Process for the preparation of N2-substituted L-argininamides

摘要

N<2>-Substituted L-argininamides of the formula I in which the symbols have the meaning stated in the claims are highly specific thrombin inhibitors. They are suitable for the treatment or prophylaxis of thrombophilic diatheses. The compounds of the formula I are prepared by a) reacting an appropriate L-argininamide of the formula V with a sulphonyl halide of the formula R'SO2X in the presence of a base, or b) reacting an N<2>-substituted L-arginyl halide of the formula X with an amine of the formula R-H, or c) reacting an N<2>-substituted L-arginine ester of the formula XII with an amine of the formula R2NH2 and, where appropriate, converting the compound obtained as in a), b) or c) into a salt with an acid.