4.8 Article

Palladium-Catalyzed Fluorocarbonylation Using N-Formylsaccharin as CO Source: General Access to Carboxylic Acid Derivatives

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ORGANIC LETTERS
卷 15, 期 20, 页码 5370-5373

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AMER CHEMICAL SOC
DOI: 10.1021/ol4026815

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  1. Daiichi Sankyo Co., Ltd.
  2. Grants-in-Aid for Scientific Research [23790016] Funding Source: KAKEN

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N-Formylsaccharin, an easily accessible crystalline compound, has been employed as an efficient CO source in Pd-catalyzed fluorocarbonylation of aryl halides to afford the corresponding acyl fluorides in high yields. The reactions use a near-stoichiometric amount of the CO source (1.2 equiv) and tolerate diverse functional groups. The acyl fluorides obtained could be readily transformed into various carboxylic acid derivatives such as carboxylic acid, esters, thioesters, and amides in a one-pot procedure.

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