Tetrahedron Letters

Synthesis of functionalized hydroxy-thiophene motifs as amido-and sulfonamido-phenol bioisosteres

J Chao, AG Taveras, CJ Aki

Index: Chao, Jianhua; Taveras, Arthur G.; Aki, Cynthia J. Tetrahedron Letters, 2009 , vol. 50, # 35 p. 5005 - 5008

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Citation Number: 9

Abstract

Novel highly substituted hydroxy thiophene motifs were designed and synthesized as viable amido phenol and sulfonamido phenol bioisosteres. Hydroxy group-directed regioselective bromination and palladium-catalyzed amination of thienyl bromide via Buckwald protocol are the key elements of the synthetic approach. The hydroxy thiophene-containing compounds displayed good binding inhibitions.