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.
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