PDF(Pubmed)
Abstract：
A highly efficient and facile protocol for the selective reduction of carboxylic acid of Fenofibric acid to corresponding alcohol was developed. The selective reduction was carried out by activation of carboxylic acid by mixed anhydride followed by the reaction of sodium borohydride in presence of methanol. This is the first example of chemoselective reduction of carboxylic acid to alcohol in presence of a ketone without any external catalyst or ligand in a single step. The reaction offers wide applicability for the selective carboxylic group reduction methodology. The chemoselective reduction was demonstrated by the reduction of Fenofibric acid, an active metabolite of the drug Fenofibrate, to corresponding alcohol in excellent selectivity, yield, and purity.
摘要：
开发了一种高效，简便的方法，用于将非诺贝特酸的羧酸选择性还原为相应的醇。通过用混合酸酐活化羧酸,然后在甲醇存在下使硼氢化钠反应,进行选择性还原。这是在酮存在下在单个步骤中没有任何外部催化剂或配体的情况下将羧酸化学选择性还原为醇的第一个实例。该反应为选择性羧基还原方法提供了广泛的适用性。非诺贝酸的还原证明了化学选择性还原，非诺贝特药物的活性代谢产物，以优异的选择性对相应的醇，产量，和纯洁。
