Progress in Enzyme-Catalyzed C(sp3)–H Amination

Amine structures are widely present in various biologically active natural products, drug molecules, and material structures. Among the various strategies of amine synthesis, C(sp³)–H amination has become a powerful strategy due to its atom economy and multiple potential reaction sites compared with conventional amine synthesis methods. Due to the advantages of high catalytic efficiency, high selectivity, environmental friendliness, and high modifiability of the enzyme, the enzymatic C(sp³)–H amination is of great research significance. However, it was not until recent years that natural enzymes capable of catalyzing the amination of C(sp³)–H bonds were discovered. Modifying enzymes to confer unnatural C(sp³)–H amination activity holds great potential. In the past decade, a series of protocols for the amination of C(sp³)–H bonds using engineered enzymes have been developed, several of which showed comparable properties to those of natural enzymes.