吲哚嗪衍生物的多组分一锅法合成

Multi-component one-pot synthesis of indolizine derivatives

以吡啶乙酸乙酯1和苄溴类化合物2为原料,以原甲酸三乙酯为添加剂、Cs_(2)CO_(3)做碱,以乙腈为溶剂,回流反应7 h,四组分“一锅法”合成了多取代吲哚嗪衍生物3a~3i.实验中发现原甲酸三乙酯在反应体系中作为干燥剂能极好地除去反应体系中残余的微量水分,保证反应顺利进行.所合成的产物都经^(1)H NMR、^(13)C NMR和HRMS表征.结果表明,该方法具有原料易得,操作简单,路线简洁等特点,为筛选具有潜在生物活性的吲哚嗪衍生物提供了新的合成方法.

In this paper,polysubstituted indolizine derivative 3 was synthesized with ethyl pyridine acetate 1 and benzyl bromide 2 as raw materials,triethyl orthoformate as additive and Cs_(2)CO_(3) as base in acetonitrile solution by reflux reaction for 7 h.The yield was medium to excellent.It was also found that triethyl orthoformate had water absorption in the reaction system.The synthesized products were characterized by ^(1)H NMR,^(13)C NMR and HRMS.The method described in the paper highlights the advantages of easily accessible raw materials,simple reaction procedure,and a straightforward synthesis route.This method offers a new approach for the synthesis of potential bioactive indolizine derivatives,which could be useful in the discovery of new drug candidates or bioactive compounds.