Ether-Directed Enantioselective C(sp)-H Borylation for the Synthesis of Axially Chiral Biaryls.

Org Lett

State Key Laboratory of Petroleum Molecular & Process Engineering, Shanghai Key Laboratory of Green Chemistry and Chemical Processes, School of Chemistry and Molecular Engineering, East China Normal University, Shanghai 200062, China.

Published: April 2025


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Article Abstract

We report an ether-directed enantioselective C(sp)-H borylation catalyzed by a chiral bidentate boryl ligand (CBL)/iridium system for constructing axially chiral biaryls. This method delivered diverse chiral biaryls with good to high enantioselectivities, accommodating varied electronic and steric substituents on the aryl rings. Gram-scale synthesis and downstream transformations of the C-B bond underscored its practicality.

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http://dx.doi.org/10.1021/acs.orglett.5c00919DOI Listing

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