled bis phenoxides and their use in olefin polymerization catalyst systems with activator-supports

Disclosed herein are methods of making bis(phenol) ligand compounds and transition metal bis(phenolate) compounds. The transition metal bis(phenolate) compounds can be used as components in catalyst systems for the polymerization of olefins.

Condensed compound and organic light emitting diode comprising the same

축합환 화합물 및 이를 포함한 유기 발광 소자가 개시된다. Disclosed are a condensed cyclic compound and an organic light emitting device including the same.

Ｎ 오르토 아실 치환된 질소-포함 헤테로시클릭 화합물 및 이의 아미날 철 （ⅱ） 착체의 제조 방법

N 오르토 아실 치환된 질소-함유 헤테로시클릭 화합물, 및 이의 아미날 철 (II) 착체의 제조 방법과, 상기 방법에 의해 수득되는 착체의, 올레핀 올리고머화 촉매에 있어서의 용도가 제공된다. 본 발명에서, N 오르토 아실 치환된 질소-함유 헤테로시클릭 화합물은, 예를 들어 화학식 b로 표시되는 2-아실-1,10-페난트롤린 또는 2,6-디아세틸 피리딘이며; 본 발명에서, N 오르토 아실 치환된 질소-함유 헤테로시클릭 화합물은 치환 또는 비치환된 니트로벤젠 중에서의 이의 전구체의 반응에 의해 제조된다. 바람직하게는, 본 발명의 화학식 I로 표시되는 전구체는, 1,10-페난트롤린이 트리알킬 알루미늄, 또는 할로게노알킬 알루미늄 R n AlX m , 또는 치환 또는 비치환된 벤질 리튬 Ph'CH 2 Li와 반응한 다음, 가수분해 반응함으로써 제조된다. 본 발명에서 제공된 제조 방법은, 합성 단계의 수가 적으며, 공정이 용이하고, 독성 효과가 낮으며, 촉매의 제조 비용을 경감시켜서, 산업적인 적용에서 큰 가능성을 가지고 있다.

酰胺加成反应

制备式(II)的化合物的方法，包括使式RCONH 2 的化合物与式(III)的化合物反应

一种n邻位酰基取代的含氮杂环化合物及其缩胺合铁（ⅱ）配合物的制备方法

本发明提供一种N邻位酰基取代的含氮杂环化合物及其缩胺合铁(II)配合物的制备方法，以及由该方法制得的配合物在烯烃齐聚催化剂中的应用。本发明中所述N邻位酰基取代的含氮杂环化合物例如为式b所示的2-酰基-1,10-菲咯啉或2,6-二乙酰基吡啶；本发明所述N邻位酰基取代的含氮杂环化合物是通过其前体物质在取代或未取代的硝基苯中反应生成。优选本发明中式Ⅰ所示前体化合物是由1,10-菲咯啉与三烷基铝或卤代烷基铝R n AlX m 、或取代或未取代的苄基锂Ph’CH 2 Li反应，再经水解而生成。本发明提供的制备方法合成步骤少，工艺简单，低毒害且降低了催化剂制备成本，其工业化前景广阔。

一种2,2’-联吡啶的合成方法

本发明属于化学工业合成领域，具体涉及一种2，2’-联吡啶的合成方法。本发明方法包括如下顺序的步骤：(1)环辛二烯在氨基钠(或金属钠)的催化下和无水氯化钴反应，生成环辛二烯基茂钴，是一种活性较高的催化剂(2)2-氰基吡啶在环辛二烯基茂钴的催化下和乙炔气体反应，生成2，2’-联吡啶。

钯催化剂、其制备方法及其用途

本发明涉及式(I)的钯(0)-四{三-[3,5-二(三氟甲基)-苯基]-膦}配合物,以及其制备和用途。该化合物非常稳定，可用作催化剂，具有优异的结果。

new palladium catalyst, method for its preparation and use

Synthesis of aryl coupled bis phenoxides and their use in olefin polymerization catalyst systems with activator-supports

