【摘要】 以10-甲氧基-5H-二苯并[b,f]氮杂(艹卓)为原料,通过酰氯化、氨解、水解得到抗癫痫药物奥卡西平,总收率达72%左右,纯度大于99%。在10-甲氧基-5H-二苯并[b,f]氮杂(艹卓)酰用量为20 g的情况下,氯化反应的优化条件为:温度105℃,反应时间3.5 h,催化剂用量7.2 g,溶剂甲苯140mL,反应收率在86%左右。应用双(三氯甲基)碳酸酯替代光气,避免了有毒危险性试剂的使用,工艺简洁、操作方便。更多还原

【Abstract】 Synthesis method of oxcarbanzepine(OCBZ) was introduced in this paper.10-methoxy-5H-dibenz(b,f)azepine was used as the starting material,via acylchlorination,ammonolysis and hydrolysis to give OCBZ with the total yield about 72%and purity over 99%.Hydroxyquinoxaline was prepared by reacting phenylenediamine with glyoxylic acid of different grades.The yield is 86%while the optimized conditions were as follows:the temperature of chlorination is 105℃,reaction time is 3.5 h,and the reacting dose of 10-methoxy-5H-dibenz(b,f) azepine,catalyst,toluene are 20 g,7.2 g,140 mL.The above process of initial material of oxcarbazepine was simplified tremendously,thus avoiding the use of a dedicated plant.,which is of great economic and social benefit.更多还原