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<i>cine</i>-Silylative Ring-Opening of α-Methyl Azacycles Enabled by the Silylium-Induced C–N Bond Cleavage

Jianbo Zhang, Sukbok Chang

2020Journal of the American Chemical Society57 citationsDOI

Abstract

Described herein is the development of a borane-catalyzed cine-silylative ring-opening of α-methyl azacycles. This transformation involves four-step cascade processes: (i) exo-dehydrogenation of alicyclic amine, (ii) hydrosilylation of the resultant enamine, (iii) silylium-induced cis-β-amino elimination to open the ring skeleton, and (iv) hydrosilylation of the terminal olefin. The present borane catalysis also works efficiently for the C–N bond cleavage of acyclic tertiary amines. On the basis of experimental and computational studies, the silicon atom was elucidated to play a pivotal role in the β-amino elimination step.

Topics & Concepts

ChemistryCleavage (geology)Bond cleavageRing (chemistry)Medicinal chemistryStereochemistryOrganic chemistryCatalysisComposite materialFracture (geology)Materials scienceOrganoboron and organosilicon chemistryCatalytic Cross-Coupling ReactionsAsymmetric Hydrogenation and Catalysis
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