Jiang-Hao's work appears in iScience! Check it out!
发布时间：2023-03-04
Highlights
- 1.
A direct deaminative halogenation of primary amines mediated by N-anomeric amide
- 2.
Mild reaction conditions, broad substrate scope, and good to high yields
- 3.
The successful decoration of some drugs demonstrated the robustness of our method
Summary
The primary amino group has been seldom utilized as a transformable functionality in organic synthesis. Reported herein is a deaminative halogenation of primary amines using N-anomeric amide as the nitrogen-deletion reagent. Both aliphatic and aromatic amines are competent substrates for direct halogenations. The mildness and robustness of the protocol is evidenced by the successful reactions of several complex and functional group-enriched bioactive compounds or drugs. Elaboration of the resulting products provides interesting analogues of drug molecules.
For more detail:
https://www.cell.com/iscience/fulltext/S2589-0042(23)00332-2