他克林的合成研究

Synthesis of Tacrine

目的 :合成抗早老性痴呆药他克林。方法 :以邻氨基苯甲酸为原料 ,经缩合、氯化、氨化反应 ,制得他克林。结果 :每步反应均经改进 ,总收率达 40 .7%。所得产品熔点、IR、1HNMR光谱数据 ,与文献报道值一致。结论 :本工艺路线方法简单 ,原料易得 ,易工业化生产。

OBJECTIVE:To synthesize Tacrine,a new drug for the treatment of Alzheimer′s disease.METHOD:With the 2 aminobenzoic acid as the starting material,Tacring was synthesized via condensation cyclization,chlorization and amination.RESULTS:Each step was modified and improved.The overall yields was 40.7%.The melting point and IR、 1HNMR of the product prepared were identical as that of the reportedone.CONCLUSION:The process can be easily controled and is suitable for a scale production.