抗血吸虫药物吡喹酮的新合成路线  

A new and efficient method for the synthesis of praziquantel,an antischistosomiasis drug

作　　者：程训官[1] 郑小红[1] 夏铸[1] 张昕宇[1] 王宇[1] 余瑜[1] 

机构地区：[1]重庆医科大学药学院药物化学教研室重庆市药物工程研究中心,重庆400016

出　　处：《重庆医科大学学报》2011年第10期1208-1210,共3页Journal of Chongqing Medical University

基　　金：国家自然科学基金资助项目(编号:30772595;30171070;30371632);科技重大专项资助项目(编号:2010ZX09401-306-1-1);重庆市科委攻关资助项目(编号:20021425);重庆市教委资助项目(编号:20021804)

摘　　要：目的:构建一条绿色、环保且能适合工业化生产抗血吸虫药物吡喹酮的新合成路线。方法:以苯乙胺为原料,用氯乙酰氯酰化,再用邻苯二甲酰亚胺钾氨基化反应,在P2O5作用下经Bischler-Napieralski环合反应制得N-[(1-亚甲基)-3,4-二氢异喹啉]邻苯二甲酰亚胺,经肼解和还原得到1-氨甲基-1,2,3,4-四氢异喹啉盐酸盐,经环己烷甲酰化、氯乙酰氯酰化和环合得目标化合物。结果:该合成路线的总收率可达32.8%,为原总收率的2.13倍。结论:该合成工艺路线操作简便,原料廉价易得,条件温和,绿色环保,收率较高,具有一定的工业化生产前景。Objective：To establish an industrial synthetic route for praziquantel.Methods：Praziquantel was synthesized with an overall yield of about 32.8% from phenylethylamine via acylation,amination with phthalimide potassium,Bischler-Napieralski cyclization,hydrazine solution,reduction,followed by acylation with cyclohexanecarboxylic acid chloride and chloroacetyl chloride,and then cyclization.Results：Target structures werecharacterized by IR,UV and MS.Conclusion：The method has the advantages of convenient operation,mild reaction conditions and high yield.This method is fit for industrial process.

关 键 词：吡喹酮 合成 环合 四氢异喹啉 血吸虫病 

分 类 号：R916[医药卫生—药学]