有机化学 ›› 2014, Vol. 34 ›› Issue (6): 1227-1230.DOI: 10.6023/cjoc201311035 上一篇    下一篇

研究简报

一种氨基甲酰氯的选择性酰化法

郎明, 颜瑞佐, 王玉强, 于沛   

  1. 暨南大学药学院 广州 510632
  • 收稿日期:2013-11-20 修回日期:2014-01-15 发布日期:2014-02-14
  • 通讯作者: 于沛 E-mail:pennypeiyu@163.com
  • 基金资助:

    广州市国际科技合作(No. 11S52070024)资助项目.

A Selective O- and N-Acylation Protocol for Carbamyl Chloride

Lang Ming, Yan Ruizuo, Wang Yuqiang, Yu Pei   

  1. College of Pharmacy, Jinan University, Guangzhou 510632
  • Received:2013-11-20 Revised:2014-01-15 Published:2014-02-14
  • Supported by:

    Project supported by the Guangzhou International Science and Technology Cooperation Projects (No. 11S52070024).

采用3-(1-甲胺基乙基)苯酚为原料,在同一分子中有氨基(胺)和羟基同时存在下,通过改变碱的强弱,用氨基甲酰氯可选择性地进行羟基或氨基上酰化反应,一步获得相应的酯或酰胺,所合成化合物用1H NMR,13C NMR,ESI MS和HRMS进行了结构确证,并对其反应机理进行了推测. 该反应步骤简单,收率高,是一种高效实用的选择性酰化方法.

关键词: 氨基甲酰氯, 酰化, 选择性, 合成方法

A practical and efficient selective O- and N-acylation protocol for carbamyl chloride by using different bases was developed. The structures of the products were identified by 1H NMR, 13H NMR, ESI-MS and HRMS. The mechanism for the selective acylation is proposed.

Key words: carbamyl chloride, acylation, selectivity, synthetic method