益智和记忆增强药物PRL-8-53的合成方法改进研究

Improvement on the synthesis of a nootropic and hypermnesic drug PRL-8-53

研究了一种促进学习和记忆力增强的药物PRL-8-53的新型合成方法。采用间三氟甲基苯乙酸作为起始原料,经氯化、胺化,再经四氢铝锂还原,得到N-甲基,N-苄基-3-三氟甲基苯乙胺,经酯化成盐酸盐,得到PRL-8-53。该方法原料易得,操作简便,总收率达到45.7%。

A new synthetic method of a nootropic and hypermnesic drug PRL-8-53 was studied.The PRL-8-53 was synthesized from m-trifluoromethylphenylacetic acid.N-benzyl-N-methyl-2-（3-（trifluoromethyl）phenyl）acetamide,the key intermediate was got via chlorination,amination,then reduction with lithium aluminum hydride.PRL-8-53 was synthesized via esterification,hydrochloride from the intermediate.The raw materials were easily obtained.The method had simple operation and the total yield was up to 45.7%.