Zhaomei Sun; Jie Zhang; Huanqing Zhang; Hongli Cao; Lingqian Xiao; Kexin Yang; Yunjin Hu
Bioconjugate Chem., 2022, 33, 9, 1585-1594
https://doi.org/10.1021/acs.bioconjchem.2c00340

Abstract

Through a modified Kinugasa reaction, a novel method of amidation on terminal oligo alkyne conjugates by copper-promoted oxidation with nitrones has been developed. Unprotected bifunctional carboxylic acid–amine reagents can be transformed directly to the respective amide products under these edited Kinugasa reaction conditions. 3-Cycle DNA-encoded libraries (DELs) can be built in three steps of chemical conversion.