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Updated: Sep 29, 2026

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
Ethyl 2-chlorooxazole-4-carboxylate: a versatile intermediate for the synthesis of substituted oxazoles
Kevin J Hodgetts1, Mark T Kershaw
1Neurogen Corporation, 35 Northeast Industrial Road, Branford, Connecticut 06405, USA. khodgetts@nrgn.com
Abstract:
[reaction: see text] By using a sequence of regiocontrolled halogenation and palladium-catalyzed coupling reactions, the synthesis of variously substituted oxazoles from ethyl 2-chlorooxazole-4-carboxylate (2) was accomplished. The methodology was applied to the synthesis of a series of 2,4-disubstituted, 2,5-disubstituted, and 2,4,5-trisubstituted oxazoles.
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