2,2-二取代-1,3-丙二醇的简便合成及抗菌活性研究

Concise synthesis and antibacterial activities of 2,2-disubstituted propane-1,3-diol

为探究2,2-二取代-1,3-丙二醇类化合物的简便合成方法与抗菌活性,本文研究了硼氢化钠、氢化铝锂、二异丁基氢化铝对2,2-二取代丙二酸二乙酯的还原反应,并研究了产物2,2-二取代-1,3-丙二醇类化合物的体外抗菌活性。结果发现二异丁基氢化铝在室温下能够还原二取代丙二酸二乙酯衍生物,并以较高的产率生成相应的1,3-丙二醇,但低温发生脱羧副反应导致产率降低。体外抗菌活性实验表明,所合成的2,2-二取代-1,3-丙二醇对革兰氏阳性菌金黄色葡萄球菌和蕈状芽孢杆菌具有一定的抑菌活性,MIC 16~32μg·mL^(-1)。本研究为合成2,2-二取代-1,3-丙二醇提供了简便的合成方法,也为开发多元醇类化合物的抗菌剂提供了参考。

To investigate the concise synthesis and antibacterial activities of the 2,2-disubstituted propane-1,3-diol,the reduction of the disubstituted diethyl malonate by sodium borohydride,lithium aluminum tetrahydride and diisobutylaluminum hydride were studied,and the antibacterial activities of the 2,2-disubstituted propane-1,3-diols were investigated.The results showed that diisobutylaluminum hydride could reduce the disubstituted diethyl malonate derivatives in high yields at room temperature,but with the decarboxylation side reaction at low temperature decreasing the yields.The in vitro antibacterial activity experiments showed that the 2,2-disubstituted propane-1,3-diols exhibited antibacterial activities against Gram-positive bacteria staphylococcus aureus and bacillus mycoides,with MIC 16~32μg·mL^(-1).This study provided a concise synthetic method for the synthesis of 2,2-disubstituted propane-1,3-diols,and also provided a reference for the development of antibacterial agents for polyol compounds.