Amide addition reaction

制备式(II)的化合物的方法，包括使式RCONH 2 的化合物与式(III)的化合物反应

Lamotrigine and 2,2 '-dipyridyl pharmaceutical co-crystals and preparation method thereof

本发明涉及一种拉莫三嗪与2,2’-联吡啶药物共晶及其制备方法。选用拉莫三嗪原料药作为药物API，选用的药物前驱体为2,2’-联吡啶。采用溶液介导转变法或研磨法，本发明制备得到的拉莫三嗪与2,2’-联吡啶药物共晶,共晶熔点为123-127℃，该DSC图谱并不存在两种原料的熔点峰，而是产生了新的熔点峰，这也是形成共晶的标志。新的共晶大幅度提高了拉莫三嗪在水中的溶解度和溶解速率。溶液中得到的共晶在水中的溶解度为≧1.36mg/ml；同时溶解速率在溶解度范围内提高了20％以上；尤其是研磨得到的共晶溶解速率更快，提高了拉莫三嗪的生物利用度。便于在工业制药中大量推广，成本低廉。

A new palladium catalyst, method for its preparation and its use

본 발명은 공식(I)의 팔라듐(0)-테트라키스{트리-[3,5-비스(트리플루오르메틸)-페닐]-포스핀} 착물과 그 제조 방법 및 그 이용에 관한 것이다. 이와 같은 화합물은 대단히 안정되고, 우수한 결과를 갖는 촉매제로 이용될 수 있다. (I)

A series of PHOLED (phosphorescent organic light-emitting diode) materials

本发明公开了一系列磷光OLED材料。该磷光OLED材料的结构通式如式I-1或式I-2所示。本发明基于电致磷光材料需要高的热稳定性、高的量子效率，同时具有较低的掺杂比例，提供了一系列具有环己基和环己烯基团的铱配合物电致磷光发光材料。该类化合物具有成膜性成优异，不易结晶，发光效率高等特点，而且原料易得，制备简便，总体收率高，大大降低的磷光材料的成本，具有重要的应用价值。

Aromatic compounds

Die vorliegende Erfindung betrifft aromatische Verbindungen, welche sich zur Herstellung von asymmetrischen polydentaten Liganden eignen. Ferner beschreibt die vorliegende Erfindung ein Verfahren zur Herstellung von asymmetrischen polydentaten Liganden und Metallkomplexen, die diese Liganden umfassen, welche sich für den Einsatz als Emitter in organischen Elektrolumineszenzvorrichtungen eignen.

A series of phosphorescent OLED materials

本发明公开了一系列磷光OLED材料。该磷光OLED材料的结构通式如式I‑1或式I‑2所示。本发明基于电致磷光材料需要高的热稳定性、高的量子效率，同时具有较低的掺杂比例，提供了一系列具有环己基和环己烯基团的铱配合物电致磷光发光材料。该类化合物具有成膜性成优异，不易结晶，发光效率高等特点，而且原料易得，制备简便，总体收率高，大大降低的磷光材料的成本，具有重要的应用价值。

The preparation method and applications of a kind of chirality six-membered heterocycle carbene precursor salt

本发明涉及有机合成领域，具体为具有四氢嘧啶骨架的手性六元氮杂环卡宾前体盐的合成及其应用。本发明所述的手性六元氮杂环卡宾前体化合物为具有式(Ⅲ)所示结构的化合物或者其如式(Ⅲ’)所示的对映异构体： R 1 选自苯基、1‑萘基、2‑萘基、苄基、异丙基、异丁基、仲丁基、叔丁基或环己基；R 2 选自氯离子、溴离子、四氟硼酸根离子或六氟磷酸根离子，优选自氯离子和四氟硼酸根离子；R 3 选自氢、1‑萘甲酰基、2‑萘甲酰基、2,4,6‑三甲基苯甲酰基、对甲氧基苯甲酰基或对叔丁基苯甲酰基。本发明开发一种C 2 对称的新型手性六元氮杂环卡宾前体化合物的合成方法，扩大其在药物中间体合成及有机不对称合成反应中的应用范畴。

