4.8 Article

Trifluoromethylation of Benzoic Acids: An Access to Aryl Trifluoromethyl Ketones

Journal

ORGANIC LETTERS
Volume 23, Issue 12, Pages 4930-4934

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.1c01720

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Funding

  1. Key R&D project of Hainan province [ZDYF2020168]
  2. National Natural Science Foundation of China [21871070]

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The trifluoromethylation of benzoic acids using anhydrides as in situ activating reagents allows for a wide range of carboxylic acids to react efficiently, providing a facile method for preparing aryl trifluoromethyl ketones from readily available starting materials.
The trifluoromethylation of benzoic acids with TMSCF3 was achieved through nucleophilic substitution with the use of anhydrides as an in situ activating reagent. Under the reaction conditions, a wide range of carboxylic acids including the bioactive ones worked well, thus providing a facile and efficient method for preparing aryl trifluoromethyl ketones from the readily available starting materials.

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