7-氮杂吲哚N-氧化物的区域选择性脱氧硫醚化反应

Regioselective Deoxygenative Thioetherification of 7-Azaindole N-oxides

本文开发了一种3-硫代-7-氮杂吲哚衍生物的合成方法。研究发现,在30%的I_(2)的催化作用下,磺酰肼和7-氮杂吲哚N-氧化物在正丁醇中110℃条件下反应以53%~86%的产率得到硫醚化产物。该反应有较好的区域选择性和底物适应性,并具有反应时间较短、绿色环保和操作简便等优点。

A convenient, general method has been developed for the synthesis of 3-thio-7-azaindoles via a thioetherification reaction. In the presence of 30% I_(2), sulfonyl hydrazide reacted with 7-azaindole N-oxide in n-butanol at 110℃ to afford the desired thioetherification products in good yields(53%~86%). This reaction exhibits broad substrate scope and excellent regioselectivity. The main advantage of this method is the short reaction time, green reaction conditions and simple operation.