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吲哚嗪衍生物的多组分一锅法合成

Multi-component one-pot synthesis of indolizine derivatives

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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、Cs2CO3 做碱,以乙腈为溶剂,回流反应 7h,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1H NMR、13C 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 Cs2CO3 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 1H NMR,13C 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.

benzyl bromideethyl pyridine acetateindolazinetriethyl orthoformatemulticomponent

陈丽、熊雨婷、郝天辉、周博、贾慧婷、严胜骄

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云南大学化学科学与工程学院,云南昆明 650500

苄溴 吡啶乙酸乙酯 吲哚嗪 原甲酸三乙酯 多组分

国家级大学生创新创业训练项目云南省高校科技创新团队

202210673071C17624011121

2024

云南大学学报(自然科学版)
云南大学

云南大学学报(自然科学版)

CSTPCD北大核心
影响因子:0.663
ISSN:0258-7971
年,卷(期):2024.46(4)