Organic electroluminescent material and preparation method thereof and organic electroluminescent device

本发明涉及一种有机电致发光材料及其制备方法和有机电致发光器件，有机电致发光材料以苯并[g]屈结构为中心，将第一苯环引入苯并[g]屈结构的g位，然后用第二苯环取代所述第一苯环上的氢基，再用含氮杂环取代所述第二苯环上的氢基，具有如下结构： 其中Ar为具有电子传输功能的含氮杂环；与现有技术相比，本发明中的有机电致发光材料具有非常合适的三重态能级，同时具备较高的玻璃化转变温度、较好的热稳定性和较强的载流子传输能力，并且制备方法简单，操作容易，产量高，成本低，使用该有机电致发光材料作为主体材料代替CBP制作有机电致发光器件，具有更低的启亮电压和更好的最大电流效率，启亮电压可降低0.5‑1.1V，最大电流效率可提高18％‑24％。

One kind efficiently preparing boron hydride ion [RnH4-nB]-Method

本发明公开了一种高效制备硼氢阴离子[R n H 4‑n B] ‑ 的方法，以路易斯酸R n X 3‑n B为催化剂，氢硅烷为还原剂，可将各类卤代硼阴离子铵盐[R` 4 N] + [R n X 4‑n B] ‑ 还原为对应的硼氢阴离子铵盐[R` 4 N] + [R n H 4‑n B] ‑ 。该方法不但可制备BH 4 ‑ 阴离子盐、三苯基硼氢化铵盐[Ph 3 HB] ‑ ，而且还可合成各种其它类型的[R n H 4‑n B] ‑ 硼氢阴离子，适用性广，合成方法简单、高效。本发明为[R n H 4‑n B] ‑ 硼氢阴离子的合成提供新途径。

Isoxazole derivatives as FXR agonists and methods of use thereof

The present invention provides compounds of Formula I: and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising these compounds and methods of using these compounds to treat or prevent a disease or disorder mediated by FXR. Specifically, the present invention relates to isoxazole derivatives useful as agonists for FXR and methods for their preparation and use.

Organic light emitting diode

유기전계발광소자(1)를 제공하고, 양극(20), 음극(80), 및 유기층을 포함하고, 유기층은 정공주입층(30), 정공수송층(40), 전자주입층(70), 전자수송층(60), 발광층(50) 중 적어도 발광층(50)을 포함하는 한 층 또는 다층이고; 발광층(50)은 호스트 물질과 게스트 물질로 구성된 호스트-게스트 도핑 시스템이고, 발광층(50)의 발광구역은 490 내지 750nm이고, 호스트 물질은 식(I) 구조의 화합물을 가지고 있고, 상기 유기전계소자 적색광 및 녹색광은 전계발광효율이 우수하며 색 순도가 탁월할 뿐만 아니라 수명이 긴 장점을 나타낸다. An organic light emitting display device 1 is provided, and includes an anode 20, a cathode 80, and an organic layer, and the organic layer includes a hole injection layer 30, a hole transport layer 40, an electron injection layer 70, and an electron. One layer or a multilayer including at least the light emitting layer 50 among the transport layer 60 and the light emitting layer 50; The light emitting layer 50 is a host-guest doping system composed of a host material and a guest material, the light emitting region of the light emitting layer 50 is 490 to 750 nm, the host material has a compound of formula (I), Red light and green light have excellent electroluminescent efficiency, excellent color purity and long life.

