摘要
1,3-环己二酮(2)经溴代、与硫脲环合、酮的-溴代及叠氮取代制得2-氨基-6-叠氮-7-氧代-4,5,6,7-四氢苯并噻唑(6),6依次经硼氢化钠和锌粉还原后经正丙醛/三乙酰氧基硼氢化钠还原氨化,最后由氯铬酸吡啶鎓盐(PCC)氧化得到盐酸普拉克索质量研究的杂质对照物消旋-7-氧代普拉克索,总收率为11.7%。
Rac-7-oxopramipexole, an impurity reference during the quality study of pramipexole, was synthesized from 1,3-cyclohexanedione by bromination with bromine, cyclization with thiourea, bromination and substitution with sodium azidc to give 2-amino-6-azido-7-oxo-4,5,6,7-tetrahydrobenzothiazole （6）, which was subjected to successive reduction with sodium borohydride and zinc powder, reductive amination with n-propanal and sodium triacetoxyborohydride, followed by oxidation with PCC with an overall yield of about 11.7 %.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2013年第6期551-553,共3页
Chinese Journal of Pharmaceuticals
