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| 5-羟基-6-甲氧基-2-苄基-3,4-二氢异喹啉-1-酮的合成 | |
| 引用本文： | 祝丽永,程彬,张三奇,陈战国. 5-羟基-6-甲氧基-2-苄基-3,4-二氢异喹啉-1-酮的合成[J]. 西北药学杂志, 2008, 23(2): 104-105 |
| 作者姓名： | 祝丽永 程彬 张三奇 陈战国 |
| 作者单位： | 1. 陕西师范大学化学与材料科学学院,陕西,西安,710062 2. 西安交通大学医学院药物研究所,陕西,西安,710061 |
| 摘 要： | 目的研究5-羟基-6-甲氧基-3,4-二氢异喹啉-1-酮衍生物的合成方法。方法以异香草酸甲酯为原料,通过烯丙基醚化、Claisen重排、氧化、西佛碱的制备、还原、分子内酯的胺解6步反应合成了5-羟基-6-甲氧基-2-苄基-3,4-二氢异喹啉-1-酮(1),总收率达55.0%。Schiff碱的制备、还原、酯的胺解3步在"一锅"内完成。结果合成了新的3,4-二氢异喹啉-1-酮衍生物,其结构经IR和1HNMR确认。结论设计的合成路线具有反应条件温和、操作简便、反应总收率高等优点。 |
| 关 键 词： | 二氢异喹啉酮衍生物 Claisen重排 一锅法 |
| 文章编号： | 1004-2407(2008)02-0104-02 |
| 修稿时间： | 2007-12-20 |
Synthesis of 2-benzyl-5-hydroxy-6-methoxy-3,4-dihydroisoquinolin-1(2H)-one |
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| ZHU Liyong,CHENG Bin,ZHANG Sanqi,CHEN Zhanguo. Synthesis of 2-benzyl-5-hydroxy-6-methoxy-3,4-dihydroisoquinolin-1(2H)-one[J]. Northwest Pharmaceutical Journal, 2008, 23(2): 104-105 | |
| Authors: | ZHU Liyong CHENG Bin ZHANG Sanqi CHEN Zhanguo |
| Abstract: | Objective To investigate a new method of synthesis of 2-benzyl-5-hydroxyl-3,4-dihydroisoquinolin-1(2H)-one.Method 2-benzyl-5-hydroxy-6-methoxy-3,4-dihydro-isoquinolin-1(2H)-one(1)was synthesized from methyl 3-hydroxy-4-methoxyben-zoate via allyl etherification,Claisen rearrangement,oxidation,reductive amination and amidation.Reductive amintion and ami-nolysiswere completed in one-pot.Results A new derivative of 3,4-dihydro-isoquinolin-1(2H)-one was synthesized and its structure was identified by IR and 1HNMR.Conclusion The designed synthetic route was mild and simple in operation with higher yield. |
| Keywords: | 3,4-Dihydroisoquinolin-1(2H)-one Claisen rearrangement One-Pot method |
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