2-氟丙二酸二烷基酯的合成及应用

Synthesis and Application of Dialkyl 2-fluoromalonate

很多含氟医药产品都具有氟化单元和三氟甲基芳基结构,其主要原因是由于这些含氟基团能够显著增强医药化合物的活性。生命科学领域越来越多地以三维结构作为先导化合物,这就要求在脂肪族体系和单氟杂环中复杂的有机分子与sp3杂化碳相连。2-氟丙二酸二烷基酯是一种用途广泛的含氟单元,可将氟原子引入脂肪族和芳香族体系。讨论了几种合成2-氟丙二酸二烷基酯的方法,并介绍了2-氟丙二酸二烷基酯在烷基化、酰化、迈克尔加成和生物转化领域的应用,为其他氟化结构含氟药物的合成提供了多种可能性。

Many fluorinated pharmaceutical products have fluorinated units and trifluoromethyl aryl structures, mainly because these fluorinated groups can significantly enhance the activity of pharmaceutical compounds. More and more three-dimensional structures are used as lead compounds in the life sciences, which requires complex organic molecules to be bonded to sp3 hybrid carbons in aliphatic systems and monofluorinated heterocycles. Dialkyl 2-fluoromalonate is a versatile fluorine-containing unit that can introduce fluorine atoms into aliphatic and aromatic systems. In this paper, several methods of synthesis of dialkyl 2-fluoromalonate are discussed, and the applications of dialkyl 2-fluoromalonate in alkylation, acylation, Michael addition and biotransformation are introduced, which provides many possibilities for the synthesis of fluorinated medicines with other structures.