Parallel Synthesis of Structurally Diverse Aminobenzimidazole Tethered Sultams and Benzothiazepinones

结构多样的氨基苯并咪唑连接的磺内酰胺和苯并噻唑酮的平行合成

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Abstract

A solid-phase methodology to construct aminobenzimidazole tethered sultams and benzothiazepinones from commercial amino acids, amines, carboxylic acids and sulfonyl chlorides is described. Coupling of Fmoc-Cys(Trt)-OH to resin-bound aminobenzimidazole scaffold provided an essential precursor for the construction of a variety of seven membered benzofused cyclic sulfonamides and thiazepinones via palladium catalyzed Buchwald-Hartwig type intramolecular cyclization.

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