摘要
Aim To synthesize dutasteride. Methods The target compound was synthesized from pregnenolol via eight steps, including esterification, oxidation, hydrolysis, then oxidative ring-opening, cyclization, reduction, oxidization and finally acylation. Results The structure of the target molecule was identified by ^1H NMR, ^13C NMR and element analysis. The overall yield was 31.5%. Conclusion The effects of different reaction conditions on the yield of product in each step have been investigated and the optimal reaction conditions have been established.
目的制备度他雄胺。方法孕烯酮醇经过酯化、氧化(沃氏反应)、水解得孕烯酮酸,再经过氧化开环、环合、还原、氧化、酰基化共八步制得目标产物。结果最终产物由核磁共振谱和元素分析进行结构鉴定。总收率为31.5%。结论探索了不同条件对各个合成中间体的产率的影响,找出合适的反应条件,使之更适于工业生产。
