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FSO 2 N 3 -Mediated On-DNA Diazo-Transfer Chemistry

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 FSO N as the diazo-transfer reagent in solution. This reaction demonstrates high...

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Bibliographic Details
Published in:ACS medicinal chemistry letters 2024-09, Vol.15 (9), p.1591-1597
Main Authors: Huang, Qianping, Gu, Yuang, Qin, An, Ma, Peixiang, Xu, Hongtao, Zhang, Shuning
Format: Article
Language:English
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Summary: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 FSO N 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.
ISSN:1948-5875
1948-5875
DOI:10.1021/acsmedchemlett.4c00307