期刊文献+

肾上腺素的合成工艺研究 被引量:1

Study on the Synthesis Technology of Epinephrine
下载PDF
导出
摘要 目的:对肾上腺素合成工艺参数进行了优化研究.方法:以2-氯-3,4-二羟基苯乙酮为起始原料,经胺化、还原、手型拆分合成出L构型的原料药肾上腺素.结果:胺化反应2-氯-3,4-二羟基苯乙酮和N-甲基苄最佳摩尔比为1:1.5,最佳反应温度为(40±2)℃,最佳反应时间为5 h;还原反应Pd/C的最佳用量为苄基肾上腺酮质量的20%,最佳温度为(35±2)℃,最佳反应时间为7 h;手性拆分DL-肾上腺素和拆分剂L-酒石酸最佳摩尔比为1:2.结论:该合成工艺反应条件温和,安全可行,收率高,适合工业化生产. Objective:The synthesis process parameters of epinephrine were optimized.Methods:L-Epinephrine was synthesized by amination,reduction and chiral resolution from 2-chloro-3,4-dihydroxyacetophenone which as starting material.Results:The optimum molar ratio of 2-chloro-3,4-dihydroxyacetophenone and N-methylbenzyl in amination is 1∶1.5,the optimum reaction temperature is(40±2)℃,and the optimum reaction time is 5 hours.The optimum amount of Pd/C in the reduction reaction process is 20%of the mass of N-benzyl epinephrine,the optimum reaction temperature is(35±2)℃,and the optimum reaction time is 7 hours.The optimum molar ratio of DL-epinephrine and L-tartaric acid in the chiral resolution process is 1∶2.Conclusion:The reaction conditions of the synthesis process are mild,safe and feasible,and the yield is high,which is suitable for industrial production.
作者 李立标 郑爱 施务务 LI Li-biao;ZHENG Ai;SHI Wu-wu(Bengbu BBCA Pharmaceutical Technology Development Co.Ltd.,Bengbu 233000,China;Fiest People's Hospital of Bengbu City,Bengbu 233000,China)
出处 《安徽化工》 CAS 2020年第4期66-68,73,共4页 Anhui Chemical Industry
关键词 肾上腺素 抗休克 手性拆分 epinephrine antishock chiral resolution
  • 相关文献

参考文献3

二级参考文献60

  • 1王天龙,杨拔贤.去甲肾上腺素在肝移植麻醉中的应用[J].中华普通外科杂志,2006,21(1):76-78. 被引量:7
  • 2金有豫.药理学[M].第5版.北京:人民卫生出版社,2001.63~64.
  • 3Dalvi, M. B., Kenny, R. S., Kawle, G. R. Process for preparation of (D/L)-norepinephrine acid addition salt, a key intermediate of (R)-(-)-norepinephrine: WO2013008247[P]. 2013.
  • 4Tullar, B. F. The resolution of dl-arterenol [J]. J. Am. Chem. Soe., 1948, 70(6): 2067-2068.
  • 5Qin Y H, Guillory J K, Schoenwald R D. Formulation, in vitro dissolution, and ocular bioavailability of high- and low-melting phenylephrineoxazolidines[J].PharmaceuticalResearch, 1993, 10 (11): 1627-1631.
  • 6Dewani A P, Dabhade S M, Bakal R L. Development and validation of a novel RP-HPLC method for simultaneous determination of paracetamol, phenylephrinehydrochloride, caffeine, cetirizineand nimesulide in tablet formulation[J]. Arabian Journal of Chemistry, 2013, 4 (5): 501-505.
  • 7Ma J, Wu L N, Hou Z, et al. Visualizing the endocytosis of phenylephrine in living cells by quantum dot-based tracking[J]. Biomaterials, 2014, 35: 7042-7049.
  • 8Dousa M, Gibala P, Havlicek J, et al. Drug-excipient compatibility testing-Identification and characterization of degradation products of phenylephrine in several pharmaceutical formulations against the common cold[J]. Journal of Pharmaceutical and Biomedical Anatysis,2011,55:949-956.
  • 9Legerlotz H. Monohydric amino alcohols and their derivatives: DE, 566578[P]. 1927-03-22.
  • 10Legerlotz H. Optically active monohydroxyphenylalkylamines: DE, 543529[P]. 1929-05-28.

共引文献5

同被引文献1

引证文献1

相关作者

内容加载中请稍等...

相关机构

内容加载中请稍等...

相关主题

内容加载中请稍等...

浏览历史

内容加载中请稍等...
;
使用帮助 返回顶部