双消除一锅简便法合成1-丙炔基芳香化合物

Convenient Synthesis of (1-Propynyl)arenes through a One-Pot Double Elimination Reaction

报道了一种便捷合成1-丙炔基芳香化合物的新方法.在充分探讨反应条件的基础上,利用硫试剂乙基苯基砜与芳香醛组合,采用双消除反应成功地一锅合成了一系列1-丙炔基芳香化合物1a～1s.运用此法不仅合成出一些含有醚键、萘环、杂环以及含有两个1-丙炔基的化合物,重要的是芳环上含有卤原子(Br和I)的化合物也能顺利地合成出来.该方法原料易得,操作简单,产物容易分离纯化并且产率理想.

Presented here is a new convenient synthetic protocol to （1-propynyl）arenes. The synthesis methodology through one-pot double elimination procedure was developed based on detailed examination of the reaction condition. Reaction of ethyl phenyl sulfone with aryl aldehyde followed by a one-pot double elimination procedure afforded an array of （1-propynyl）arenes in moderate to good yields. Some products included methoxy group, naphthyl and heterocyclic aromatic moieties, and some were borne with two 1-propynyl groups. It is more important that compounds bearing halogens were also synthesized via this protocol. The virtues of this present protocol are facile available starting materials, convenient operation, and easy separation of desired products.