超声化学合成唑吡坦关键中间体

Synthesis of Key Intermediate of Zolpidem via Ultrasound-promoted Three-component Reaction

改进了唑吡坦关键中间体6-甲基-3-氰甲基-2-(4-甲基苯基)咪唑[1,2-a]吡啶的合成工艺。以5-甲基-2-氨基吡啶、4-甲基苯乙酰溴和溴乙腈为原料,无需催化剂和添加剂,通过超声促进的三组分串联反应,实现了6-甲基-3-氰甲基2-(4-甲基苯基)咪唑[1,2-a]吡啶的快速合成,收率84%,目标产物结构经^(1)H NMR、^(13)C NMR和高分辨质谱表征确证。该方法合成路线短、原料廉价易得、操作简便、安全稳定、收率高。为唑吡坦关键中间体的高效合成提供了新思路。

The synthesis of key intermediate of Zolpidem was improved.The target product was synthesized using 2-amino-5-methylpyridine,α-bromo-4-methylacetophenone and bromoacetonitrile as starting materials by ultrasound-promoted three-component reaction under catalyst-free,oxidant-free and mild conditions.The yield reached 84%and the product was characterized by NMR and HRMS.This method had the advantage of short synthetic route,cheap raw materials,easy operating,safe,stability and high yield,which provided a new strategy for the synthesis of key intermediate-Zolpidem.