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Highly Selective C–F Bond Functionalization of Tetrasubstituted <i>gem</i>-Difluoroalkenes and Trisubstituted Monofluoroalkenes Using Grignard Reagents

Yanhui Wang, Yihan Tang, Yuwei Zong, Gavin Chit Tsui

2022Organic Letters28 citationsDOI

Abstract

We herein describe selective C–F bond functionalizations of tetrasubstituted gem-difluoroalkenes and trisubstituted monofluoroalkenes using Grignard reagents without the transition metal catalyst. β,β-Difluoroacrylates react with Grignard reagents under mild conditions to afford tetrasubstituted (E)-β-monofluoroacrylates. Experimental and computational studies revealed that the selectivity stems from the intrinsic reactivity difference between the (E)- and (Z)-isomers toward excess Grignard reagent, which leads to the resolution of the two products.

Topics & Concepts

ChemistryReagentReactivity (psychology)Grignard reagentCombinatorial chemistrySurface modificationSelectivityCatalysisMedicinal chemistryOrganic chemistryPathologyPhysical chemistryAlternative medicineMedicineFluorine in Organic ChemistryCyclopropane Reaction MechanismsCarbohydrate Chemistry and Synthesis
Highly Selective C–F Bond Functionalization of Tetrasubstituted <i>gem</i>-Difluoroalkenes and Trisubstituted Monofluoroalkenes Using Grignard Reagents | Litcius