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Radical 1‐Fluorosulfonyl‐2‐alkynylation of Unactivated Alkenes

Nils Lennart Frye, Constantin G. Daniliuc, Armido Studer

2021Angewandte Chemie International Edition64 citationsDOIOpen Access PDF

Abstract

Abstract Sulfonyl fluorides have found widespread use in chemical biology and drug discovery. The development of synthetic methods for the introduction of the sulfonyl fluoride moiety is therefore of importance. Herein, a transition‐metal‐free radical 1,2‐difunctionalization of unactivated alkenes via FSO 2 ‐radical addition with subsequent vicinal alkynylation to access β‐alkynyl‐fluorosulfonylalkanes is presented. Alkynyl sulfonyl fluorides are introduced as highly valuable bifunctional radical trapping reagents that also serve as FSO 2 ‐radical precursors. The β‐alkynyl‐fluorosulfonylalkanes obtained in these transformations can be readily diversified by using SuFEx click chemistry to obtain sulfonates and sulfonamides.

Topics & Concepts

SulfonylAlkynylationMoietyChemistryFluorideCombinatorial chemistryRadicalDrug discoveryOrganic chemistryCatalysisInorganic chemistryBiochemistryAlkylSulfur-Based Synthesis TechniquesRadical Photochemical ReactionsFluorine in Organic Chemistry
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