| 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 |
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| 引用本文： | 蔡进,李铭东,张姣月,周文,华维一,吉民.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[J].中国新药杂志,2006,15(12):987-989. |
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| 作者姓名： | 蔡进 李铭东 张姣月 周文 华维一 吉民 |
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| 作者单位： | 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 |
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| 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-苯并吡喃-4-酮.结果：以总收率43.4%合成了多巴胺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：该法原料价廉易得,反应条件温和,收率较高.
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| 关 键 词： | 多巴胺D3受体选择性激动剂 化学合成 |
| 文章编号： | 1003-3734（2006）12-0987-03 |
| 收稿时间： | 2005-11-03 |
| 修稿时间： | 2005年11月3日 |
Synthesis of 3-amino-6-methoxy-3,4-dihydro-2H-[ 1 ] benzopyran -4-one hydrochloride, an important intermediate of PD128907 |
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| CAI Jin,LI Ming-dong,ZHANG Jiao-yue,ZHOU Wen,HUA Wei-yi,JI Min.Synthesis of 3-amino-6-methoxy-3,4-dihydro-2H-[ 1 ] benzopyran -4-one hydrochloride, an important intermediate of PD128907[J].Chinese Journal of New Drugs,2006,15(12):987-989. |
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| Authors: | CAI Jin LI Ming-dong ZHANG Jiao-yue ZHOU Wen HUA Wei-yi JI Min |
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| Institution: | 1 Center of Drug Discovery, China Pharmaceutical University, Nanjing 210009, China; 2 Institute of Pharmaceutical Engineering, Southeast University, Nanjing 210096, China |
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| 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. |
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| Keywords: | PD128907 |
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