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Updated: Feb 19, 2026

A Microwave-Assisted Direct Heteroarylation of Ketones Using Transition Metal Catalysis
Published on: February 16, 2020
Versatile Alkylation of (Hetero)Aryl Iodides with Ketones via β-C(sp3)-H Activation
Ru-Yi Zhu1, Luo-Yan Liu1, Han Seul Park1
1Department of Chemistry, The Scripps Research Institute , La Jolla, California 92037, United States.
Abstract:
We report Pd(II)-catalyzed β-C(sp3)-H (hetero)arylation of a variety of ketones using a commercially available 2,2-dimethyl aminooxyacetic acid auxiliary. Facile installation and removal of the auxiliary as well as its superior scope for both ketones and (hetero)aryl iodides overcome the significant limitations of the previously reported β-C(sp3)-H arylation of ketones. The ready availability of ketones renders this reaction a broadly useful method for alkyl-(hetero)aryl coupling involving both primary and secondary alkyls.
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