有机化学 ›› 2019, Vol. 39 ›› Issue (2): 538-543.DOI: 10.6023/cjoc201808023 上一篇    下一篇

研究简报

聚乙二醇200溶剂中镍催化合成喹唑啉酮衍生物

许贻文, 张鹏, 刘彩琴, 林晨, 林小燕, 柯方   

  1. 福建医科大学药学院 福州 350004
  • 收稿日期:2018-08-20 修回日期:2018-09-10 发布日期:2018-09-26
  • 通讯作者: 柯方 E-mail:kefang@163.com
  • 基金资助:

    福建省自然科学基金(Nos.2016J01686,2016J01372,2016Y9051,2017J01820)和福建医科大学基金(No.2015MP008)资助项目.

Nickel-Catalyzed Synthesis of Quinazolinone Derivatives in Polyethylene Glycol 200

Xu Yiwen, Zhang Peng, Liu Caiqin, Lin Chen, Lin Xiaoyan, Ke Fang   

  1. Department of Pharmacy, Fujian Medical University, Fuzhou 350004
  • Received:2018-08-20 Revised:2018-09-10 Published:2018-09-26
  • Contact: 10.6023/cjoc201808023 E-mail:kefang@163.com
  • Supported by:

    Project supported by the Natural Science Foundation of Fujian Province (Nos. 2016J01686, 2016J01372, 2016Y9051, 2017J01820) and the Research Fund of Fujian Medical University (No. 2015MP008).

以廉价、易得的氯化镍与脯氨酸锂为催化剂,在聚乙二醇200(PEG 200)溶剂中建立一种操作简单、经济环保的2-卤代苯甲酸和脒类盐酸盐合成喹唑啉酮衍生物的方法.该方法具有操作简便、无毒和无刺激的特点,均能以较高的产率得到一系列喹唑啉酮类衍生物,最高产率达94%.

关键词: 聚乙二醇(PEG 200), 喹唑啉酮, 氯化镍, 2-卤代苯甲酸, 脒盐

A simple and economic method for synthesizing quinazolinones from substituted 2-halobenzoic acids and amidines was developed by nickel-catalysis in wet polyethylene glycol 200 (PEG 200) as an eco-friendly medium. The present methodology is operationally simple, non-toxic and non-irritative, and varieties of quinazolinone derivatives were obtained in high yields of up to 94%.

Key words: polyethylene glycol 200 (PEG 200), quinazolinone, nickel chloride, 2-halobenzoic acid, amidine