一种制备二羟丙茶碱的新工艺

A new process to prepare dihydroxypropyl theophylline

目的针对现有二羟丙茶碱工艺方法收率低,副产物较多,对环保产生较大压力的问题,研发了一种制备二羟丙茶碱的新工艺。方法采用有机相代替水相反应,并采用弱碱性盐类作为催化剂,生成二羟丙茶碱。结果确定了生产二羟丙茶碱的最佳反应条件为DMF/无水碳酸钾体系,茶碱:氯丙醇=1∶1.2,氯丙醇滴加30min,二羟丙茶碱收率由原工艺的66%提高到82%,减少副产物产生。结论该新工艺提高了二羟丙茶碱的收率,减少副产物残留,具有很好的工业化前景。

Objective To study a new process to prepare dihydroxypropyl theophylline to solve problems caused by previous process,including low yield,more by-products and great pressure on environmental protection. Methods Organic phase was used to replace aqueous phase to react and weak alkali salts was used as catalyst to prepare dihydroxypropyl theophylline. Results Optimum reaction condition of preparing dihydroxypropyl theophylline was DMF/anhydrous potassium carbonate system.Theophylline： Chloropropanol=1 ∶ 1.2 When Chloropropanol was dropped for 30 minutes,yield of dihydroxypropyl theophylline was increased to 82% from primary 66% and byproducts became fewer. Conclusion This new process can increase yield of dihydroxypropyl theophylline and decrease by-products residual,which has good Industrialization prospect.