PROCESS FOR PREPARATION OF ENANTIOMERICALLY ENRICHED CYCLIC Β-ARYL OR HETEROARYL CARBOXYLIC ACIDS

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.