A kind of pyridine derivate and Mannich base combined high temperature acidification corrosion inhibitor

本发明公开了一种吡啶衍生物和曼尼希碱复合高温酸化缓蚀剂，包括10～18重量份的二甲氨基甲基苯丙三氮唑曼尼希碱和10～20重量份的1,3‑二氯化吡啶‑2‑羟基丙烷、3～5重量份的乌洛托品、5～7重量份的增效剂、0.5～1重量份的表面活性剂、2～3重量份的分散剂、40～60重量份的溶剂、3～5重量份的三乙醇胺和5.0～9.0重量份的甲酸；该一种吡啶衍生物和曼尼希碱复合高温酸化缓蚀剂适用于120～160℃，同时兼具优良“性质稳定、缓蚀性能好、易于现场施工与成本优势”的复合缓蚀剂配方，该体系具有与现场常用酸化添加剂配伍性良好、常用的咪唑啉缓蚀剂、其他种类的季铵盐缓蚀剂配伍性良好，可混合使用、施工方便且安全性强、方便运输储存与成本低等特点。

Process for preparing 4-(cyclopropylmethoxy)-n-(3,5-dichloro-1-oxido-4-pyridyl)-5-methoxypyridine-2-carboxamide

본 발명은 화학식 I의 4-(사이클로프로필메톡시)-N-(3,5-디클로로-1-옥시도-4-피리딜)-5-메톡시피리딘-2-카복스아미드를 염기 또는 수화물 형태로 또는 약제학적으로 허용가능한 염의 형태로 제조하기 위한 신규 방법, 및 또한 이 제조 방법에서 유용한 몇몇 신규 합성 중간체에 관한 것이다. [화학식 I]

High-efficiency environment-friendly 2-vinyl pyridine preparation method

本发明公开了一种高效环保的2-乙烯基吡啶的制备方法，该方法以2-羟乙基吡啶和催化剂，在60~160mmHg进行反应蒸馏，不断馏出2-乙烯基吡啶与水的混合液；加入强碱静置分层，得到富2-乙烯基吡啶油层，减压蒸馏，收集30℃~130℃馏分，得到2-羟乙基吡啶终产物。该制备方法，通过大量实验筛选出反应物原料和最佳的用量配比，尤其是通过大量实验筛选出最优的催化剂及其用量，并通过大量实验筛选出反应的最佳反应温度，反应时间和反应压强，整个工艺合理，环境污染小，反应温度低，反应时间短，反应效率高，对设备要求低，生产成本低，收率高，制备得到的2-乙烯基吡啶纯度高，可克服现有技术的诸多不足。

Fluoroelastomer composition

本发明涉及一种氟弹性体组合物，其包含基于偏二氟乙烯的氟弹性体、多羟基化的化合物、碱性化合物、吡啶鎓型盐以及促进剂，所述吡啶鎓型盐具有芳香族环‑季铵化氮原子并且包含至少两个具有中心碳原子(其带有酸性氢原子)的基团；所述氟弹性体组合物具有改善的模制行为，使得成形零件具有较少的起泡和表面缺陷。

Method for preparing 4- (4-amino-3-fluorophenoxy) -N-methylpyridine-2-formamide

本发明涉及一种制备4‑（4‑氨基‑3‑氟苯氧基）‑N‑甲基吡啶‑2‑甲酰胺的方法，该方法包括使4‑氯‑N‑甲基吡啶‑2‑甲酰胺与4‑氨基‑3‑氟苯酚在无机碱的存在下进行反应。本发明选用无机碱取代现有技术中的叔丁醇钾，有效解决了叔丁醇钾在工业化生产中存在的安全隐患问题，而且，本发明在反应结束后，采用析晶法分离得到反应产物，相比于现有技术采用的萃取、浓缩、柱分离纯化等方法，操作更简单，成本更低，而且环境污染小，收率高，非常适合工业化生产。

Compound comprising phenyl pyridine units

하기 화학식 I의 유기 화합물은 광전 소자에 사용될 수 있다: [화학식 I] 상기 식에서, R 1 은, 각각의 경우 독립적으로, C 1 -C 20 지방족 라디칼, C 3 -C 20 방향족 라디칼, 또는 C 3 -C 20 지환족 라디칼이고; R 2 는, 각각의 경우 독립적으로, C 1 -C 20 지방족 라디칼, C 3 -C 20 방향족 라디칼, 또는 C 3 -C 20 지환족 라디칼이고; a는, 각각의 경우 독립적으로, 0 내지 4 범위의 정수이고; b는, 각각의 경우 독립적으로, 0 내지 3 범위의 정수이고; Ar 1 은 직접 결합이거나, 헤테로아릴, 아릴, 알킬 또는 사이클로알킬이고; Ar 2 는 헤테로아릴, 아릴, 알킬 또는 사이클로알킬이고; c는 0, 1 또는 2이고; n은 2 내지 4 범위의 정수이다.

