Process For Synthesis Of Oxcarbazepine

Oxcarbazepine(OCBZ) is a ketone base derivative of Carbamazepine(CBZ).Compared with CBZ, OCBZ show an improved tolerability and liver enzyme induction. Been regarded new-type front-line medicine as resisted the epilepsy in a lot of countuies at present ,it is used in clinic to substitute CBZ.Based on the review of the literatures, two synthesis routes of oxcarbazepine are described.Firstly, the 10-methoxy-5H-dibenz[b, f]azepine is synthesized through brominating and methoxylation and hydrolyzation from 5H-dibenz[b, fJazepine-5-carbonyl chloride. Have optimized the response condition of every step, the overall yield is 49.4%.Secondly, regard 10-methoxy-5H-dibenz[b, fjazepine as initial material, adopt two routes to synthesis OCBZ.A route is: 10-methoxy-5H-dibenz[b, fjazepine react with sodium cyanate under the acid medium, and then through hydrolyzation to synthesis OCBZ. And the condensation reacting condition is optimized, find only through is it react condition be changed to be very difficult to receive the objective compound.Another route is : 10-methoxy-5H-dibenz[b, fjazepine as initial material ,react with the safe solid phosgene which substitute extremely poisonous gas phosgene ,then through ammoniation and hydrolyzation to synthesis OCBZ, has optimized the reacting condition of every step .count with 10-methoxy-5H-dibenz[b, fjazepine, the overall yield is 52.2%;count with 5H-dibenz[b, fJazepine-5-carbonyl chloride, the overall yield is 25.8%. The synthesis process of OCBZ was simpler than that of documents reported ,and the react condition is moderate, material is easier ,yield is higher.