Development of a practical synthesis of sumanirole

被引:17
作者
Wuts, PGM [1 ]
Gu, RL
Northuis, JM
Kwan, TA
Beck, DM
White, MJ
机构
[1] Pharmacia, Chem Proc Res & Dev, Kalamazoo, MI 49001 USA
[2] Pharmacia, Bioproc & Formulat Technol, Kalamazoo, MI 49001 USA
关键词
D O I
10.1351/pac200274081359
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
A new synthesis of sumanirole that is being developed to treat Parkinson's disease is described. The basic skeleton is constructed from 8-hydroxyquinoline and elaborated to the key tricylic intermediate 14. Further elaboration affords a 1,2-amino alcohol, which is converted to an aziridine by a new process. Finally, dissolving metal reduction to open the aziridine and protecting group removal affords sumanirole.
引用
收藏
页码:1359 / 1368
页数:10
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