Qianping Huang; Yuang Gu; An Qin; Peixiang Ma; Hongtao Xu; Shuning Zhang
ACS Med. Chem. Lett., 2024, 15(9), 1591–1597
https://doi.org/10.1021/acsmedchemlett.4c00307

Abstract

DNA-encoded library (DEL) is a powerful hit selection technique in both basic science and innovative drug discovery. In this study, we report a robust and straightforward DNA-compatible diazo-transfer reaction utilizing FSO2N3 as the diazo-transfer reagent in solution. This reaction demonstrates high conversions and facile operation while being metal-free and maintaining high levels of DNA fidelity. It is also compatible with a wide range of substrates, allowing for convenient access to both aliphatic and aromatic amines. Consequently, it will further enrich the DEL chemistry toolbox.