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Synthesis and chemical transformations of diazolyl α,α-difluoroacetates
Journal of Fluorine Chemistry ( IF 1.7 ) Pub Date : 2019-11-30 , DOI: 10.1016/j.jfluchem.2019.109407
Oleksandr V. Geraschenko , Vitalii V. Solomin , Bohdan V. Vashchenko , Pavlo Khodakivskyi , Andrey A. Tolmachev , Oleksandr O. Grygorenko

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



中文翻译:

重氮基α,α-二氟乙酸酯的合成与化学转化

描述了通过Morph-DAST通过相应的乙醛酸酯的脱氧氟化合成重氮基α,α-二氟乙酸酯的优化方案。该方法可以制备标题氟化的构建基块,产率最高为15 g时为73–96%。α,α-二氟乙酸杂芳基酯的实用性已通过合成用于药物化学的高级构件(即羧酸,酰胺,腈和醇)得到了证明。

更新日期:2019-11-30
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