【摘要】 目的:改进匹多莫德的合成工艺。方法:在文献方法的基础上设计出新的方法,即取L-半胱氨酸与甲醛反应生成L-4-噻唑烷甲酸,然后与L-焦谷氨酸在强酸性阳离子交换树脂的催化作用下反应得到目标化合物,并经质谱和核磁共振氢谱确证其化学结构。结果:目标化合物经确证为匹多莫德,其产率达到55.48%,含量大于98.5%。与文献方法比较,新方法路线反应步骤少,反应条件较温和,原料易得,产物结晶性好。结论:改进方法为匹多莫德的工业化生产提供了一条新型的、较为合理的工艺路线。更多还原

【Abstract】 OBJECTIVE:To improve the synthesis process of pidotimod.METHODS:New technology was designed on the basis of literature research,i.e.pidotimod was synthesized via the condensation of L-thiazolidine-4-carboxylic acid and L-pyroglutamic acid in the presence of strongly acidic cation-exchange resin.L-thiazolidine-4-carboxylic acid was prepared from L-cysteine and formaldehyde.The chemical structure of pidotimod was determined by mass spectrum and 1H NMR.RESULTS:The target compound was pidotimod with yield rate of 55.48%.The content of it was more than 98.5%.Compared with literature method,new technology was short in route,reaction,steps.Reaction condition was mild,and raw material was available easily.The crystallinity of products was excellent.CONCLUSION:Improved technology provides a new and reasonable route for industrial production of pidotimod.更多还原