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    RESOLUTION OF RACEMATES OF METHYL ALPHA-5- 4,5,6,7-TETRAHYDR O 3,2-C THIENOPYRIDYL -(2-CHLOROPHENIL)ACETATE
    1.
    发明公开
    RESOLUTION OF RACEMATES OF METHYL ALPHA-5- 4,5,6,7-TETRAHYDR O 3,2-C THIENOPYRIDYL -(2-CHLOROPHENIL)ACETATE 审中-公开
    （2-氯苯基）乙酸甲酯 - ALPHA -5- [4,5,6,7-四氢[3,2-C]噻吩并吡啶]裂解外消旋体

    公开(公告)号：EP1718654A1

    公开(公告)日：2006-11-08

    申请号：EP05706478.4

    申请日：2005-02-10

    申请人： Apotex Pharmachem Inc.

    发明人： MURTHY, Keshava, K.S. ,  BEJAN, Elena ,  WEERATUNGA, Gamini

    IPC分类号： C07D495/04

    CPC分类号： C07D495/04

    摘要： A process for the resolution of each of the (R) and (S)enantiomers of methyl-α-5-[4,5,6,7­tetra hydro[3,2-c]thienopyridyl]-(2-chlorophenyl)acetate and salts thereof by diastereomeric crystallization comprising the use of a single optically active resolving agent and at least one solvent. The isolated (R)- enantiomer can be further recemized and resolved in the same manner to maximize the recovery of the (S)- enantiomer. The isolated enantiomers can be recrystallized in an organic solvent to an enantiomeric purity of 99.5% or higher.

    AN IMPROVED PREPARATION OF ATORVASTATIN
    2.
    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.