公开(公告)号：US20050004373A1

公开(公告)日：2005-01-06

申请号：US10883880

申请日：2004-07-02

申请人： Bobba Kumar ,  Vishvas Patil ,  Changdev Raut ,  Shekhar Bhirud ,  Batchu Chandrasekhar

发明人： Bobba Kumar ,  Vishvas Patil ,  Changdev Raut ,  Shekhar Bhirud ,  Batchu Chandrasekhar

IPC分类号： C07D335/06

CPC分类号： C07D335/06

摘要： An improved process for the preparation of key intermediates for tazarotene, 4,4-dimethyl-6-ethynylthiochroman, is provided comprising (a) reacting 4,4-dimethyl-6-acetylthiochroman of the formula with an acid chloride and an amido-group containing compound of the general formula wherein R is hydrogen or a hydrocarbyl of from 1 to 15 carbon atoms and R1 and R2 can be the same or different and are hydrocarbyls of from 1 to 15 carbon atoms or R1 and R2 together with the nitrogen atom to which they are bonded are joined together to form a heterocyclic group, optionally containing one or more additional heterocyclic atoms, or one of R1 and R2 together with the nitrogen atom to which it bonded are joined together with the carbonyl radical to form a heterocyclic group, optionally containing one or more additional heterocyclic atoms to form a β-chloro vinyl carbonyl compound intermediate of the general formula wherein R has the aforestated meanings; and (b) reacting the β-chloro vinyl carbonyl compound intermediate with an alkali metal to provide the 4,4-dimethyl-6-ethynylthiochroman.

摘要翻译： 提供了一种用于制备他扎罗汀4,4-二甲基-6-乙炔基二氢苯并噻喃的关键中间体的改进方法，其包括（a）使下式的4,4-二甲基-6-乙酰基二氢苯并二氢吡喃与酰氯和酰氨基 其中R是氢或1至15个碳原子的烃基，R 1和R 2可以相同或不同，并且是具有1至15个碳原子的烃基或R 1 >和R 2与它们所键合的氮原子一起连接在一起形成杂环基，任选地含有一个或多个另外的杂环原子，或者R 1和R 2中的一个与氮一起 其键合的原子与羰基结合在一起形成杂环基，任选地含有一个或多个另外的杂环原子以形成通式其中R具有上述含义的β-氯乙烯基羰基化合物中间体; 和（b）使β-氯乙烯基羰基化合物中间体与碱金属反应，得到4,4-二甲基-6-乙炔基二氢苯并噻喃。

公开(公告)号：US20070238881A1

公开(公告)日：2007-10-11

申请号：US11784496

申请日：2007-04-06

申请人： Bobba KUMAR ,  Pravin KULKARNI ,  Changdev RAUT ,  Sanjay VAIDYA ,  Nitin PRADHAN

发明人： Bobba KUMAR ,  Pravin KULKARNI ,  Changdev RAUT ,  Sanjay VAIDYA ,  Nitin PRADHAN

IPC分类号： C07D409/02

CPC分类号： C07D409/06

摘要： The present invention provides a novel intermediate of ethyl 6-[2-(4,4-dimethylthiochroman-6-yl)ethynyl] nicotinate or a pharmaceutically acceptable salt thereof and a process for its preparation. The present invention also provides for the preparation of ethyl 6-[2-(4,4-dimethylthiochroman-6-yl)ethynyl] nicotinate of Formula I or a pharmaceutically acceptable salt thereof using the intermediate.

摘要翻译： 本发明提供6- [2-（4,4-二甲基二氢苯并噻喃-6-基）乙炔基]烟酸乙酯或其药学上可接受的盐的新型中间体及其制备方法。 本发明还提供使用该中间体制备式I的6- [2-（4,4-二甲基二氢苯并噻喃-6-基）乙炔基]烟酸酯或其药学上可接受的盐。

公开(公告)号：US20060106233A1

公开(公告)日：2006-05-18

申请号：US11155847

申请日：2005-06-17

申请人： Bobba Kumar ,  Shekhar Bhirud ,  Batchu Chandrasekhar ,  Changdev Raut

发明人： Bobba Kumar ,  Shekhar Bhirud ,  Batchu Chandrasekhar ,  Changdev Raut

IPC分类号： C07D335/06 ,  C07D215/60

CPC分类号： C07D335/06

摘要： A process for the preparation of a disubstituted acetylene bearing heteroaromatic and heterobicyclic groups of formula I is provided wherein X is S, O, or NR1 wherein R1 is hydrogen or a C1-C6 straight or branched alkyl group; R is hydrogen or a C1-C6 straight or branched alkyl group; A is a substituted or unsubstituted pyridinyl, thienyl, furyl, pyridazinyl, pyrimidinyl or pyrazinyl group; n is 0-4; and B is H, —COOH, —CH2OH, —CHO or a C1-C6 alkyl acetal derivative, —COR2 or a C1-C6 alkyl ketal derivative where R2 is —(CH2)mCH3 where m is 0-4 or COOR3 wherein R3 is a straight or branched C1-C30 alkyl group, a substituted or unsubstituted C6-C30 aromatic group, a substituted or unsubstituted C3-C30 cycloalkyl, a substituted or unsubstituted C3-C30 cycloalkylalkyl, a substituted or unsubstituted C3-C30 cycloalkenyl, a substituted or unsubstituted C5-C30 aryl, a substituted or unsubstituted C5-C30 arylalkyl, a substituted or unsubstituted C5-C30 heteroaryl, a substituted or unsubstituted C3-C30 heterocyclic ring, a substituted or unsubstituted C4-C30 heterocyclylalkyl, a substituted or unsubstituted C6-C30 heteroarylalkyl, the process comprising a Sonogashira coupling reaction between a compound of formula II wherein X and R have the aforestated meanings, with a compound of formula III X′-A-(CH2)n—B  (III) wherein X′ is a halogen and A, n and B have the aforestated meanings, in the presence of a base and a transition metal catalyst and in a polar aprotic solvent.

