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    PROCESS FOR PREPARATION OF ENANTIOMERICALLY ENRICHED CYCLIC BETA-ARYL OR HETEROARYL CARBOXYLIC ACIDS
    8.
    发明公开
    PROCESS FOR PREPARATION OF ENANTIOMERICALLY ENRICHED CYCLIC BETA-ARYL OR HETEROARYL CARBOXYLIC ACIDS 有权
    制备富含环氧化物的芳基或杂芳基羧酸的方法

    公开(公告)号：EP2029541A1

    公开(公告)日：2009-03-04

    申请号：EP07727328.2

    申请日：2007-03-26

    申请人： F. Hoffmann-La Roche AG

    发明人： BACHMANN, Stephan ,  SCALONE, Michelangelo ,  SCHNIDER, Patrick

    IPC分类号： C07D211/60 ,  C07D207/16

    CPC分类号： C07C51/36 ,  C07D207/16 ,  C07D211/60 ,  C07D401/04

    摘要： The present invention relates to a process for the preparation of cis substituted cyclic β- aryl or heteroaryl carboxylic acid derivatives in high diastereo- and enantioselectivity by enantioselective hydrogenation in accordance with the following scheme (Formula I, II) wherein X is -C(R)(R')-, -N(R')-, -O-, -S(O)0-, C(O)N(R'), -N(R')C(O)- or -C(O)-; R and R' are independently from each other hydrogen, C1-7-alkyl, C1-7-alkyl substituted by halogen, C1-7-alkoxy, hydroxy or -(CH2)P-Ar; R' is hydrogen, C1-7-alkyl, C1-7-alkyl substituted by halogen, -S(O)0-C1-7-alkyl, -S(O)0-Ar, -S(O)0-NRR', -(CH2)P-Ar, -C(O)-C1-7-alkyl, -C(O)-Ar, -C(O)-NRR' or -C(O)O-C1-7-alkyl; Ar is aryl1 or heteroaryl1; n is 0, 1, 2 or 3; m is 0, 1, 2 or 3; o is 0, 1 or 2; p is 0, 1, or 2; and corresponding salts thereof.

    摘要翻译： 本发明涉及根据下列方案（式I，II）通过对映选择性氢化制备高非对映异构体和对映选择性的顺式取代环β-芳基或杂芳基羧酸衍生物的方法，其中X是-C（R （R'） - ， - N（R'） - ， - O - ， - S（O）O-，C（O）N（R'）， C（O） - ; R和R'彼此独立地为氢，C 1-7 - 烷基，被卤素，C 1-7 - 烷氧基，羟基或 - （CH 2）p -Ar取代的C 1-7 - 烷基; R'为氢，C 1-7 - 烷基，被卤素取代的C 1-7 - 烷基，-S（O）0 -C 1-7 - 烷基，-S（O）0 -Ar，-S（O）0 -NRR （O）-C 1-7 - 烷基，-C（O）-Ar，-C（O）-NRR'或-C（O）O-C 1-7 - 烷基; Ar是芳基1或杂芳基1; n是0,1,2或3; m是0,1,2或3; o是0,1或2; p是0,1或2; 及其相应的盐。

    PROCESS FOR THE PREPARATION OF CHIRAL PROPIONIC ACID DERIVATIVES
    9.
    发明授权
    PROCESS FOR THE PREPARATION OF CHIRAL PROPIONIC ACID DERIVATIVES 有权
    用于生产手性丙酸

    公开(公告)号：EP1670792B1

    公开(公告)日：2007-12-19

    申请号：EP04765444.7

    申请日：2004-09-21

    申请人： F. HOFFMANN-LA ROCHE AG

    发明人： PUENTENER, Kurt ,  SCALONE, Michelangelo

    IPC分类号： C07D413/12

    CPC分类号： C07D413/12

    摘要： The present invention is concerned with a novel process for the preparation of compounds of formula (I) comprising catalytic asymmetric hydrogenation of a compound of formula (II) in the presence of a catalyst comprising ruthenium and a chiral diphosphine ligand or comprising rhodium and a chiral diphosphine ligand, wherein R1, R2, R3 and R4 are as defined in the specification and claims. The compounds of formula (I) and the corresponding salts and/or esters are pharmaceutically active substances.