An efficient synthesis of 3-substituted 3H-pyrimidin-4-ones.

Org Lett

Department of Medicinal Chemistry, MMPD CEDD, GlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, USA.

Published: March 2004

[reaction: see text] A novel and practical synthesis of 3-substituted 3H-pyrimidin-4-ones is described. The key step involves the cyclization of enamide esters, derived from readily available beta-keto esters, with trimethylaluminum and various primary amines.

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http://dx.doi.org/10.1021/ol049921vDOI Listing

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