摘要
目的合成多巴胺D3受体选择性激动剂PD128907。方法以对甲氧基苯酚为起始原料,经加成、酸解、环合、成肟、酯化、Neber重排、酰胺化、还原、环合、还原、烷基化以及脱甲基等12步反应制备了PD128907反式消旋体。结果以总收率4.75%合成了多巴胺D3受体选择性激动剂PD128907反式消旋体,结构经核磁氢谱(1H NMR)、质谱(MS)和红外光谱(IR)确证。结论对PD128907的合成进行了探讨,该法原料价廉易得,反应条件温和,收率较高。
AIM To synthesis trans-racemic PD128907 as a dobamine D3 receptor selective agonist. METHODS Starting from phydroxyanisole, trans-raeemic PD128907 was prepared by addition, hydrolysis, cyclization, oxSmation, estedfication, Neber arrangement, amidafion,reducfion,cyclizafion,reduction alkylation and demethylation reaction. RESULTS The total yield was 4.75%. The structure has been confirmed by ^1H NMR,MS and IR. CONCLUSIO The procedure has several advantages of cheap reagents,facile reaction conditions and high yield.
出处
《江苏药学与临床研究》
2006年第1期21-24,共4页
Jiangsu Pharmacertical and Clinical Research
基金
国家自然科学基金资助项目(项目批号:30472011)
