吡咯烷-2,4-二酮类化合物的合成

Synthesis of 2,4-pyrrolidinedione Compounds

研究发现,从天然产物中提取出的吡咯烷-2,4-二酮衍生物具有抑菌、抗肿瘤、抗溃疡、抗病毒、除草等多种活性。该类化合物具有多个手性中心,结构复杂,很多化学家对其合成方法、结构修饰和构效关系进行了大量的研究。本文以廉价的丙二酸二乙酯为原料,通过水解、酰化,制备丙二酸单乙酯酰氯;再和不同的氨基酸乙酯盐酸盐反应,通过酯缩合、脱羧等步骤,合成了一系列吡咯烷-2,4-二酮化合物类衍生物。

It is found that pyrrolidine 2,4-dione derivatives extracted from natural products have antibacterial,anti-tumor,anti-ulcer,antiviral,weeding and other activities.This kind of compound has many chiral centers and complex structure.Many chemists have studied its synthesis method,structure modification and structure-activity relationship.Ethyl malonyl chloride was prepared by hydrolysis and acylation from cheap diethyl malonate.A series of 2,4-pyrrolidinedione derivatives were synthesized by reacting with different amino acid ethyl ester hydrochloride through ester condensation,decarboxylation and so on.