FSO<sub>2</sub>N<sub>3</sub>-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<sub>2</sub>N<sub>3</sub> 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.
Authors
- Peixiang Ma (ORCID: https://orcid.org/0000-0001-6794-1663)
- Hongtao Xu (ORCID: https://orcid.org/0000-0001-5174-9079)
- Yuang Gu
- An Qin (ORCID: https://orcid.org/0000-0002-8785-8848)
- Qianping Huang (ORCID: https://orcid.org/0009-0001-7130-1279)
- Shuning Zhang (ORCID: https://orcid.org/0009-0007-8664-848X)
Institutions
- Shanghai Jiao Tong University (CN)
- ShanghaiTech University (CN)
- Shanghai Ninth People's Hospital (CN)
Publication Details
- Journal
- ACS Medicinal Chemistry Letters
- Published
- 2024-08-23
- DOI
- https://doi.org/10.1021/acsmedchemlett.4c00307
- Citations
- 9
- Primary Topic
- Chemical Synthesis and Analysis
- Type
- article
- Field-Weighted Citation Impact
- 2.10
Funders
- Natural Science Foundation of Shanghai
- National Natural Science Foundation of China
- China Postdoctoral Science Foundation