Chinese Journal of Organic Chemistry ›› 2023, Vol. 43 ›› Issue (7): 2351-2367.DOI: 10.6023/cjoc202212012 Previous Articles     Next Articles



董思凡, 李昊龙, 秦源, 范士明*(), 刘守信*()   

  1. 河北科技大学 省部共建国家重点实验室培育基地-河北省药用分子化学实验室 石家庄 050018
  • 收稿日期:2022-12-09 修回日期:2023-02-03 发布日期:2023-03-07
  • 通讯作者: 范士明, 刘守信
  • 基金资助:
    国家自然科学基金(21978067); 河北省自然科学基金(H2020208030); 河北省药用分子化学重点实验室开放课题基金(2022PT03)

Research Progress of Amino Acids as Transient Directing Groups in C—H Bond Activation Reactions

Sifan Dong, Haolong Li, Yuan Qin, Shiming Fan(), Shouxin Liu()   

  1. State Key Laboratory Breeding Base-Hebei Province Key Laboratory of Molecular Chemistry for Drug, Hebei University of Science and Technology, Shijiazhuang 050018
  • Received:2022-12-09 Revised:2023-02-03 Published:2023-03-07
  • Contact: Shiming Fan, Shouxin Liu
  • Supported by:
    National Natural Science Foundation of China(21978067); Natural Science Foundation of Hebei Province(H2020208030); the Open Funding Project of the Hebei Province Key Laboratory of Molecular Chemistry for Drug(2022PT03)

In recent years, the transient directing group (TDG)-based strategy of C—H activation has attracted significant attention. Compared with the typical C—H activation reactions, TDG-assisted C—H activation does not require external pre-installation and post-removal steps of directing groups, which significantly improve the atom and step economy. Amino acid-based TDGs for C—H activation have achieved significant successes among the known TDGs. Amino acids have the advantages including low cost, widely existing and diverse structures. The site selectivity of C—H activation can be controlled by using α- or β-amino acids. By using the inherent chirality of amino acids, the stereo-selectivity of reactions can be realized. The research progress of transition-metal-catalyzed C—H bond activation and functionalization with amino acids as TDGs in recent years is summarized, which is classified according to the type of amino acids for C—H activation reactions of various substrates. Finally, the limitations of previous works and perspectives on this cutting-edge area are also described.

Key words: transient directing group, amino acid, C—H activation, transition metal