抗肿瘤药泰克地那林的合成工艺改进

Improved synthesis of tacedinaline,a new antitumour drug

以 4 乙酰氨基苯甲酸 (2 )为原料 ,与草酰氯反应 ,不经分离 ,直接与 2 硝基苯胺反应得到中间体N (2 硝基苯基 ) 4 乙酰氨基苯甲酰胺 (4 ) ,再经催化氢化得到泰克地那林。以 4 乙酰氨基苯甲酸计 ,总收率为 2 2 2 % ,目标化合物的结构经质谱、红外光谱及核磁共振氢谱确证 ,该合成工艺简单易行。

Tacedinaline was synthesized from 4-(acetamido)benzoic acid by the reaction with oxalyl chloride to form 4-(acetamido)benzoyl chloride which was condensed with 2-nitroaniline,followed by reduction with H 2 over Pd/C.The overall yield of the improved procedure was 22.2%.The structure of tacedinaline was confirmed by IR,MS and 1H-NMR,and the process is simpler and more practical.