氢溴酸苯甲托品的合成工艺改进

Improved synthesis of benzatropine hydrobromide

目的合成抗胆碱药氢溴酸苯甲托品。方法将二苯甲醇和对甲苯磺酰氯先进行缩合,再加入托品醇采用"一锅法"制得苯甲托品,最终与氢溴酸成盐,制得氢溴酸苯甲托品。结果与结论目标化合物的结构经~1H-NMR、MS谱确定,总收率达63.10%(以二苯甲醇计),HPLC检测纯度为99.7%。该工艺路线简化了操作,提高了收率,具有潜在的工业化应用前景。

Benzatropine hydrobromide is an anticholinergic drug, developed by Merck Corporation, which was launched in 1953 for the treatment of Parkinson＇s disease. The synthesis of benzatropine hydrobromide was improved in this paper. It was synthesized from diphenylmethanol via esterification, nucleophilic substitution,and salification with an overall yield of 63.10% （based on diphenylmethanol）. The purity was 99. 7 % determined by HPLC. The structure of the target compound was identified by 1H-NMR and ESI-MS. The improved process is facile with relatively convenient operation procedures and suitable for industrial production.