PD128907中间体3-氨基-6-甲氧基-3,4-二氢-2H-苯并吡喃-4-酮盐酸盐的合成  

Synthesis of 3-amino-6-methoxy-3,4-dihydro-2H-[1]benzopyran-4-one hydrochloride,an important intermediate of PD128907

作　　者：蔡进[1] 李铭东[2] 张姣月[2] 周文[1] 华维一[1] 吉民[2] 

机构地区：[1]中国药科大学新药研究中心,南京210009 [2]东南大学制药工程研究所,南京210096

出　　处：《中国新药杂志》2006年第12期987-989,共3页Chinese Journal of New Drugs

基　　金：国家自然科学基金(30472011)

摘　　要：目的:合成多巴胺D_3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D_3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。Objective：To synthesize 3-amino-6-methoxy-3,4-dihydro-2H-[1] benzopyran4-onehydrochloride, 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 reaction. Results： The total yield was 43.4%. The structure has been confirmed byI HNMR,MS and IR. Con- clusion ： The procedure has several advantages of cheap reagents, facile reaction conditions and high yield.

关 键 词：多巴胺D3受体选择性激动剂 化学合成 PD128907 

分 类 号：R914[医药卫生—药物化学] R971[医药卫生—药学]