磷酸二酯酶抑制剂米力农的合成工艺改进  

Process improvement on synthesis of phosphodiesterase inhibitor milrinone

作　　者：刘爱芹[1,2,3,4] 许士琪[2] 郝超 于胜海 朱礼岩[2] LIU Aiqin;XU Shiqi;HAO Chao;YU Shenghai;ZHU Liyan(Institute of Materia Medica,Shandong Academy of Medical Sciences,Jinan 250062,Shandong;School of Medicine and Life Sciences,Shandong Academy of Medical Sciences,University of Jinan,Jinan 250062,Shandong;Key Lab. of Biotechnology Drugs,Ministry of Health ,Jinan 250062,Shandong;Key Lab. of Rare and Uncommon Diseases of Shandong Province,Jinan 250062,Shandong)

机构地区：[1]山东省医学科学院药物研究所,山东济南250062 [2]济南大学山东省医学科学院医学与生命科学学院,山东济南250062 [3]国家卫生部生物技术药物重点实验室,山东济南250062 [4]山东省罕少见病重点实验室,山东济南250062

出　　处：《化学研究》2019年第4期338-341,共4页Chemical Research

基　　金：山东省医学科学院院级科技计划青年基金(2018-41),山东省医学科学院医药卫生科技创新工程;济南大学大学生研究训练(SRT)计划项目(SX20170923)

摘　　要：以1-(4-吡啶基)丙酮为原料,与原甲酸三乙酯缩合得1-乙氧基-2-(4-吡啶基)-乙烯基甲基酮,然后再与腈乙酰胺环合得米力农.原料价廉易得,操作简便,降低了生产成本,适于工业化生产,总收率为52.5%.The 1-ethoxy-2-(4-pyridyl)-vinylmethyl ketone was obtained by the condensation of 1-(4-pyridyl) acetone and triethyl orthoformate, which was then cyclized with nitrile ace-tamide affored milrinone in 52.5% yield. This approach offered an easy, low-cost, practical access to valuable milrinone which was suitable for industrial production.

关 键 词：磷酸二酯酶Ⅲ(PDEⅢ)抑制剂 缩合 环合 工艺改进 

分 类 号：O627[理学—有机化学]