辛二酰苯胺异羟肟酸(Suberoylanilide Hydroxamic Acid,SAHA)是一种以组蛋白乙酰化修饰为作用靶点的新型抗肿瘤药。此文立足药学发展前沿,建立以辛二酸二乙酯为原料,经酯交换反应、苯胺酰胺化反应、羟胺胺解反应的三步合成方法,条件温和,安全性好,并选作本科生的药学综合性实验教学。
Suberoylanilide Hydroxamic Acid(SAHA) is a novel antitumor agent,which can inhibit the enzymatic activity of histone deacetylases.In this paper,based on the frontier development of Pharmacy,SAHA is synthesized from suberic acid diethyl ester by three steps of transesterification,amidation with aniline and aminolysis in hydroxylamine.With mild conditions and good security,this method has been used in teaching of undergraduate comprehensive pharmaceutical experiment.