超声波法制备2-氟丙酸

Abstract

在许多药物中，含氟类化合物，具有极强的生理活性。α-氟代丙酸是一种手性小分子有机脂肪酸，由于它有一个手性碳，所以在合成应用和某些药物结构修饰中有着重要的意义。本文主要采用了重氮化氟化法和卤化物氟取代法，对α-氟代丙酸的合成进行了研究。重氮化氟化法是一种经典的氟化反应法。然而，应用该方法合成2-氟丙酸转化率较低，文献报道仅有14%。而使用氟化物(如氟化钾)在超声波的条件下直接氟化，其转化率相比重氮化氟化方法大为提高。 In many drugs, fluorochemicals have a strong physiological activity. α-fluorine propionic acid is a small chiral organic molecule; since it has an asymmetric carbon, it has an important significance in application of organic synthesis and some drugs’ structural modification. In this paper, the syn-thesis of 2-fluorine propionic acid was studied, using fluorinated diazotization method and halogen fluorination method. It is a classic method of diazotization for fluorination. However, the reaction transformation rate is low when the method is applied to the synthesis of 2-fluorine propionic acid, which is only 14% in literatures. And the reaction transformation rate may be greatly improved by using fluoride (such as potassium fluoride) under ultrasonic condition compared with fluorinated diazotization method.