【摘要】 目的:合成多巴胺D₃受体选择性激动剂PD128907中间体3-氨基-6-甲氧基-3,4-二氢-2H-苯并吡喃- 4-酮盐酸盐。方法:以对甲氧基苯酚为起始原料,经加成、酸解、环合、成肟、酯化和Neber重排6步反应制备了3-氨基-6-甲氧基-3,4-二氢-2H-苯并毗喃-4-酮。结果:以总收率43．4%分成了多巴胺D₃受体选择性激动剂PD128907中间体,结构经核磁氢谱、质谱和红外光谱确证。结论:该法原料阶廉易得,反应条件温和,收率较高。更多还原

【Abstract】 Objective :To synthesize 3-amino-6-methoxy-3,4-dihydro-2H-[1]benzopyran-4-one hydrochloride,an important intermediate of dopamine D3 receptor selective agonist PD128907.Methods: Starting from p-hydroxyanisole,3-amino-6-methoxy-3,4-dihydro-2H-[1]benzopyran-4-one hydrochloride was preparated by addition,hydrolysis,cyclization,oximation,esterification and Neber arrangement reac- tion.Results:The total yield was 43.4%.The structure has been confirmed by ~1HNMR,MS and IR.Con- clusion:The procedure has several advantages of cheap reagents,facile reaction conditions and high yield.更多还原