贺正国, 蒋琳, 江登榜, 岳越, 李树生, 袁明伟. 艾司洛尔盐酸盐的新合成方法[J]. 云南大学学报(自然科学版), 2021, 43(5): 985-989. doi: 10.7540/j.ynu.20200649
引用本文: 贺正国, 蒋琳, 江登榜, 岳越, 李树生, 袁明伟. 艾司洛尔盐酸盐的新合成方法[J]. 云南大学学报(自然科学版), 2021, 43(5): 985-989. doi: 10.7540/j.ynu.20200649
HE Zheng-guo, JIANG Lin, JIANG Deng-bang, YUE Yue, LI Shu-sheng, YUAN Ming-wei. A new synthesis method of esmolol hydrochloride[J]. Journal of Yunnan University: Natural Sciences Edition, 2021, 43(5): 985-989. DOI: 10.7540/j.ynu.20200649
Citation: HE Zheng-guo, JIANG Lin, JIANG Deng-bang, YUE Yue, LI Shu-sheng, YUAN Ming-wei. A new synthesis method of esmolol hydrochloride[J]. Journal of Yunnan University: Natural Sciences Edition, 2021, 43(5): 985-989. DOI: 10.7540/j.ynu.20200649

艾司洛尔盐酸盐的新合成方法

A new synthesis method of esmolol hydrochloride

  • 摘要: 艾司洛尔盐酸盐是一种超短效β1受体阻滞剂,在临床上主要用于室上性心动过速、围术期高血压,也可用于室上性快速性心律失常,特点是起效快,作用时间短. 以4-溴苯酚为起始原料,经Heck反应、氢化、溴丙烯醚化、氧化、异丙胺开环、成盐6步反应合成艾司洛尔盐酸盐,总产率为46%,为艾司洛尔盐酸盐的合成提供了一条新的路线.

     

    Abstract: Esmolol hydrochloride is an ultra-short acting β1-receptor blocker, which has mainly used for supraventricular tachycardia and perioperative hypertension. It has been also used for supraventricular tachyarrhythmia in clinical practice. The drug is characterized by quick effect and short action time. In this paper using 4-bromophenol as a starting material, esmolol hydrochloride was prepared by Heck reaction with methyl acrylate, hydrogenation, etherification with 3-bromopropene, oxidation, then isopropylamine was used to open the epoxide and salinization, the overall yield of the 6 synthetic steps is 46%. This method provides a new synthetic route for the synthesis of esmolol hydrochloride.

     

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