3-苯甲酰氧基-4-苯基-5-α-羟苄基-N-甲基-2-吡咯烷酮的制备及生物活性初步评价  

Preparation and Activity Evaluation of 3-Benzoyloxy-4-phenyl-5-αhydroxybenzyl-N-methyI-2-pyrrolidone

作　　者：李建组[1] 定力[1] 李骏[1] 林汉森[1] 

机构地区：[1]广东药学院药科学院,广东广州510006

出　　处：《广东化工》2014年第6期35-36,共2页Guangdong Chemical Industry

摘　　要：以3-羟基-4-苯基-5-苯甲酰基-N-甲基-2-吡咯烷酮(1)为原料,通过先酰化3位羟基,再将5位苯甲酰基还原为5-α-羟苄基得标题产物3-苯甲酰氧基-4-苯基-5-α-羟苄基-N-甲基-2-吡咯烷酮(3),两步反应总收率为49.1%。以抑制乙酰胆碱酯酶作为生物活性评价指标,实验结果显示,其对乙酰胆碱酯酶没有抑制作用。： 3-Benzoyloxy-4-phenyl-5-a-hydroxybenzyI-N-methyl- 2-pyrrolidone was synthesized from 3-hydroxy-4-phenyl-5-benzoyl-N-methyl-2-pyrrolidone in two- steps with a total yield of 49.1%. The experiment indicate that Title compound 3 has no obvious effect on acetylcholinesterase inhibitory activity. Further structural modification and activityevaluation are in progress.

关 键 词：制备 酰化反应 生物活性 

分 类 号：TQ[化学工程]