4.7 Article

Exploration of Aryl Phosphates in Palladium-Catalyzed Mono-α-arylation of Aryl and Heteroaryl Ketones

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JOURNAL OF ORGANIC CHEMISTRY
卷 84, 期 10, 页码 6337-6346

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AMER CHEMICAL SOC
DOI: 10.1021/acs.joc.9b00669

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  1. Hong Kong Polytechnic University Start-up Fund [1-BE0Z]
  2. Shenzhen Strategic New Industry Development Research Fund of Shenzhen Science, Technology and Innovation Commission (SZSTI) [JCYJ20180306173843318]

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This paper presents the first general examples of selective palladium-catalyzed mono-alpha-arylation of aryl and heteroaryl ketones with aryl phosphates. The catalyst system, consisting of [Pd(2-butenyl)Cl](2) and MorDalPhos, exhibited high catalytic reactivity toward this reaction. A wide range of aryl phosphates were efficiently coupled with aryl and heteroaryl ketones with good selectivity. Excellent-to-good product yields were afforded. The gram-scale reaction was conducted smoothly. Reductive elimination or transmetalation mightbe a rate-determining step in this reaction.

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