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Transition Metal‐Free Regio‐ and Stereo‐Selective <i>trans</i> Hydroboration of 1,3‐Diynes: A Phosphine‐Catalyzed Access to (<i>E</i>)‐1‐Boryl‐1,3‐Enynes

Swetha Jos, Connor Szwetkowski, Carla Slebodnick, Robert Ricker, Ka Lok Chan, Wing Chun Chan, Udo Radius, Zhenyang Lin, Todd B. Marder, Webster L. Santos

2022Chemistry - A European Journal21 citationsDOIOpen Access PDF

Abstract

We report a transition metal-free, regio- and stereo-selective, phosphine-catalyzed method for the trans hydroboration of 1,3-diynes with pinacolborane that affords (E)-1-boryl-1,3-enynes. The reaction proceeds with excellent selectivity for boron addition to the external carbon of the 1,3-diyne framework as unambiguously established by NMR and X-ray crystallographic studies. The reaction displays a broad substrate scope including unsymmetrical diynes to generate products in high yield (up to 95 %). Experimental and theoretical studies suggest that phosphine attack on the alkyne is a key process in the catalytic cycle.

Topics & Concepts

HydroborationPhosphineChemistryCatalysisTransition metalSelectivityYield (engineering)BoronMedicinal chemistryStereochemistryOrganic chemistryMaterials scienceMetallurgyOrganoboron and organosilicon chemistryCatalytic Cross-Coupling ReactionsCatalytic C–H Functionalization Methods
Transition Metal‐Free Regio‐ and Stereo‐Selective <i>trans</i> Hydroboration of 1,3‐Diynes: A Phosphine‐Catalyzed Access to (<i>E</i>)‐1‐Boryl‐1,3‐Enynes | Litcius