Green Synthesis of Novel Pyrrole and Its Derivatives Based on(4 +1)Cyclization Reaction
付雪菊 1徐可 1韩波 1何享鸿1
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作者信息
1. 成都中医药大学 药学院 西南特色中药资源国家重点实验室,四川 成都 611137
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摘要
吡咯结构广泛存在于自然界中,是一类具有多种生物活性的药物骨架.传统合成方法主要是由金属催化且常以有机溶剂作为媒介进行合成,然而以水作溶剂的绿色合成方法鲜有报道.以2-烯丙基丙二腈与S,S-二苯基硫亚胺为原料,以水为溶剂,在温度为50℃且无催化剂的温和绿色的条件下发生(4 +1)环化反应,顺利构建了9 个不同取代的 5,5-二氰基-3-羧酸乙酯吡咯烷(3a～3i),分离收率为 62%～77%,其结构经1 H NMR,13 C NMR和HR-MS(ESI-TOF)表征.
Abstract
Pyrrole structure is a drug backbone with various biological activities in nature.Convention-al synthesis methods are mainly metal-catalyzed,generally mediated by organic solvents,while water as the solvent are rarely reported.Nine differently substituted 5,5-dicyano-3-carboxylic acid ethyl pyr-rolidines(3a～3i)were successfully constructed by the(4 +1)cyclization reaction at 50℃with water as solvent and in the absence of catalyst,and their structures were characterized by 1 H NMR,13 C NMR and HR-MS(ESI-TOF)in 62%～77%isolated yields.
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