公开(公告)号：US20050240029A1

公开(公告)日：2005-10-27

申请号：US11158856

申请日：2005-06-22

申请人： Bobba Venkata Kumar ,  Vishvas Patil ,  Changdev Raut ,  Shekhar Bhirud ,  Batchu Chandrasekhar

发明人： Bobba Venkata Kumar ,  Vishvas Patil ,  Changdev Raut ,  Shekhar Bhirud ,  Batchu Chandrasekhar

IPC分类号： C07D335/06 ,  C07D335/04 ,  A61K31/382

CPC分类号： C07D335/06

摘要： An improved process for the preparation of key intermediates for tazarotene, 4,4-dimethyl-6-ethynylthiochroman, is provided comprising (a) reacting 4,4-dimethyl-6-acetylthiochroman of the formula with an acid chloride and an amido-group containing compound of the general formula wherein R is hydrogen or a hydrocarbyl of from 1 to 15 carbon atoms and R1 and R2 can be the same or different and are hydrocarbyls of from 1 to 15 carbon atoms or R1 and R2 together with the nitrogen atom to which they are bonded are joined together to form a heterocyclic group, optionally containing one or more additional heterocyclic atoms, or one of R1 and R2 together with the nitrogen atom to which it bonded are joined together with the carbonyl radical to form a heterocyclic group, optionally containing one or more additional heterocyclic atoms to form a chloro vinyl carbonyl compound intermediate of the general formula wherein R has the aforestated meanings; and (b) reacting the β-chloro vinyl carbonyl compound intermediate with an alkali metal to provide the 4,4-dimethyl-6-ethynylthiochroman.

摘要翻译： 提供了一种用于制备他扎罗汀4,4-二甲基-6-乙炔基二氢苯并噻喃的关键中间体的改进方法，其包括（a）使下式的4,4-二甲基-6-乙酰基二氢苯并二氢吡喃与酰氯和酰氨基 其中R是氢或1至15个碳原子的烃基，R 1和R 2可以相同或不同，并且是烃基的通式 1至15个碳原子或R 1和R 2与它们所键合的氮原子一起连接在一起形成杂环基，任选地含有一个或多个 另外的杂环原子或R 1和R 2中的一个与其键合的氮原子一起与羰基连接在一起形成杂环基，任选地含有 一个或多个另外的杂环原子以形成通式的氯乙烯基羰基化合物中间体，其中R具有af ;意 和（b）使β-氯乙烯基羰基化合物中间体与碱金属反应，得到4,4-二甲基-6-乙炔基二氢苯并噻喃。

公开(公告)号：US20070043085A1

公开(公告)日：2007-02-22

申请号：US11507284

申请日：2006-08-21

申请人： Bobba Kumar ,  Pravin Kulkarni ,  Anil Suryawanshi ,  Changdev Raut ,  Nitin Pradhan

发明人： Bobba Kumar ,  Pravin Kulkarni ,  Anil Suryawanshi ,  Changdev Raut ,  Nitin Pradhan

IPC分类号： A61K31/4439 ,  C07D403/02

CPC分类号： C07D401/12

摘要： A process for preparing neutral esomeprazole in an amorphous form is provided comprising (a) providing an aqueous solution comprising a salt of esomeprazole; (b) neutralizing the solution with a neutralization agent to provide a neutralized solution; (c) contacting the neutralized solution with an extracting solvent; and (d) recovering the neutral esomeprazole in an amorphous form.

摘要翻译： 提供了一种制备无定形形式的中性艾美拉唑的方法，包括（a）提供包含艾美拉唑盐的水溶液; （b）用中和剂中和溶液以提供中和的溶液; （c）使中和的溶液与提取溶剂接触; 和（d）以无定形形式回收中性埃索美拉唑。

公开(公告)号：US20060111560A1

公开(公告)日：2006-05-25

申请号：US11264835

申请日：2005-11-01

申请人： Bobba Kumar ,  Changdev Raut ,  Shekhar Bhirud

发明人： Bobba Kumar ,  Changdev Raut ,  Shekhar Bhirud

IPC分类号： C07H17/08

CPC分类号： C07H17/08

摘要： A process for preparing Form II crystals of clarithromycin is provided comprising (a) treating clarithromycin with a carboxylic acid in an organic solvent to provide a clarithromycin acid salt; and, (b) heating the clarithromycin acid salt at a temperature capable of providing Form II crystals of clarithromycin.

摘要翻译： 提供了一种制备克拉霉素II型晶体的方法，包括（a）在有机溶剂中用羧酸处理克拉霉素以提供克拉霉素酸盐; 和（b）在能够提供克拉霉素II型晶体的温度下加热克拉霉素酸盐。