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    AN IMPROVED PROCESS FOR THE PREPARATION OF ATORVASTATIN AND INTERMEDIATES
    1.
    发明公开
    AN IMPROVED PROCESS FOR THE PREPARATION OF ATORVASTATIN AND INTERMEDIATES 审中-公开
    一种用于阿托伐他汀和中间体的制备过程

    公开(公告)号：EP1853559A1

    公开(公告)日：2007-11-14

    申请号：EP06705198.7

    申请日：2006-02-21

    申请人： Apotex Pharmachem Inc.

    发明人： FAUGHT, Jody ,  CHOW, Alan ,  WANG, Fan ,  CHE, Daqing ,  GUNTOORI, Bhaskar Reddy ,  ZHAO, Yajun ,  KINSMAN, Aaron, C.

    IPC分类号： C07D207/34

    CPC分类号： C07D207/34

    摘要： A process is provided for preparing (R)-5-[2-(4-fluorophenyl)-5-(l- methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-lH-pyrrol-l-yl]-5-hydroxy-3-oxo- 1-heptanoic acid, R-substituted ester 9 comprising: (a) reacting 5-(4-fluorophenyl)-2-(l -methylethyl)-l -(3-oxopropyl)-N,4- diphenyl-lH-pyrrole-3-carboxamide, 1, with the enolate form of (S)-2- hydroxy- 1 ,2,2-triphenylethyl acetate substituent in a chelating co- solvent; (b) hydrolysis of (R,S)-5-[2-(4-fluorophenyl)-5-(l -methylethyl)-3-phenyl- 4-[(phenylamino)carbonyl]- 1 H-pyrrol- 1 -yl]-3-hydroxy- 1 -pentanoic acid, (S)-2 -hydroxy- 1 ,2,2-triphenylethyl ester (2a and 2b) using a base, preferably an alkali metal base, preferably in a solvent to form the (R,S)-5-[2-(4-fluorophenyl)-5-(l -methylethyl)-3-phenyl-4- [(phenylamino)carbonyl]- 1 H-pyrrol- 1 -yl]-3 -hydroxy- 1 -pentanoic acid, 7; (c) treating the carboxylic acid 7 with a chiral base to form a salt and purifying the salt to obtain enantiomerically enriched (R)-7 chiral base salt; (d) alkylation of the (R)-7 chiral base salt or the free acid derived from (R)-7, forming (R)-5-[2-(4-fluorophenyl)-5-(l-methylethyl)-3-phenyl- 4-[(phenylamino)carbonyl]-lH-pyrrol-l-yl]-5-hydroxy-3-oxo-l- heptanoic acid, R-substituted ester 9, wherein the R substituent is a Cl to C6 alkyl, C6 to C9 aryl or C7 to Cl0 aralkyl. Subsequently, R-substituted ester 9 may be converted into atorvastatin calcium 6 based on procedures known in the art.

    FORMS OF DEXLANSOPRAZOLE AND PROCESSES FOR THE PREPARATION THEREOF
    2.
    发明公开
    FORMS OF DEXLANSOPRAZOLE AND PROCESSES FOR THE PREPARATION THEREOF 审中-公开
    DEXLANSOPRAZOL和用于生产过程的表格

    公开(公告)号：EP2467375A1

    公开(公告)日：2012-06-27

    申请号：EP10809403.8

    申请日：2010-08-19

    申请人： Apotex Pharmachem Inc.

    发明人： WANG, Fan ,  KELLS, Kevin W. ,  MILNES, Kaarina ,  MCPHAIL, Cameron L.

    IPC分类号： C07D401/12 ,  A61K31/4439 ,  A61K47/10

    CPC分类号： C07D401/12 ,  A61K31/4439 ,  C07D235/28

    摘要： Provided is dexlansoprazole propylene glycolate hydrate. Polymorphic forms thereof are also provided. The dexlansoprazole propylene glycolate hydrate maybe such that the propylene glycol component is present in approximately equal proportions of (R) absolute configuration and (S) absolute configuration, or present in predominantly (R) absolute configuration, or predominantly (S) absolute configuration. Salts of dexlansoprazole are also provided. In particular, crystalline dexlansoprazole isopropylammonium salt and crystalline MTBE solvate of dexlansoprazole t-butylammonium salt are provided. Pharmaceutical formulations comprising dexlansoprazole propylene glycolate hydrate are also provided. Furthermore, processes for preparation of dexlansoprazole propylene glycolate hydrate are provided.

    AN IMPROVED PREPARATION OF ATORVASTATIN
    4.
    发明公开
    AN IMPROVED PREPARATION OF ATORVASTATIN 审中-公开
    阿托伐他汀提高生产

    公开(公告)号：EP1725527A1

    公开(公告)日：2006-11-29

    申请号：EP05714608.6

    申请日：2005-03-11

    申请人： Apotex Pharmachem Inc.

    发明人： GUNTOORI, Bhaskar, Reddy ,  CHE, Daqing ,  WANG, Fan ,  ZHAO, Yajun ,  MURTHY, Keshava, K.S. ,  HORNE, Stephen, E.

    IPC分类号： C07D207/416 ,  C07D207/34

    CPC分类号： C07D207/416 ,  C07D207/34

    摘要： A process for preparing (R)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4­[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-5-hydroxy-3-oxo-l-heptanoic acid, tert-butylester comprising: (a) reduction of 5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4­[(phenylamino)carbonyl]-1H-pyrrol-l-yl]-3-oxo-l-pentanoic acid, (R)-2-hydroxy­1,2,2-triphenylethyl ester; (b) hydrolysis of (R)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4­[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-3-hydroxy-l-pentanoic acid, (R)-2­hydroxy-1,2,2-triphenylethyl ester using an alkali base in a solvent to form the acid; (c) alkylation of the acid forming (R)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3­phenyl-4-[(phenylamino)carbonyl]-1 H-pyrrol-1-yl]-5-hydroxy-3-oxo- l -heptanoic acid, tert-butylester.

    A NOVEL PROCESS FOR THE PREPARATION OF ESOMEPRAZOLE AND SALTS THEREOF
    6.
    发明公开
    A NOVEL PROCESS FOR THE PREPARATION OF ESOMEPRAZOLE AND SALTS THEREOF 审中-公开
    新工艺用于生产埃索美拉唑及其盐类

    公开(公告)号：EP2035410A1

    公开(公告)日：2009-03-18

    申请号：EP07719921.4

    申请日：2007-06-08

    申请人： Apotex Pharmachem Inc.

    发明人： WANG, Fan ,  MONTEMAYOR, Laura, Kaye ,  CHE, Daqing ,  HORNE, Stephen, E.

    IPC分类号： C07D401/12

    CPC分类号： C07D401/12 ,  Y02P20/55

    摘要： A novel process for the preparation of omeprazole and its enantiomers, such as esomeprazole, as well as the preparation of related 2-(2-pyridinylmethyl-sulphinyl)-1H-benzimidazoles, including pantoprazole, lansoprazole and rabeprazole, as recemates or single enantiomers, and their alkali or alkaline salts has been developed. The novel process involves the surprising discovery that protection of the free-base benzimidazole sulfoxide (e.g. omeprazole or esomeprazole), by reaction with an alkyl, aryl or aralkyl chloroformate following oxidation of the corresponding sulfide, eliminates the need for its direct isolation. Subsequent removal of the protecting group with a solution of alkali or alkaline earth alkoxide in a C1-C4 alcohol directly provides the corresponding salt. By eliminating the need to handle the free-base benzimidazole sulfoxide, this advantageous procedure provides increased chemical yields over processes described in the art.