胡艾希, 董先明, 曹声春, 程雅平, 陈龙. 一锅重排法合成萘普生J. 药学学报, 2000, 35(11): 818-820.
引用本文: 胡艾希, 董先明, 曹声春, 程雅平, 陈龙. 一锅重排法合成萘普生J. 药学学报, 2000, 35(11): 818-820.
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HU Ai-xi, CAO Sheng-chunCHENG Ya-ping, CHEN Long, DONG Xian-ming, . ONE-POT SYNTHESIS OF dl-NAPROXEN BY REARRANGEMENTJ. Acta Pharmaceutica Sinica, 2000, 35(11): 818-820.
Citation: HU Ai-xi, CAO Sheng-chunCHENG Ya-ping, CHEN Long, DONG Xian-ming, . ONE-POT SYNTHESIS OF dl-NAPROXEN BY REARRANGEMENTJ. Acta Pharmaceutica Sinica, 2000, 35(11): 818-820.
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一锅重排法合成萘普生

ONE-POT SYNTHESIS OF dl-NAPROXEN BY REARRANGEMENT

    摘要
  • 摘要: 目的　“一锅”重排法合成非甾体消炎镇痛药外消旋萘普生。方法　以卤化铜为选择性卤化剂，6-甲氧基-2-丙酰基萘经羰基α-卤化、缩酮化、重排和水解等反应合成外消旋体萘普生。结果　“一锅法”合成萘普生总收率74.0%～92.6%(以6-甲氧基-2-丙酰基萘计)。结论　“一锅重排法”合成萘普生，操作简便，收率较高。

     

    Abstract: AIM　To synthesize dl-naproxen by rearrangement method. METHODS　dl-Naproxen was synthesized by halogenation, ketalization, rearrangement and hydrolysis, using cupric halide as halogenation agent. RESULTS　Total yields were 74.0%～92.6% based on 6-methoxy-2-propionyl naphthalene. CONCLUSION　Total yield was higher by one-pot rearrangement approach.

     

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