Propionamide antitumor agents

摘要

The present invention encompasses compounds of the formula <IMAGE> AND THE PHARMACEUTICALLY ACCEPTABLE ACID ADDITION SALTS THEREOF WHEREIN R represents hydrogen or hydroxymethyl. The compounds of the present invention are prepared by condensing N-carbobenzyloxyserine or 2-carbobenzyloxyamino-3-hydroxy-2-hydroxymethylpropionic acid with p-[N,N-bis(2-chloroethyl)]phenylenediamine hydrochloride and removing the carbobenzyloxy protecting group by catalytic hydrogenation. These compounds are useful as cytotoxic agents, in particular, antitumor agents.