吡喹酮合成新方法研究  

Study on New Synthetic Method of Praziquantel

作　　者：王东升[1] 沙娜[1] 陈勇[1] 

机构地区：[1]上海应用技术学院化学与环境工程学院,上海201418

出　　处：《化学世界》2013年第11期666-669,共4页Chemical World

基　　金：国家自然科学基金青年基金资助项目(21005049)

摘　　要：研究了抗血吸虫药物吡喹酮的合成新方法。以甘氨酸乙酯盐酸盐和溴代乙醛缩二乙醇为原料,经N-烃化、N-酰化和Pictet-Spengler缩合三步反应合成出了吡喹酮。探讨了催化剂用量、缚酸剂、反应温度和酸催化剂对反应的影响。三步反应总收率为32%。产物结构经IR、1 H NMR、13C NMR、MS和HRMS确证。该方法反应条件温和,成本低,环境污染少,具有一定的工业化前景。A new synthetic method of praziquantel used as antischistosomal was introduced. Praziquantel was synthesized by N-alkylation reaction, N-acylation reaction and Pictet-Spengler reaction from glycine ethyl ester hydrochloride and bromoacetaldehyde diethyl acetal as the starting materials. The effect of mo lar ratio of catalyst, acid binding reagent, reaction temperature and acid catalyst was studied. The total yield was 32%. The structure of the product was confirmed byIR, 1H NMR, ~3CNMR, MS and HRMS. This method has the advantages of mild reaction conditions, low cost and less environmental pollution, and is suitable for industrial production in the future.

关 键 词：吡喹酮 抗血吸虫药物 甘氨酸乙酯盐酸盐 溴代乙醛缩二乙醇 合成 

分 类 号：R978.63[医药卫生—药品]