[Synthesis of N alpha-(benzoylglycyl)- and N alpha-(benzyloxycarbonylglycyl)-4-amidinophenylalanine amides as thrombin inhibitors].

The 4-nitrophenyl esters of hippuric acid and benzyloxycarbonylglycine had been aminolyzed by racemic 4-cyanphenylalanine into the compounds 3 and 4. After activation as 4-nitrophenyl esters and following reaction with amines the amides 7-14 were formed. These cyano compounds were converted into the amidines via the thioamides 15-22 and the thioimidic esters 23-30. The piperidide 35 was most effective against thrombin.