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A practical access to fluoroalkylthio(seleno)-functionalized bicyclo1.1.1pentanes
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A practical access to fluoroalkylthio(seleno)-functionalized bicyclo1.1.1pentanes
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Journal Article
A practical access to fluoroalkylthio(seleno)-functionalized bicyclo1.1.1pentanes
2020
Overview
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 SCF
3
, SCF
2
H, SCFH
2
, SeCF
3
, SeC
4
F
9
, and SeC
8
F
17
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.
Publisher
Science China Press,Springer Nature B.V
Subject
