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多巴胺D3受体选择性激动剂PD128907的合成
Synthesis of trans-racemic PD128907 as a dopamine D3 receptor selective agonist
【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。
【Abstract】 AIM To synthesis trans-racemic PD128907 as a dobamine D3 receptor selective agonist.METHODS Starting from p-hydroxyanisole,trans-racemic PD128907 was prepared by addition,hydrolysis,cyclization,oximation,esterification,Neber arrangement,amidation,reduction,cyclization,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.
【Key words】 Medicinal chemistry; Chemical synthesis; PD128907;
- 【文献出处】 江苏药学与临床研究 ,Jiangsu Pharmaceutical and Clinical Research , 编辑部邮箱 ,2006年01期
- 【分类号】TQ467
- 【被引频次】3
- 【下载频次】193