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    Process for the preparation of 4,4-dimethyl-6-ethynylthiochroman
    2.
    发明申请
    Process for the preparation of 4,4-dimethyl-6-ethynylthiochroman 失效
    制备4,4-二甲基-6-乙炔基二氢苯并噻喃的方法

    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。

    Amorphous pregabalin and process for the preparation thereof
    3.
    发明申请
    Amorphous pregabalin and process for the preparation thereof 审中-公开
    无定形普瑞巴林及其制备方法

    公开(公告)号：US20080014280A1

    公开(公告)日：2008-01-17

    申请号：US11879405

    申请日：2007-07-17

    申请人： Bobba Kumar ,  Girish Dixit

    发明人： Bobba Kumar ,  Girish Dixit

    IPC分类号： A61K9/14 ,  A61K31/195 ,  C07C205/51

    CPC分类号： C07C229/08 ,  A61K9/14 ,  A61K9/19 ,  A61K31/195

    摘要： Pregabalin substantially in an amorphous form is disclosed. A composition comprising amorphous pregabalin in a solid form, wherein at least about 80% by weight of the solid is amorphous pregabalin in an amorphous form is also disclosed. The present invention also provides a process for preparing amorphous pregabalin substantially in an amorphous form by providing a solution of amorphous pregabalin in one or more solvents capable of dissolving the pregabalin and substantially removing the solvent from the solution.

    摘要翻译： 公布了基本上为无定形形式的普瑞巴林。 包含固体形式的无定形普瑞巴林的组合物，其中至少约80重量％的固体是无定形形式的无定形普瑞巴林。 本发明还提供了通过在一种或多种能够溶解普瑞巴林并基本上从溶液中除去溶剂的溶剂中提供无定形普瑞巴林溶液来制备基本上为无定形形式的无定形普瑞巴林的方法。

    Process for the preparation of disubstituted acetylenes bearing heteroaromatic and heterobicyclic groups
    5.
    发明申请
    Process for the preparation of disubstituted acetylenes bearing heteroaromatic and heterobicyclic groups 审中-公开

    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.

    Process for the preparation of crystalline form II of clarithromycin
    7.
    发明申请
    Process for the preparation of crystalline form II of clarithromycin 审中-公开
    制备克拉霉素晶型II的方法

    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。