含共轭烯炔结构单元的药物前体的合成和表征

Synthesis and characterization of pre-pharmaceutical containing structural unit of conjugated enyne

目的:合成含共轭烯炔结构单元的药物前体烯基砜。方法:通过端炔与烯基砜发生了Sonogashira偶联反应,生成含共轭烯炔结构单元的药物前体烯基砜。结果:产物经过1H NMR,13C NMR,HRMS(EI),IR和X-ray等表征。数据表明该反应合成的含共轭烯炔结构单元的药物前体烯基砜中的双键构型为Z型。结论:端炔与烯基砜发生了Sonogashira偶联反应区域和立体选择性地合成了含共轭烯炔结构单元的烯基砜,该反应为合成药物前体烯基砜提供了新方法。

Objective：To synthesize the pre-pharmaceutical containing the structural unit of coniugated enyne. Methods ： Sonogashira coupling reaction of terminal alkyne and （ E ）-β-iodovinyl sulfone was used to synthesis the product. Results： The product was characterized by ^1H NMR, ^13C NMR, FIRMS （EI）, IR and X-ray with configuration in Z - fashion. Conclusion ：The findings show a promising methods for synthesizing pre-pharmaceutical containing the struclural unit of conjugated enynes.