Journal
JOURNAL OF ORGANIC CHEMISTRY
Volume 87, Issue 5, Pages 2551-2558Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.joc.1c02496
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Funding
- National Natural Science Foundation of China [21907011, 22107016, 22107017]
- Fundamental Research Funds for the Central Universities [2020CQJQY-Z002, 2021CDJYGRH-002]
- graduate research and innovation foundation of Chongqing, China [CYB21074]
- Beijing National Laboratory for Molecular Sciences [BNLMS202104]
- Natural Science Foundation of Chongqing [cstc2020jcyj-jqX0009, cstc2021jcyj-msxmX0016, cstc2021jcyj-cxttX0002]
- China Postdoctoral Science Foundation [2020M683251]
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This study reported a new DNA-compatible protocol for the transformation of amines into drug-like moieties, expanding the application of DNA-encoded chemical libraries.
The incorporation of the isoindole core into the DNA-encoded chemical library is highly desirable for the great potential pharmacological characters exampled by molecules like lenalidomide. Herein, we reported a DNA-compatible protocol for the OPA-mediated transformation of amines into drug-like moieties represented by isoindolinone and thio-2-isoindole, respectively. The high conversion and wide substrate-scope property of our protocol render its feasibility in the manipulation of terminal amines on oligonucleotide conjugates, including cap-and-catch purification, sequential synthesis during DEL construction, and on-DNA macrocyclization.
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