摘要/Abstract

发展了一种使用廉价碘单质作为催化剂, 乙烯基叠氮作为自由基受体, 芳基亚磺酸钠作为自由基源, 合成Z型结构的N-未保护的β-磺酰基烯胺类化合物的方法. 该反应中乙醇作为溶剂, 双三氟甲烷磺酰亚胺(Tf₂NH)作为添加剂, 在40 ℃下反应4~6 h, 可以以优良的产率得到β-磺酰基烯胺类化合物. 该方法无需使用金属催化剂, 具有条件简单、反应时间短、底物适用范围广等优点.
关键词: 碘催化, 乙烯基叠氮, 自由基加成, 磺酰基烯胺
The present protocol provides the facile and highly efficient synthesis of various Z-structure N-unprotected β-sulfonyl enamine compounds in a manner by using inexpensive molecular iodine as catalyst, vinyl azides as free radical acceptor, and sodium arylsulfinates as free radical sources. In this reaction, ethanol was used as solvent and bistrifluoromethanesulfonimide (Tf₂NH) was used as additive. The reaction was carried out at 40 ℃ for 4~6 h to obtain β-sulfonyl enamine compounds with good yields. The method does not need to use metal catalyst, and has the advantages of simple conditions, short reaction time and wide substrate application range.
Key words: iodine catalysis, vinyl azide, free radical addition, sulfonyl enamine


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