有机化学 ›› 2010, Vol. 30 ›› Issue (02): 282-284. 上一篇    下一篇

研究简报

拟肾上腺素药盐酸甲氧明的绿色合成

谢宇*,胡金刚,贾杰,洪小伟,魏娅   

  1. (南昌航空大学环境与化学工程学院 南昌 330063)
  • 收稿日期:2009-02-25 修回日期:2009-08-04 发布日期:2010-02-20

Green Synthesis of the Adrenomimetic Drug Methoxamine Hydro-chloride

Xie Yu* Hu Jingang Jia Jie Hong Xiaowei Wei Ya   

  1. (School of Environmental and Chemical Engineering, Nanchang Hangkong University, Nanchang 330063)
  • Received:2009-02-25 Revised:2009-08-04 Published:2010-02-20

以对苯二酚为原料经羟基的甲基化、傅克酰基化、肟化、肟基还原、酮胺氢化5步反应合成了盐酸甲氧明, 中间体和目标产物经核磁共振氢谱、红外光谱及元素分析仪确证了其化学结构, 总收率为37.6%. 与传统盐酸甲氧明工艺相比, 该工艺反应条件温和、简便、经济、产率高及对环境友好.

关键词: 甲氧明, 甲基化, 肟化, 还原, 绿色合成

Methoxamine hydrochloride was synthesized from p-dihydroxybenzene by O-methylation, Friedel-Crafts acylation, oximation reaction, oxime reduction and keto-amine hydrogenation reactions. All intermediates and products were characterized by IR, 1H NMR spectra and elemental analysis. The total yield was 37.6%. Compared to the traditional synthetic procedures of methoxamine hydrochloride, the procedures were temperate, convenient, economical, high-yielding and environment-friendly.

Key words: methoxamine, methylation, oximation, reduction, green synthesis