Practical synthesis of tetrasubstituted thiophenes for use in compound libraries

Bryan P. McKibben*,Craig H. Cartwright and Arlindo L. Castelhano*

*Cadus Pharmaceutical Corporation, Tarrytown, NY 10591 USA

B. P. McKibben, C. H. Cartwright, A. L. Castelhano, Tetrahedron Lett., 1999, 5471-5474.

DOI: 10.1016/S0040-4039(99)01108-9

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Abstract

Optimized conditions were developed to carry out Gewald's reaction at room temperature to give tetrasubsituted thiophenes in good yield. These thiophenes served as key templates for structural diversification and semi-automated library synthesis.

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Key Words

thiophene derivatives, multicomponent reactions, Gewald reaction

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ID: J72-Y1999-570