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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

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【Author】 CAI Jin~1,LI Ming-dong,ZHOU Wen~1,ZHANG Jiao-yue~2,HUA Wei-yi~1,JI Min~2()~1Center of Drug Discovery,China Pharmaceutical University(Nanjing 210009);()~2Institute of Pharmaceutical Engineering,Southeast University(Nanjing 210096,China)

【机构】中国药科大学新药研究中心；东南大学制药工程研究所；东南大学制药工程研究所南京210009；南京210096；南京210009；

【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。更多还原

【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.更多还原