(±)-瑞枯灵的合成 |
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引用本文: | 张建革,闻韧.(±)-瑞枯灵的合成[J].中国医药工业杂志,2005,36(1):3-6. |
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作者姓名: | 张建革 闻韧 |
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作者单位: | 复旦大学药学院药物化学教研室,上海,200032 |
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摘 要: | 4-羟基-3-甲氧基苯乙胺和3-羟基-4-甲氧基苯乙酸经缩合、O-苄基保护得到2-(3-苄氧基-4-甲氧基苯基)-N-2-(4-苄氧基-3-甲氧基苯基)乙基]乙酰胺,在POCl3作用下进行Bischler-Napieralski环合反应后,不经分离纯化直接与氯甲酸甲酯进行N-酰化得到7-苄氧基-1-(3-苄氧基-4-甲氧基苯亚甲基)-6-甲氧基-3,4-二氢-1H-异喹啉-2-羧酸甲酯,再经Pd-C氢化脱苄基和用四氢铝锂还原得到(±)-瑞枯灵,总收率23%.
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关 键 词: | 瑞枯灵 生物碱 合成 |
文章编号: | 1001-8255(2005)01-0003-04 |
修稿时间: | 2004年4月2日 |
Synthesis of (±)-Reticuline |
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Authors: | ZHANG Jian-Ge WEN Ren |
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Affiliation: | ZHANG Jian-Ge1,WEN Ren1* |
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Abstract: | Reticuline was synthesized from 4-hydroxy-3-methoxyphenylethylamine and 3-hydroxy- 4-methoxyphenylacetic acid by condensation and O-benzylation to give 2-(3-benzyloxy-4-methoxyphenyl)-N-2-(4- benzyloxy-3-methoxyphenyl)ethyl]acetamide, which subjected to Bischler-Napieralski reaction with POCl3, N-acylation with methyl chloroformate to give 7-benzyloxy-1-(3-benzyloxy-4-methoxybenzylidene)-6-methoxy-3,4-dihydro-1H- isoquinoline-2-carboxylicacid methyl ester followed by deprotection and reduction with an overall yield of 23%. |
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Keywords: | reticuline alkaloid synthesis |
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