摘要/Abstract

β-氨基砜是一种特别有用的生物活性分子的骨架.β-氨基乙烯基砜加氢法是合成β-氨基砜的一种简便、高效的方法. 提出了一种以苯亚磺酸钠和叔胺为底物的电化学法合成β-氨基乙烯基砜. 在无金属催化剂和无氧化剂的条件下, 仅合成E构型的β-氨基乙烯基砜. 循环伏安实验和对照实验表明, 该电合成反应经历了磺酸自由基与烯胺的加成, 并生成碳自由基的过程.
关键词: β-氨基砜, β-氨基乙烯基砜, 苯亚磺酸钠, 叔胺
β-Amido sulfone motif reprents a particularly useful scaffold for the biologically active molecules. The hydrogenation ofβ-amidovinyl sulfon is an alternative method to synthesizeβ-amido sulfone. Herein, one electrochemical method to synthesizeβ-amido sulfone using sodium sulfites and tertiary amines as substrates is presented. OnlyE-configurations ofβ-amidovinyl sulfonyl were synthesized under metal catalyst- and oxidant-free condition. Cyclic voltammetry (CV) and control experiments indicate that this electrosynthesis reaction goes through a radical process which the sulfonyl radical adds to enamine to form the carbon radical.
Key words: β-amido sulfone, β-amidovinyl sulfon, sodium sulfites, tertiary amines


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