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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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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

ID: J72-Y1999-570