有机化学 ›› 2017, Vol. 37 ›› Issue (11): 2985-2992.DOI: 10.6023/cjoc201703050 上一篇    下一篇

研究论文

铟粉促进下“一锅法”合成α-亚甲基-γ-三氟甲基-γ-丁内酰胺化合物

李军, 黄丹凤, 张怀远, 张兴虎, 王娟娟, 王克虎, 苏瀛鹏, 胡雨来   

  1. 西北师范大学化学化工学院 兰州 730070
  • 收稿日期:2017-03-30 修回日期:2017-07-03 发布日期:2017-07-14
  • 通讯作者: 黄丹凤, 胡雨来 E-mail:huangdf@nwnu.edu.cn;huyl@nwnu.edu.cn
  • 基金资助:

    国家自然科学基金(Nos.21662030,21462037)资助项目.

Indium-Promoted Preparation of α-Methylene-γ-trifluoromethyl-γ-lactams via One-Pot Reaction

Li Jun, Huang Danfeng, Zhang Huaiyuan, Zhang Xinghu Wang Juanjuan, Wang Ke-Hu, Su Yingpeng, Hu Yulai   

  1. College of Chemistry and Chemical Engineering, Northwest Normal University, Lanzhou 730070
  • Received:2017-03-30 Revised:2017-07-03 Published:2017-07-14
  • Contact: 10.6023/cjoc201703050 E-mail:huangdf@nwnu.edu.cn;huyl@nwnu.edu.cn
  • Supported by:

    Project supported by the National Natural Science Foundation of China (Nos. 21662030, 21462037).

探索了铟粉促进下,三氟乙醛甲基半缩醛或三氟苯乙酮与酰肼、2-(溴甲基)丙烯酸乙酯的"一锅法"反应,得到了一系列α-亚甲基-γ-三氟甲基-γ-丁内酰胺化合物.该方法使用价廉易得的三氟乙醛甲基半缩醛或三氟苯乙酮作为三氟甲基合成砌块,反应条件温和、产率高、操作简单,为合成含三氟甲基的α-亚甲基-γ-丁内酰胺化合物提供了一种新方法.

关键词: 一锅法, 铟粉, 三氟乙醛甲基半缩醛, 三氟苯乙酮, 2-(溴甲基)丙烯酸乙酯, 酰肼, α-亚甲基-γ-三氟甲基-γ-丁内酰胺

An one-pot reaction of trifluoroacetaldehyde methyl hemiacetal or trifluoroketones, acylhydrazines and ethyl 2-(bromomethyl)acrylate promoted by indium powder has been investigated and a series of α-methylene-γ-trifluoromethyl-γ-lactams were obtained with high yieds. The features of this process include readily available starting materials as trifluoromethyl source, mild conditions and easy operation. The reaction provides a new method for the snythesis of trifluoromethylated α-methylene-γ-lactams.

Key words: one-pot, indium powder, trifluoroacetaldehyde methyl hemiacetal, trifluoroketone, 2-(bromomethyl) acrylate, arylacylhydrazine, α-methylene-γ-trifluoromethyl-γ-lactams