Complexes

본 발명은 화학식 1의 팔라듐(II) 착물 또는 화학식 2의 팔라듐(II) 착물을 제공한다. <화학식 1> <화학식 2> 상기 식에서, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , R 11 , R 12 , R 18 , R 19 , R 20 , R 21 , R 22 , R 23 및 R 24 , m, E 및 X는 명세서에 기재되어 있다. 본 발명은 또한, 착물의 제조 방법, 및 탄소-탄소 및 탄소-헤테로원자 커플링 반응에서의 이들의 용도를 제공한다.

lSOXAZOLE DERIVATIVES AS FXR AGONISTS AND METHODS OF USE THEREOF

The present invention provides compounds of Formula I: (I) and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising these compounds and methods of using these compounds to treat or prevent a disease or disorder mediated by FXR. Specifically, the present invention relates to isoxazole derivatives useful as agonists for FXR and methods for their preparation and use.

Anthracene-containing compound and preparation method and application thereof as well as organic light-emitting device

本发明提供了一种用于荧光主体材料，空穴注入材料或者空穴传输材料蒽类化合物及其应用,和包含有该有机发光化合物的有机发光器件。所述蒽类化合物的分子结构通式为：

Method of preparing benzy 4-amino-3-chloro-5-fluoro-6-(4-chloro-2-fluoro-3-methoxyphenyl)picolinate

A method of preparing benzyl 4-amino-3-chloro-5-fluoro-6-(4-chloro-2-fluoro-3-methoxyphenyl)picolinate (I) from benzyl 4,5-difluoro-6-(4-chloro-2-fluoro-3-methoxyphenyl)picolinate (II) is described. The method includes the use of amination and chlorination process steps to provide the compound of Formula I.

Process for preparing atazanavir bisulfate and novel forms

A process is provided for preparing the HIV protease inhibitor atazanavir bisulfate wherein a solution of atazanavir free base is reacted with concentrated sulfuric acid in an amount to react with less than about 15% by weight of the free base, seeds of Form A crystals of atazanavir bisulfate are added to the reaction mixture, and as crystals of the bisulfate form, additional concentrated sulfuric acid is added in multiple stages at increasing rates according to a cubic equation, to effect formation of Form A crystals of atazanavir bisulfate. A process is also provided for preparing atazanavir bisulfate as Pattern C material. A novel form of atazanavir bisulfate is also provided which is Form E3 which is a highly crystalline triethanolate solvate of the bisulfate salt from ethanol.

Amide addition reaction

A new palladium catalyst, method for its preparation and its use

The invention relates to palladium(0)-tetrakis{tri-[3,5-bis(trifluoromethyl)- phenylj-phosphine} complex of formula (I), as well as to its preparation and use. This compound is outstandingly stable, and can be used as catalyst with excellent results.

Process of manufacture of a compound for inhibiting the activity of shp2, as well as products resulting from acid addition

本發明係關於製造如上所述之具有式I之化合物或其藥學上可接受的 鹽、酸共晶體、水合物或其他溶劑化物之方法，所述方法包括： 根據以下反應方案，使具有式II之化合物與具有式III之化合物反應： 其中在上式中，A係酸的陰離子，LG係脫離基，並且n和m係整數，例如，1、2或3，使得具有式II之化合物係不帶電荷的。 前述反應包括根據以下反應方案使具有式VIII之化合物與具有式IX之化合物反應以得到具有式VII之化合物： 該等部分如說明書和申請專利範圍中所定義。 酸與具有式I之化合物之反應產物，以及所得產物和其特定形式/變型也是本發明。

