A safe, simple, and selective method and reagent for deoxyfluorination is disclosed. With the method and reagent disclosed herein, organic compounds such as carboxylic acids, carboxylates, carboxylic acid anhydrides, aldehydes, and alcohols can be fluorinated by using the most common nucleophilic fluorinating reagents and electron deficient fluoroarenes as mediators under mild conditions, giving corresponding fluoroorganic compounds in excellent yield with a wide range of functional group compatibility and easy product purification. For example, directly utilizing KF for deoxyfluorination of carboxylic acids provides the most economical and the safest pathway to access acyl fluorides, key intermediates for syntheses of peptide, amide, ester, and dry fluoride salts.
揭示了一种安全、简单和选择性的脱氧
氟化方法和试剂。利用本公开的方法和试剂,有机化合物如
羧酸、
羧酸盐、
羧酸酐、醛和醇可以在温和条件下通过使用最常见的亲核
氟化试剂和电子亏损的
氟代
芳烃作为介质进行
氟化,产率极高地得到相应的
氟有机化合物,具有广泛的官能团兼容性和易于产品纯化。例如,直接利用KF对
羧酸进行脱氧
氟化提供了最经济和最安全的途径,以获得酰
氟,这是合成肽、酰胺、酯和干
氟化盐的关键中间体。