Process for preparation of enantiomerically enriched cyclic beta-aryl or heteroaryl carboxylic acids

摘要

The present invention relates to a process for the preparation of cis substitutedcyclic β- aryl or heteroaryl carboxylic acid derivatives in high diastereo-and enantioselectivity by enantioselective hydrogenation in accordance withthe 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' areindependently from each other hydrogen, C-alkyl, C-alkylsubstituted by halogen, C-alkoxy, hydroxy or -(CH)-Ar;R" is hydrogen, C-alkyl, C-alkyl substitutedby halogen, -S(O)-C-alkyl, -S(O)-Ar,-S(O)-NRR', -(CH)-Ar, -C(O)-C-alkyl,-C(O)-Ar, -C(O)-NRR' or -C(O)O-C-alkyl; Ar is arylor heteroaryl; n is 0, 1, 2 or 3; m is 0, 1, 2 or 3; o is 0, 1 or 2; p is 0, 1, or2; and corresponding salts thereof.