Manufacturing process for triazine, pyrimidine and pyridine derivatives

The invention relates to a method of manufacturing triazine, pyrimidine and pyridine derivatives of formula (l) wherein U, V, W and Z are nitrogen or carbon atoms, whereby at least one of U, V and W is nitrogen, by condensing a corresponding halo-triazine, pyrimidine or pyridine in a type of Suzuki coupling with a pyridyl- or pyrimidinyl-borane, wherein the amino function is protected as a formamidine. The invention further relates to suitable intermediates and methods of manufacturing of such intermediates. Furthermore the invention relates to pure 5-(4,6-dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine in solid form.

Production of aromatic nitrile

(57)【要約】 （修正有） 【課題】 水と混和しない有機溶剤中において、第三級 アミン塩基の存在下で、対応するアルデヒドをヒドロキ シルアミンの硫酸塩と反応させることによる芳香族ニト リルの製造を提供する。 【解決手段】 式IIのアルデヒドとヒドロキシルアミン の硫酸塩とを、式III、IVまたはＶの第三級アミンの存 在下、１００乃至１６０℃の温度において、反応で遊離 する水を０．０２乃至１．５ｂａｒの範囲において留去 しながら反応させ、アンモニウム塩を除去し、常法によ って式Ｉのニトリルを単離する方法。

A method of synthesizing medicine intermediate phenanthrene compound using copper trifluoromethanesulfcomposite

本发明涉及一种应用三氟甲磺酸铜合成下式(I)所示菲化合物的方法， 所述方法包括：惰性气氛下，在含三氟甲磺酸铜的催化剂、有机配体和碱存在下，于溶剂中，下式(II)化合物与式(III)化合物发生反应，从而得到式(I)化合物； 其中，R 1 、R 2 各自独立地为H、C 1 ‑C 6 烷基、C 1 ‑C 6 烷氧基或卤素；R3为C 6 ‑C 10 芳基或C 5 ‑C 8 杂芳基，所述C 6 ‑C 10 芳基或C 4 ‑C 8 杂芳基任选被1‑3个取代基取代，所述取代基为C 1 ‑C 6 烷基或卤素。所述方法通过合适催化剂、有机配体、碱和溶剂的选择而取得了良好的效果，具备广泛的工业应用前景。

Organic electroluminescent devices

Die Erfindung betrifft ein organisches Elektrolumineszenz-Bauelement, das eine Anode, eine Kathode und eine organische Schicht umfasst, wobei die organische Schicht eine oder mehrere Schichten aus einer Lochinjektionsschicht, einer Lochtransportschicht, einer Elektroneninjektionsschicht, einer Elektronentransportschicht und einer lichtemittierenden Schicht ist und mindestens die lichtemittierenden Schicht umfasst. Die lichtemittierende Schicht ist ein dotiertes Wirt-Gast-System aus Wirtsmaterial und Gastmaterial, der lichtemittierende Bereich der lichtemittierenden Schicht liegt zwischen 490 und 750nm, und das Wirtsmaterial weist eine Verbindung mit der Struktur von Formel (I) auf. Das organische Elektrolumineszenz-Bauelement emittiere rotes Licht oder grünes Licht und weist die Vorteile von hohem lichtemittierenden Wirkungsgrad, ausgezeichneter Farbreinheit und langer Lebensdauer auf. The invention relates to an organic electroluminescent device comprising an anode, a cathode and an organic layer, wherein the organic layer is one or more layers of a hole injection layer, a hole transport layer, an electron injection layer, an electron transport layer and a light emitting layer and at least the light emitting Layer includes. The light-emitting layer is a doped host-guest system of host material and guest material, the light-emitting region of the light-emitting layer is between 490 and 750 nm, and the host material has a compound having the structure of formula (I). The organic electroluminescent device emits red light or green light and has the advantages of high light-emitting efficiency, excellent color purity and long life.

