Ying Yao,Haozhi Jing,Wanting Cui,Kangyin Pan,Guang Yang,Hongtao Xu

Organic Letters

DOI: 10.1021/acs.orglett.6c01622

Abstract

To incorporate the N-sulfonylguanidine chemotype into DNA-encoded libraries (DELs), a cobalt-promoted, DNA-compatible N-sulfonylguanidine formation method has been developed. This method utilizes DNA-conjugated sulfonyl azides, isonitriles, and amines as readily accessible building blocks to enable modular, high-yielding synthesis of structurally diverse N-sulfonylguanidines, a privileged scaffold widely represented in biologically active small molecules.