有机化学 ›› 2018, Vol. 38 ›› Issue (4): 719-737.DOI: 10.6023/cjoc201710002 上一篇    下一篇

综述与进展

亚氨基砜衍生物的合成研究进展(封面文章)

周豪, 陈知远   

  1. 江西师范大学化学化工学院 功能有机小分子教育部重点实验室 南昌 330022
  • 收稿日期:2017-10-06 修回日期:2017-11-29 发布日期:2017-12-15
  • 通讯作者: 陈知远 E-mail:zchen@jxnu.edu.cn
  • 基金资助:

    国家自然科学基金(Nos.21462022,21672085)资助项目.

Recent Achievements in the Synthesis of Sulfoximine Derivatives

Zhou Hao, Chen Zhiyuan   

  1. Key Laboratory of Functional Small Organic Molecules, Ministry of Education, College of Chemistry & Chemical Engineering, Jiangxi Normal University, Nanchang 330022
  • Received:2017-10-06 Revised:2017-11-29 Published:2017-12-15
  • Contact: 10.6023/cjoc201710002 E-mail:zchen@jxnu.edu.cn
  • Supported by:

    Project supported by the National Natural Science Foundation of China (Nos. 21462022, 21672085).

亚氨基砜系列化合物具有广泛的生物或药物活性.近年来,在过渡金属催化下,亚氨基砜系列化合物的合成取得了长足的进展.直接以NH-亚氨基砜作为反应底物,可实现N-H键的直接官能团化反应,如炔基化、烯基化、烷基化、芳基化等等.此外,利用S=NH结构片段作为分子内的导向基团,还可以实现底物分子内芳香环的C(sp2)-H活化反应,合成结构各异的芳(杂)环衍生物.综述了亚氨基砜化合物N-H官能化反应和C-H官能化反应,并对部分反应的机理进行了讨论.

关键词: NH-亚氨基砜, 过渡金属催化, C-H官能化反应

The sulfoximine derivatives are widely known for their potent biological and medicinal activities. Recently, due to the transition-metal catalysis, great advancements have been achieved in the synthesis of sulfoximine derivatives. Utilizing free NH-sulfoximines as the starting materials, various the direct N-H functionalizations can be accomplished, such as alkynylation, alkenylation, alkylation, arylation, etc. In addition, the ortho arene C(sp2)-H activation can also be obtained through C-H activation reaction with the assistance of S=NH as intramolecular directing groups, thus giving varies (hetero)aromatic molecules. N-H and C-H functionalization reactions of sulfoximines were summarized, and the mechanisms of some novel model reactions are also briefly discussed.

Key words: NH-sulfoximine, transition-metal-catalysis, C-H functionalization