A general method for the synthesis of benzimidazole-4-sulfonamides

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Abstract

A general method for the synthesis of benzimidazole-4-sulfonamides is described. This methodology employs commercially available benzothiadiazole-4-sulfonyl chloride as a benzimidazole equivalent. Reaction with a variety of amines followed by highly chemoselective reductive desulfurization gives intermediate 1,2-phenylenediamines, which may then react with aryl, heteroaryl, and alkyl aldehydes to provide substituted benzimidazole sulfonamides. © 2009 Elsevier Ltd. All rights reserved.

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Rosen, M. D., Simon, Z. M., Tarantino, K. T., Zhao, L. X., & Rabinowitz, M. H. (2009). A general method for the synthesis of benzimidazole-4-sulfonamides. Tetrahedron Letters, 50(11), 1219–1221. https://doi.org/10.1016/j.tetlet.2009.01.015

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