抗癌药物泰克地那林的合成工艺优化

摘要

Aim:Applying p-aminobenzoic acid as starting material, Tacedinaline has been synthe-sized via acetylation of amino group; activation of carboxylic group followed the reaction with o-phenyl di-amine immediately. The overall yield for this three-step process reached 47. 5%. The structures of all products were confirmed by NMR and ESI-MS. Furthermore, the purification process of Tacedinaline was optimized and became more green and environmental protective.%以对氨基苯甲酸为起始原料,经氨基乙酰化、羧基活化后与邻苯二胺反应合成泰克地那林,三步反应的总收率为47.5％,并用质谱和核磁共振谱对所合成化合物进行结构确证.另外,优化了泰克地那林的纯化工艺,使得更加绿色环保.