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Updated: Jul 27, 2025

A Microwave-Assisted Direct Heteroarylation of Ketones Using Transition Metal Catalysis
Published on: February 16, 2020
Metallaphotoredox-Mediated Decarboxylative Cross-Coupling of α-Oxy Morpholine Carboxylic Acids and (Hetero)Aryl
Jack L Sloane1, Anna Beatriz Santos1, Eric M Simmons2
1Small Molecule Drug Discovery, Bristol Myers Squibb, Cambridge, Massachusetts 02142, United States.
Abstract:
A decarboxylative C(sp2)-C(sp3) cross-coupling reaction of α-oxy carboxylic acids using dual nickel/photoredox catalysis has been developed for the synthesis of complex morpholines and other saturated heterocycles, affording direct entry to scaffolds of interest in drug discovery. This chemistry can be applied to the coupling of an array of (hetero)aryl halides and α-heteroatom acids, providing C(sp2)-C(sp3)-coupled products in modest to excellent yields and enabling access to intermediates that can be further derivatized to multivector architectures.
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