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Paper | Regular issue | Vol 71, No. 1, 2007, pp.39-48
Published online, 17th November, 2006
DOI: 10.3987/COM-06-10884
One-Pot Conversion 2-Nitrobenzonitriles to Quinazolin-4(3H)-ones and Synthesis of Gefitinib and Erlotinib Hydrochloride

Venkateshappa Chandregowda, Gudapati Venkateswara Rao, and Goukanapalli Chandrasekara Reddy*

*Vittal Mallya Scientific Research Foundation, P.O. Box No. 406, K. R. Road, Bangalore-560004, India

Abstract

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®) and erlotinib HCl (Tarceva®).