普拉克索重要中间体合成路线改进研究

The Improved Synthetic Route for the Intermediate of Pramipexole

普拉克索是一种帕金森病症的新型治疗药物,对其研究具有重要意义。文章通过前人对普拉克索合成的研究进行探讨,并且由此寻找到一条新的普拉克索中间体合成路线。本实验以反式对氨基环己醇为原料,经丙酰化保护氨基,Jones试剂氧化和溴化,再与硫脲进行Hantzsch反应,最后还原得到普拉克索中间体(R,S)-2-氨基-6-丙酰胺基-4,5,6,7-四氢苯并噻唑。通过最后中间体的1H-NMR谱图等可以确定其结构与目标相符,验证了该路线的可行性。

Pramipexole is a new treatment of Parkinson＇s disease, the study for its synthesis has important significance. In the paper, on the base of previous studies of synthesis of Pramipexole, we managed to find a new synthetic route to intermediates of pramipexole, which was efficient and convenient. In the experiment, we took trans-amino cyclohexanol as starting materials, through the five-step reaction, such as propylation, Jones oxidization, bromination, hantzsch reaction and reduction, finally we got well-quality intermediates of pramipexole in overall yield 10.90 %. We adopted 1H-NMR to determine the structure of the intermediate. That was in line with the target to verify the feasibility of the route.