Preparation of the Key Intermediate in a Novel Synthesis of ZD9063P: The Chemical Component of ADEPT, a Targeted Cytotoxic Therapy

摘要

A novel regioselective opening of the cyclic anhydride of a urethane derivative of glutamic acid using 4-(dimethylamino)-pyridine (DMAP) as the catalyst has greatly simplified the synthesis of the target compound, ZD9063P, 5-(N-[(S)-N-{N,N-bis(2-chloroethyl)amino}phenoxycarbonyl)-γ-glutamyl]amino)-isophthalic acid.