Process for preparing atazanavir bisulfate and novel forms

Fluorine-containing negative ion room temperature ionic liquid and preparation method thereof

本发明涉及一种新型含氟负离子的室温离子液体及其制备方法，其特征在于制备了阴离子为氟离子的室温离子液体，具有离子液体和氟负离子的双重功能，既有离子液体的绿色溶剂和催化剂功能，又可作为氟离子来源参与氟代反应。该发明的含氟离子液体制备方法简单，成本低，拓展了离子液体的种类，同时提供了一种高效的氟负离子来源，可作为溶剂、催化剂、氟化剂等广泛应用于氟代反应、离子聚合等反应中。

A kind of device and method of synthesis 2,2 bipyridyls

本发明公开了一种合成2,2‑联吡啶装置及方法，属于精细化工领域。该装置包括预热器、反应器、出料装置，其中反应器内部从上到下依次是液体分布器、催化剂床层、催化剂托板及卸催化剂装置、气体分布器，出料装置包括调节阀，后处理装置即蒸发器。其工艺为吡啶通过预热器进入到反应器，经过液体分布器，均匀的洒到催化剂床层，然后反应过后通过调节阀，出料，未反应的吡啶经过蒸发器蒸馏回收套用，蒸出吡啶后的残留物即为2,2‑联吡啶。

Process for preparing atazanavir bisulfate and novel forms

본 발명은 아타자나비르 유리 염기의 용액을 아타자나비르 유리 염기의 약 15 중량％ 미만과 반응하는 양의 진한 황산과 반응시키고, 아타자나비르 비술페이트 형태의 결정으로서 아타자나비르 비술페이트의 형태 A 결정의 시드를 반응 혼합물에 첨가하고, 추가의 진한 황산을 다단계에서 3차 방정식에 따른 증가 속도로 첨가하여 아타자나비르 비술페이트의 형태 A 결정의 형성을 수행하는, HIV 프로테아제 저해제 아타자나비르 비술페이트를 제조하는 방법에 관한 것이다. 본 발명은 또한 아타자나비르 비술페이트를 패턴 C 물질로서 제조하는 방법에 관한 것이다. 본 발명은 또한 형태 E3인 아타자나비르 비술페이트의 신규 형태에 관한 것이며, 이는 에탄올로부터의 비술페이트 염의 고도로 결정질인 트리에탄올레이트 용매화물이다. 아타자나비르 비술페이트, HIV 프로테아제 저해제

A kind of Phosphine ligands of the structure containing benzofuran and its preparation method and application

本发明公开一种含苯并呋喃结构的膦配体及其制备方法和应用，该膦配体是具有式（Ⅰ）所示化学结构式的化合物或它的对映体或消旋体。本发明的膦配体引进了呋喃环，其芳香环的电子云密度增大，空间位阻改变，从而使得该膦配体应用在钯催化的Suzuki‑Miyaura模型反应中具有反应活性好、收率高达99%的特点。本发明含苯并呋喃结构的膦配体，其合成方法简单，成本低廉，适用于多种底物的钯催化Suzuki‑Miyaura反应。

Organic electroluminescent device

本发明涉及一种有机电致发光器件，包含阳极，阴极，和有机层，所述有机层为空穴注入层、空穴传输层、电子注入层、电子传输层、发光层中至少包括发光层在内的一层或多层；所述发光层为由主体材料和客体材料组成的主客体掺杂体系，发光层的发光区域为490-750nm，所述主体材料具有式(I)所述结构的化合物，该有机电致器件发红光或绿光，具有电致发光效率良好和色纯度优异以及寿命长的优点。

A kind of bipyridyl gemini quaternary ammonium salt corrosion inhibiter and preparation method and application

