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2-氨基噻唑-4-甲酸合成方法的改进 被引量：1

Improved Method for Synthesis of 2-Aminothiazole-4-formic Acid
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摘要 以硫脲为原料、溴代丙酮酸乙酯为试剂,采用无溶剂的方法合成出2-氨基噻唑-4-甲酸乙酯,然后经碳酸钾-甲醇溶液皂化反应,最后通过调节pH得到目标化合物2-氨基噻唑-4-甲酸。两步收率达75%,此方法操作简单,可实现连续放大生产,提高了收率和效率。各步化合物经熔点、红外、质谱、氢核磁谱等分析手段,验证结构符合及纯度很高。 2-Aminothiazole-4-ethyl formate was synthesized from thiourea and ethyl bromopyruvate by the method of solvent-free. Then through saponification in potash-methanol solvent, we got the targe compound of 2-aminothiazole-4-formic acid by adjusting the pH. The two steps were prepared with overall yield of 75 %. The method has a remarkable virtue of high yield, lugh efficiency, and low cost： it can be used to produce continuously. The compounds were determined by means of melting point measurement, IR, MS（ESI）, 1H-NMR. The result showed exact structure and high purity.
作者 张秀芹 张俊俊 应林 周琢强
机构地区 华南农业大学理学院
出处 《广东化工》 CAS 2009年第6期55-55,254,共2页 Guangdong Chemical Industry
关键词 2-氨基噻唑-4-甲酸 无溶剂 皂化 2-aminothiazole-4-formicacid solvent-free saponification
分类号 TQ252.5 [化学工程—有机化工] S379.5 [农业科学—农产品加工]
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参考文献5

  • 1Oxford, Alexander William. Preparation of N-substituted (hetero)aryl, particularly furan-2-yl, carboxamides and related compounds as prostanoid EP2 receptor agonists. US543538.
  • 2Houssin, Raymond, et al. Design, Synthesis, and Pharmacological Evaluation of New Farnesyl Protein Transferase Inhibitors, Journal of Medicinal Chemistry, 2002, 45(2): 533-536.
  • 3Plouvier, Bertrand. Journal of Heterocyclic Chemistry. 1989, 26(6): 1643 - 1647.
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  • 5Canas-Rodriguez. A. 2-Amino-4-polyhydroxyalkylthiazole. Chemistry & Industry (London, United Kingdom) (1957) : 666.

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.
  • 6Chapple C R, Nitti V W, Khullar V, et al. Onset of action of the 133- adrenoceptor agonist, mirabegron, in Phase II and III clinical trials in patients with overactive bladder [J]. World Journal of Urology, 2014, 32(6): 1 565-1 572.
  • 7Bhide A A, Digesu G A, Femando R, et al. Use of mirabegron in treating overactive bladder[J]. International Urogynecology Journal, 2012, 23(23): 1 345-1 348.
  • 8胡凡.一种米拉贝隆新的合成方法:中国,103304511A[P].2013-09-18.
  • 9Maruyama T 1. Amide derivatives or salts thereof: US, 6346532[P]. 2002-02-12.
  • 10Reid E B, Ruby W R. The synthesis of a lactone related to auxin bl [J]. Journal of the American Chemical Society, 2002, 73(3): 1 054- 1 061.

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二级引证文献4

广东化工
2009年 第6期

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