聚乙二醇酸性双子离子液体催化6-氨基取代嘌呤衍生物的合成及其抑菌活性

Synthesis of 6-Amino-purine Derivatives Catalyzed by Polyethylene Glycol_(1000)-Dicationic Acidic Ionic Liquid

以4,6-二氯-5-氨基嘧啶为起始原料,利用聚乙二醇酸性双子离子液体(PEG1000-DAIL)为催化剂,通过3步反应合成了一系列6-氨基取代嘌呤衍生物并测试了其抑菌活性.与现有方法相比,该方法反应时间短且收率高,并能避免闭环过程中嘌呤6位氯的水解,目标化合物分离简单且离子液体易回收利用.

A series of 6-amino-purine derivatives were synthesized from 4,6-dichloro-5-pyrimidine via three step reactions： N-alkylation, cyclization and N-alkylation of purine. All the reactions were catalyzed by the polyethylene glycoll000-dicationic acidic ionic liquid （PEG10o0-DAIL）. Compared to other synthetic methods, this method not only enhanced the yield, but also avoided the hydrolysis of the chloride to the hydroxyl group during the cyclization. The product can be isolated easily and the catalytic system can be recycled and reused for subsequent reactions.