摘要
分析了双氢青蒿素醚化反应的机理。通过单因素实验和正交实验对影响β-蒿甲醚合成的主要因素二氯甲烷用量、催化剂用量、反应温度和反应时间进行了优化,确定最佳工艺条件如下:二氯甲烷与甲醇的体积比为4∶1、双氢青蒿素与三氟乙酸的摩尔比为10∶1、反应温度为40℃、反应时间为2.5 h,此时β-蒿甲醚的产率达到69.9%,用HPLC直接分析法测定其平均含量达到99.29%。
The etherification mechanism of dihydroartemisinine was analyzed. The dominant influential factors for synthesis of β-ARM such as the amount of dichloromethane, the amount of catalyst, the reaction temperature and the reaction time were optimized through single factor experiment and orthogonal experiment. The optimum etherification conditions for dihydroartemisinine were determined as follows: the volume ratio of dichloromethane to methanol was 4 : 1, the molar ratio of dihydroartemisinine to trifluoroacetic acid was 10: 1, the reaction temperature was 40℃ and the reaction time was 2.5 h. Under above conditions,the yield of fl-ARM reached 69.9%. In addition,its average content reached 99.29% determined by HPLC method.
出处
《化学与生物工程》
CAS
2009年第6期54-58,共5页
Chemistry & Bioengineering