摘要
非那雄胺能抑制5α-还原酶的活性,明显降低二氢睾酮水平,是一种治疗良性前列腺增生的有效药品。该合成工艺以甾烯酮酸为原料,将其与氯化亚砜反应,无须分离即与叔丁胺反应得17β-酰胺化合物,再氧化开环,环合,氢化,脱氢合成了非那雄胺。经元素分析、IR、1HNMR、13CNMR、MS分析表征了其结构。该法无须使用昂贵的2,2-二吡啶二硫化物和剧毒药品苯亚硒酸酐,且以乙酸铵代替氨气,降低了对设备的要求和腐蚀,更适用于工业生产。
Finasteride, which can inhibit the activity of 5α-reductase and obviously reduce the DHT level, is a new efficient drug for treatment of BPH. Finasteride was synthesized from zaixitongsuan （3-carbonyl-4-androstene-17β-carboxylic acid）, which reacted with thionyl chloride and then with t-butylamine in one pot to yield the 17β-carboxamide. Then through oxygenizement for decydization, cycli condensation, hydrogenated and dehydrogenated, the target compound was produced. Then the structure is characterized by element analysis, IR, ^1NMR, ^13CNM-R, MS. The new synthetic route avoids the use of expensive reagent 2,2-dipuridyl disulfide and toxicant （PhgeO）20. The ammonia was replaced with NH4OAc in new technology, which decreased the requirement and erosion for a equipment. It is suitable for plant-scale production.,
出处
《广州化学》
CAS
2006年第2期18-22,共5页
Guangzhou Chemistry
关键词
非那雄胺
5Α-还原酶
合成
工艺改进
finasteride, 5α-reductase, synthesis, improvement of technique
