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Synthesis and chemical transformations of diazolyl α,α-difluoroacetates

J. Fluorine Chem. 2020, 229

DOI: 10.1016/j.jfluchem.2019.109407

Geraschenko O.; Solomin V.; Vashchenko B.; Khodakivskyi P.; Tolmachev A.; Grygorenko O.

Optimized protocols for the synthesis of diazolyl α,α-difluoroacetates via deoxofluorination of the corresponding glyoxylates with Morph-DAST are described. The method allowed the preparation of the title fluoridated building blocks in 73–96 % yield on up to 15 g scale. Utility of the hetaryl α,α-difluoroacetates was demonstrated by the synthesis of advanced building blocks for medicinal chemistry, i.e. carboxylic acids, amides, nitriles, and alcohols.

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