简便的区域选择性合成3-O-乙基维生素C

A Facile Regioselective Synthesis of 3-O-Ethy1-L-ascorbic Acid

采用微波辅助法在三乙胺的催化条件下,一步完成3-O-乙基维生素C的区域选择性烷基化反应,通过单因素和L9(34)正交试验确定了最佳反应条件为反应时间8 min,n(VC)∶n(三乙胺)∶n(硫酸二乙酯)=1.0∶1.15∶1.2,功率为200 W,反应总产率可达74.73%(HPLC),该反应条件温和,产率较高,产物选择性好,产物结构经IR和1H NMR得到了确证。

3-O-Ethyl-L-ascorbic acid was regioselectively synthesized in the presence of triethylamine under microwave radiation.Through single-factor and orthogonal experiments,the optimal reaction conditions were： reaction time,8 min;mole ratio of L-ascorbic acid,triethylamine and diethyl sulfate,1.0∶1.15∶1.2;microwave power,200 W.The reaction was readily performed with good yield and good selectivity under mild conditions and convenient operations.The yield of 3-O-ethyl-L-ascorbicacid acid was up to 74.73%（HPLC）.The product was determined by IR and 1H NMR spectroscopy.