一种简单合成反式-5-(4-氯苯基)-4-甲基-2-氧代噻唑烷酮的路线

A Synthesis Route of the 5-(4-chlorophenyl)-4-methylthiazolidin-2-one

摘要:

摘要：本文报道了一种合成噻螨酮关键中间体——反式-5-(4-氯苯基)-4-甲基-2-氧代噻唑烷酮的方法。以赤式-1-对氯苯基-2-氨基丙醇盐酸盐和二硫化碳为原料，在130℃下直接环合得到反式-5-(4-氯苯基)-4-甲基-2-氧代噻唑烷酮，收率82%，含量99%；再经双氧水氧化得到噻螨酮关键中间体——反式-5-(4-氯苯基)-4-甲基-2-氧代噻唑烷酮，收率84%，含量95%。该工艺流程经两步合成得到目标产物，简化了操作步骤，缩短了反应时间，杜绝了酸性废水的排放，符合绿色化工的要求。

Abstract:

Abstract: A concise synthetic route was developed for the key intermediate of hexythiazox—5-(4-chlorophenyl)-4-methylthiazolidin-2-one. The cyclocondensation of carbon disulfide with 1-(4-chlorophenyl)-1-hydroxypropan-2-aminium chloride would proceed in one-step at 130 oC, providing (4R,5R)-5-(4-chlorophenyl)-4- methylthiazolidine-2-thione in 82% yield with 99% purity. Subsequently, the intermediate was oxidized by hydrogen peroxide oxidation, producing (4S,5S)-5-(4-chlorophenyl)-4-methylthiazolidin-2-one in 84% yield with 95%purity. It represents a simple and facile method to access (4S,5S)-5-(4-chlorophenyl)- 4-methylthiazolidin-2-one, which shortens the reaction time and reduces the waste discharge. Thus, it is ecology benigh.