Journal
SCIENCE CHINA-CHEMISTRY
Volume 63, Issue 8, Pages 1025-1029Publisher
SCIENCE PRESS
DOI: 10.1007/s11426-020-9733-y
Keywords
bicyclo[1; 1; 1]pentane; propellane; bioisostere; trifluoromethylthio; trifluoromethylseleno
Categories
Funding
- National Natural Science Foundation of China [21722205, 21971173]
- Project of Scientific and Technologic Infrastructure of Suzhou [SZS201905]
- Priority Academic Program Development of Jiangsu Higher Education Institutions (PAPD)
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Rational design of new bioisosteres through introduction of high-value functional groups to bicyclo[1.1.1]pentane (BCP) is of particular use for drug discovery. Disclosed herein is the first access to valuable fluoroalkylthio(seleno)-functionalized BCPs. A range of SCF3, SCF2H, SCFH2, SeCF3, SeC4F9, and SeC8F17 groups are readily incorporated to BCPs under mild conditions. Concomitant installation of a sulfone provides a platform for incorporation of the BCP motif to bioactive molecules. This practical protocol features novel BCP scaffolds, broad substrate scope, excellent atom-economy, simple operation, and gram-scale preparation.
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