非那雄胺合成工艺改进

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。

Improvement of Techniques of Synthesis of Finasteride

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,1HNMR,13CNM-R,MS.The new synthetic route avoids the use of expensive reagent 2,2-dipuridyl disulfide and toxicant(PhSeO)2O.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.