关键词: Bezafibrate Chemoselectivity Mixed anhydride Reduction of carboxylic acid Sodium borohydride

来  源:   DOI:10.1016/j.rechem.2022.100417   PDF(Pubmed)

Abstract:
A facile method for the reduction of carboxylic acid group of Bezafibrate, an approved drug, is described. The selective reduction of carboxylic acid group to corresponding alcohol was carried out by activation of the carboxylic acid moiety via mixed anhydride followed by the addition of stoichiometric amount of NaBH4 and methanol to obtain the first alcohol variant of Bezafibrate. The reaction was completed in 5-10 min in excellent yield and purity. The new alcohol derivative was characterized by spectroscopic methods. This is the first report on this new molecule.
摘要:
一种简便的还原苯扎贝特羧酸基团的方法,一种被批准的药物,被描述。通过经由混合酸酐活化羧酸部分,随后加入化学计量的NaBH4和甲醇,以获得苯扎贝特的第一醇变体,将羧酸基团选择性还原为相应的醇。反应在5-10分钟内以优异的产率和纯度完成。通过光谱方法对新的醇衍生物进行了表征。这是关于这种新分子的第一份报告。
公众号