Deoxyfluorination of Carboxylic Acids via an In Situ Generated Trifluoromethoxide Salt

利用原位生成的三氟甲氧基盐对羧酸进行脱氧氟化反应

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Abstract

An in situ generated pyridinium trifluoromethoxide salt (PyOCF(3)) is a highly effective deoxyfluorination reagent for the synthesis of acid fluorides. PyOCF(3) is formed at room temperature from the reaction of 2,4-dinitro(trifluoromethoxy)benzene with 4-dimethylaminopyridine. PyOCF(3) undergoes slow release of fluorophosgene and fluoride, which serve as the electrophile and nucleophile, respectively, for deoxyfluorination. A wide substrate scope and high functional group tolerance are demonstrated. Furthermore, the acid fluorides can be purified by filtration and telescoped to various known reactions.

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