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米拉贝隆的合成新方法研究 被引量：1

Study on a New Method for Synthesis of Mirabegron
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摘要 （R）-1-苯基-1,2-乙二醇与对甲苯磺酰氯经取代反应得到（R）-1-苯基-1,2-羟基-对甲苯磺酸酯,再与对硝基苯乙胺在碳酸钾作用下得到（R）-2-（（4-硝基苯乙基氨基）-1-苯乙醇,最后通过还原铁粉催化硝基还原、与2-氨基噻唑-4-乙酸胺酯缩合得到米拉贝隆,总收率为58%. （R）-2-hydroxy-2-phenylethyl 4-methylbenzenesulfonate was synthesized by the displacement reaction of（R）-1-phenylethane-1,2-diol with 4-toluene sulfonyl chloride,which was reacted with 4-Nitrophenethylamine to afford（R）-2-（（4-nitrophenethyl）amino）-1-phenylethanol in the presence of K2CO3.Finally,the intermediate products was reduced by Iron powders and condensation with 2-（2-aminothiazol-4-yl）acetic acid to produce Mirabegron in 58%total yield.
作者 李芷琪 毛龙飞
机构地区 大连理工大学石油与化学工程学院 河南师范大学化学化工学院
出处 《河南师范大学学报（自然科学版）》 CAS 北大核心 2016年第2期85-88,共4页 Journal of Henan Normal University(Natural Science Edition)
基金 河南省产学研合作项目（122107000014）
关键词 (R)-1-苯基-1 2-乙二醇 对甲苯磺酰氯 米拉贝隆 （R）-1-phenylethane-1 2-diol 4-toluene sulfonyl chloride mirabegron
分类号 R914.5 [医药卫生—药物化学]
  • 相关文献

参考文献14

  • 1唐启东,宫平.米拉贝隆[J].中国药物化学杂志,2012,22(6):544-544. 被引量：18
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二级参考文献11

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共引文献19

同被引文献15

  • 1胡凡,王伸勇,贾新赞,等.一种米拉贝隆的合成方法:中国,103193730[P].2013-04-17.
  • 2阿不都赛米·马木提,贲一飞.一种米拉贝隆的合成方法:104016943A[P].2014-09-03.
  • 3张华,李杨,陈仕杰.米拉贝隆的合成方法:103896872A[P].2014-07-02.
  • 4Takusagawa S, Van Lier J J, Suzuki K, et al. Absorption, metabolism and excretion of [(14)C]mirabegron (YM178), a patent and selective/3 (3)-adrenoceptor agonist, after oral administration to healthy male volunteers [J]. Drug Metabolism & Disposition the Biological Fate of Chemicals, 2012, 40(4): 815-824.
  • 5Takasu T, Ukai M, Sato S, et al. Effect of (R)-2-(2-aminothiazol- 4-yl)-4'-{2-[(2-hydroxy-2- phenylethyl)amino]ethyl acetanilide (YM178), a novel selective beta3-adrenoceptor agonist, on bladder function[J]. Journal of Pharmacology & Experimental Therapeutics, 2007, 321(2): 642-647.
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引证文献1

二级引证文献4

河南师范大学学报（自然科学版）
2016年 第2期

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