Abstract

AbstractWe have developed an efficient ligand‐free copper‐catalyzed regio‐ and stereoselective carbo‐borylation of heteroatom‐substituted internal alkynes using bis(pinacolato)diboron as boron source and alkyl halides as an electrophile. Both chemical yields and functional group tolerance are excellent. Our method provides an efficient synthesis of tri‐ and tetra‐substituted alkenylboronates which could be further transformed to highly substituted alkenes via subsequent cross‐coupling reactions in one pot.magnified image

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