摘要/Abstract

报道了一种简洁、高效的合成方法, 即铜催化的磺酰胺与脂肪族环状叔胺直接碳氢脱氢偶联, 实现高区域选择性地合成(E)-N-磺酰甲脒衍生物. 该反应条件简单, 无需使用腐蚀性酸或碱作为添加剂, 并兼容多种底物和官能团. 同时该方法能够实现克级反应和药物分子的后期功能修饰.
关键词: 铜催化, 脂肪族环状叔胺, 区域选择性, 磺酰甲脒
This paper reports a concise and efficient synthesis method, namely copper-catalyzed direct hydrocarbon dehydrogenation coupling of sulfonamides and aliphatic cyclic tertiary amines, to realize the highly regioselective synthesis of (E)-N-sulfonylformamidines. The reaction is accomplished without any corrosive acid or base as an additive. It tolerates a broad scope of substrates, good functional group compatibility, and generates exclusive (E)-stereoselectivity. Moreover, this utility of the protocol is successfully demonstrated in a late-stage functionalization of medicinally active molecules and gram-scale synthesis.
Key words: copper catalysis, aliphatic cyclic tertiary amines, regioselective, sulfonylformamidines


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