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一种有效的芳基乙酮α-溴代的实用方法

邢瑞娟, 潘莉, 温西, 王健, 程卯生*   

  1. 沈阳药科大学 制药工程学院 基于靶点的药物设计与研究教育部重点实验室, 辽宁 沈阳 110016
  • 收稿日期:2009-12-23 修回日期:2010-07-30 出版日期:2010-09-20 发布日期:2010-09-20
  • 通讯作者: 程卯生*

A practical and efficient procedure for the α-bromination of arylethanones

Rui-Juan Xing, Li Pan, Xi Wen, Jian Wang, Mao-Sheng Cheng*   

  1. Key Laboratory of Structure-Based Drugs Design & Discovery of Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China
  • Received:2009-12-23 Revised:2010-07-30 Online:2010-09-20 Published:2010-09-20
  • Contact: Mao-Sheng Cheng*

摘要: 本文报道了采用溴素进行羰基α-溴代反应而后经亚磷酸二乙酯和三乙胺脱溴反应制得羰基α-单溴代物的方法, 该方法具有实用、收率高和易于工业化等优点。

关键词: α-溴代芳基乙酮, 溴, 亚磷酸二乙酯, α-溴代

Abstract:

A series of α-bromoarylethanones were prepared in high yields by a practical and efficient method. The arylethanones were reacted with bromine to give a mixture of α- and α, α-dibromides, which were debrominated with diethylphosphite in the presence of triethylamine to give the desired α-monobromo products.

Key words: α-Bromoarylethanones, Bromine, Diethylphosphite, α-Bromination

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Supporting: *Corresponding author. Tel.: 86-24-23986413; fax: 86-24-23995043