4.8 Article

Direct Arylation of Azoles Enabled by Pd/Cu Dual Catalysis

Journal

ORGANIC LETTERS
Volume 23, Issue 6, Pages 1996-2001

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.1c00100

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Funding

  1. Merck Sharp Dohme Corp.

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A practical method for the synthesis of 2-arylazoles via direct arylation using a Pd/Cu cocatalyst system with low catalyst loadings is described. The reaction conditions are tolerant of a wide range of functional groups and nitrogen-containing hetero-cycles commonly used in drug discovery.
A practical approach toward the synthesis of 2-arylazoles via direct arylation is described. The transformation relies on a Pd/Cu cocatalyst system that operates with low catalyst loadings. The reaction conditions were found to be tolerant of a wide range of functional groups and nitrogen-containing hetero-cycles commonly employed in a drug discovery setting.

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