一种联吡啶双子季铵盐缓蚀剂及此类化合物的制备方法，此类缓蚀剂的结构特点是在4,4‑联吡啶的两端通过季铵化反应连接了长度不同的碳链，该缓蚀剂的制备方法为：以4,4‑联吡啶和氯代十二烷为原料，溶于有机溶剂后，在40～80℃的条件下，经季铵化反应制备而得，该发明的有益效果在于，这类缓蚀剂的制备方法涉及的原料廉价易得，反应条件温和，合成步骤简单。同时其具有良好的缓蚀性能，在40ppm用量下，缓蚀率均可达到96％以上，缓蚀时间长且稳定性好，安全高效，适用于大规模应用。

Method for synthesizing pharmaceutical intermediate phenanthrene compound in sodium hydroxide environment

本发明涉及一种氢氧化钠环境下合成下式(I)所示菲化合物的方法， 所述方法包括：惰性气氛下，在催化剂、有机配体和氢氧化钠存在下，于溶剂中，下式(II)化合物与式(III)化合物发生反应，从而得到式(I)化合物； 其中，R 1 、R 2 各自独立地为H、C 1 ‑C 6 烷基、C 1 ‑C 6 烷氧基或卤素；R3为C 6 ‑C 10 芳基或C 5 ‑C 8 杂芳基，所述C 6 ‑C 10 芳基或C 4 ‑C 8 杂芳基任选被1‑3个取代基取代，所述取代基为C 1 ‑C 6 烷基或卤素。所述方法通过合适催化剂、有机配体、碱和溶剂的选择而取得了良好的效果，具备广泛的工业应用前景。

Preparation method of 9-di (3-pyridine) ethylene-fluorene with aggregation-induced emission effect

本发明公开了具有聚集诱导发光效应的9‑二(3‑吡啶)乙烯‑芴的制备方法。将9‑芴酮、四溴化碳和三苯基膦加入二氯甲烷中加热搅拌反应，反应结束后采用柱层析法分离，重结晶得到黄色9‑二溴乙烯‑芴；将9‑二溴乙烯‑芴、3‑吡啶硼酸、无水碳酸钠、三苯基膦和醋酸钯加入1,4‑二氧六环与水的混合溶液中加热搅拌反应，反应结束后用乙酸乙酯萃取收集有机层，用无水硫酸钠干燥，减压旋蒸，采用柱层析法分离得到粗产物，再用乙酸乙酯洗涤得到淡黄色产物9‑二(3‑吡啶)乙烯‑芴。本发明的优点为：制备方法简单，产率高，反应活性好，产物具有明显的聚集诱导发光效应，是一种具有广泛应用价值的新材料。

method for synthesizing 1, 2-disubstituted olefin compound by alkyne alkylation

本发明公开了一种炔烃高选择性烷基化合成1,2‑二取代烯烃类化合物的方法，所述的方法具体按如下步骤进行：将光敏剂、式I所示炔烃化合物、汉斯酯加入Schlenk反应管中，在保护气体气氛下，再将式II所示的醛和仲胺溶解于有机溶剂或1,4‑二氧六环与水的混合溶剂中得到混合液，在保护气体条件下，将所述的混合液加入到所述的Schlenk反应管中，在光源照射下，于25℃搅拌反应6～14小时(优选为12小时)，得到反应液经后处理得到式III所示的1,2‑二取代烯烃类化合物。本发明所述的方法可以合成现存的方法难以制备的多取代烯烃，具有反应的立体选择性高；催化剂价廉易得，毒性较低；反应条件较温和，节约能源消耗；产率高，底物普适性强，操作简便等优点。

Preparation method of amantadine

本发明公开了一种金刚烷胺的制备方法，属于有机化学合成技术领域，其特征在于：以化合物金刚烷为起始原料，在乙腈和聚离子液体PIL催化剂以及硫酸的存在下，生成中间体1‑乙酰氨基金刚烷，然后在醇和碱的体系下水解成金刚烷胺；本发明的制备方法，绿色环保、后处理方便，催化剂聚离子液体大大降低了硫酸和乙腈的用量，后处理简单。离子液催化剂可回收再利用，大大节约了成本，适合大规模工业化生产。