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Note | Regular issue | Vol 45, No. 12, 1997, pp.2437-2442
Published online, 1st January, 1970
DOI: 10.3987/COM-97-7907
Stereoselective Synthesis of a 2,3-Disubstituted 5-Pyrrolidinone Derivative of Quinazolin-4(3H)-one

Mónika Szabó, József Kökösi,* Attila Kovács, Zsolt Böcskei, and István Hermecz

*R & D Directorate Preclinical Development, CHINOIN Pharmaceutical and Chemical Works Ltd., P. O. Box 110, H-1325 Budapest, Hungary

Abstract

Thermal cyclization of acetoacetamide (3), prepared from 2[1’-(p-methoxyphenylaminoethyl]quinazolin-4(3H)-one (2) and ethyl acetoacetate, resulted in the formation of 2-(5-oxopyrrolidin-2-yl)quinazolin-4(3H)-one (6) with high selectively in excellent yield. The stereostructure of 6 was investigated by NMR spectroscopy, and determined by X-Ray investigations.