一锅合成嘧啶胺类化合物

文档编号:CL050  文档字数:11739,页数:22

摘 要：研究了嘧啶苄胺类化合物的新合成方法。该法采用了以胺类化合物及邻羟基苯甲醛作为初始原料，通过一锅连续反应合成嘧啶苄胺类化合物。室温下将邻羟基苯甲醛同苯胺类化合物进行混合反应，能迅速生成苄胺类化合物。使用硼氢化钠为还原剂，还原苄胺类化合物。再加入碳酸钾与2-氨基-4,6-二甲氧基嘧啶，加热回流7小时后即可合成取代基不同的嘧啶苄胺化合物。此路线总收率较高, 操作简便。最终用1H NMR、LS-MS等对其结构进行表征。该类化合物是一具有高效生物活性的冬油菜子萌后除草剂。

关键词：一锅连续反应；嘧啶苄胺；生物活性；除草剂；

Abstract: A new synthetic method of pyridine-benzylamine was described. A series of pyridine-benzylamines derivatives were synthesized by using amines and salicylaldehyde as the starting material， to produce the pyridine-benzylamines via a one-pot sequential process. The reaction of salicylaldehyde  with amines stirring under room temperature will generate the benzyl amines. The reduction of  benzyl amines was carried out by using soldium borohydride as reducing agent. After that, potassium carbonate and 2-Amino-4,6-dimethoxypyrimidine were added and heated to refluxing. After the mixture had been stirred for 7h with refluxing，the filtrate was evaporated to give the pyridine-benzylamine. The advantages of  this method are high yield and simple work-up. Finally the structures of the compounds were determined by 1H NMR and LC-MS. The compounds were high efficiency postemergent herbicides for winter oilseed rape.

Keywords：one-pot synthesis; pyridine-benzylamine；biological activity；herbicide 

目  录
中文摘要 I
英文摘要 II
目录 III
1. 绪论 1
 1.1  前言 1
 1.2  嘧啶苄胺类化合物简述 2
 1.1.1 概述 2
 1.1.2 基本合成路线 4
2. 实验部分 5
 2.1  验仪器与药品 5
 2.2  原料及合成 5
     2.2.1 一锅连续投料法合成 N-（4-溴苯基）-2-（4,6-二甲氧基-2-嘧
           啶氧基）苄胺 5
     2.2.2 合成其他带不同取代基的嘧啶苄胺类化合物 7
3. 结果与讨论 10
 3.1  底物的选择及溶剂的影响 10
 3.2  还原剂的选择 11
 3.3  亲核取代的条件要求 12
 3.4  催化剂的影响 13
 3.5  关于嘧啶氧基苄基取代苯基胺类衍生物的除草性讨论 14
4．总结与展望 16
致谢 17
参考文献 18

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