以脱氢枞胺和苯甲酰氯为原料,合成了N-苯甲酰基-脱氢枞胺。通过B环氧化,得到N-苯甲酰基-脱氢枞胺-7-酮,用IR、MS和1HNMR光谱确证其结构。对N-苯甲酰基-脱氢枞胺-7-酮进行了雄激素受体(AR)结合活力测试。结果表明,N-苯甲酰基-脱氢枞胺-7-酮与AR具有一定的结合活性,半数抑制浓度(IC50)为83.8nmol/L。
N-benzoyl-dehydroabietylamine was synthesized from dehydroabietylamine and benzoyl chloride. Then N-benzoyldehydroabietylamine-7-one was synthesized from the former by oxidizing at ring-B. Their structures were characterized by IR, MS and 1H NMR spectroscopies. The androgen receptor(AR) binding activities of N-benzoyl-dehydroabietylamine-7-one was tested. It has been found that N-benzoyl-dehydroabietylamine-7-one presents certain androgen receptor binding activity with IC50 value of 83.8 nmol/L.