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Deprotonative Functionalization of the Difluoromethyl Group

Laura L. Santos, Armen Panossian, Morgan Donnard, Jean‐Pierre Vors, Sergii Pazenok, David Bernier, Frédéric R. Leroux

2020Organic Letters32 citationsDOIOpen Access PDF

Abstract

The functionalization of 3-(difluoromethyl)pyridine has been developed via direct deprotonation of -CHF 2 with a lithiated base and subsequent trapping with various electrophiles in THF. In situ quenching gives access to 3-pyridyl-CF 2 -SiMe 2 Ph as a new silylated compound, which can be postfunctionalized with a fluoride source to obtain a larger library of 3-(difluoroalkyl)pyridines that could not be accessed via direct deprotonation.

Topics & Concepts

DeprotonationChemistryElectrophileSurface modificationPyridineFluorideTrappingGroup (periodic table)Quenching (fluorescence)Medicinal chemistryCombinatorial chemistryPhotochemistryOrganic chemistryCatalysisInorganic chemistryPhysical chemistryIonEcologyQuantum mechanicsBiologyPhysicsFluorescenceFluorine in Organic ChemistryInorganic Fluorides and Related CompoundsSynthesis and Reactions of Organic Compounds
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