无碱条件下直接多组分反应选择性合成非对称含氮杂芳基硫醚

Selective Synthesis of Unsymmetrical N-Heteroaryl Thioethers by Base-Free Direct Multi-Component Reaction

杂芳基硫醚,尤其是烷基杂芳基硫醚,一般通过强碱性条件下的催化或非催化偶联方法来合成,缺点多,废弃物多.本文报道一种卤代含氮杂芳烃、硫脲及溴代烷烃在无碱、无添加剂及无溶剂条件下的一锅多组分反应直接合成杂芳基硫醚的新方法.本方法以硫脲为硫源,并可兼容各种卤代含氮杂芳烃和溴代烷烃,提供了一种含氮杂芳基硫醚的简洁、高效、选择性合成新方法.

Heteroaryl thioethers,especially alkyl heteroaryl thioethers,were usually obtained by catalytic or non-catalytic coupling reactions under strong basic conditions,but these methods usually have many drawbacks such as generation of large amounts of wastes.In this work,a new method for the direct synthesis of N-heteroaryl thioethers through a base-,additive-,and solvent-free one-pot multi-component reaction of N-heteroaryl halides,thiourea,and alkyl bromides was reported.This method can employ thiourea as the sulfur surrogate and tolerate various alkyl bromides and N-heteroaryl halides,providing a concise,selective,and efficient new method for heteroaryl thioether synthesis.