ONE-POT CONVERSION OF 2-NITROBENZONITRILES TO QUINAZOLIN-4(3H)-ONES AND SYNTHESIS OF GEFITINIB AND ERLOTINIB HYDROCHLORIDE

摘要

A simple and efficient one-pot conversion of 2-nitrobenzonitriles to quinazolin-4(3H)-ones involving reduction, formylation, hydrolysis and cyclization is reported. These quinazolinones have been used for making in economical way the anticancer drug molecules gefitinib (Iressa~R) and erlotinib HC1 (Tarceva~R).