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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
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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.
作者 刘爱芹 许士琪 郝超 于胜海 朱礼岩 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)
出处 《化学研究》 CAS 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)
关键词 磷酸二酯酶Ⅲ(PDEⅢ)抑制剂 缩合 环合 工艺改进 milrinone phosphodiesterase Ⅲ(PDE Ⅲ) inhibitors condensation cyclization process improvement
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