Synthesis of Thiohydantoin Scaffolds on DNA for Focused DNA-Encoded Library Construction
Thiohydantoin represents a significant class of biologically active privileged heterocyclic scaffolds. Herein, we present a convenient and robust DNA-compatible method for constructing a thiohydantoin-focused DNA-encoded library. This reaction can be applied to a wide variety of isothiocyanate partners, arylamine feedstocks, and diverse α-amine acid derivatives, exhibiting excellent conversions, high functional group tolerance, and preservation of DNA tag integrity. Our method allows for easy access to a valuable three-cycle thiohydantoin-focused DNA-encoded library.
Authors
- Xianfu Fang (ORCID: https://orcid.org/0000-0002-0648-9340)
- Yangfeng Li (ORCID: https://orcid.org/0000-0002-4780-6154)
- Gong Zhang (ORCID: https://orcid.org/0000-0002-6992-176X)
- Yizhou Li (ORCID: https://orcid.org/0000-0003-1650-3780)
- Yunzhu Ju
- Jiayou Wang
Institutions
- Chongqing University (CN)
- Chongqing Three Gorges University (CN)
Publication Details
- Journal
- Organic Letters
- Published
- 2024-10-03
- DOI
- https://doi.org/10.1021/acs.orglett.4c03369
- Citations
- 8
- Primary Topic
- Chemical Synthesis and Analysis
- Type
- article
- Field-Weighted Citation Impact
- 1.87
Funders
- National Natural Science Foundation of China
- Natural Science Foundation of Chongqing
- Fundamental Research Funds for the Central Universities