一鍋合成嘧啶胺類(lèi)化合物

材料科學(xué)論文編號(hào):CL050  論文字?jǐn)?shù):11739,頁(yè)數(shù):22
目  錄
中文摘要 I
英文摘要 II
目錄 III
1. 緒論 1
 1.1  前言 1
 1.2  嘧啶芐胺類(lèi)化合物簡(jiǎn)述 2
 1.1.1 概述 2
 1.1.2 基本合成路線 4
2. 實(shí)驗(yàn)部分 5
 2.1  驗(yàn)儀器與藥品 5
 2.2  原料及合成 5
     2.2.1 一鍋連續(xù)投料法合成 N-（4-溴苯基）-2-（4,6-二甲氧基-2-嘧
           啶氧基）芐胺 5
     2.2.2 合成其他帶不同取代基的嘧啶芐胺類(lèi)化合物 7
3. 結(jié)果與討論 10
 3.1  底物的選擇及溶劑的影響 10
 3.2  還原劑的選擇 11
 3.3  親核取代的條件要求 12
 3.4  催化劑的影響 13
 3.5  關(guān)于嘧啶氧基芐基取代苯基胺類(lèi)衍生物的除草性討論 14
4．總結(jié)與展望 16
致謝 17
參考文獻(xiàn) 18

摘 要：研究了嘧啶芐胺類(lèi)化合物的新合成方法。該法采用了以胺類(lèi)化合物及鄰羥基苯甲醛作為初始原料，通過(guò)一鍋連續(xù)反應(yīng)合成嘧啶芐胺類(lèi)化合物。室溫下將鄰羥基苯甲醛同苯胺類(lèi)化合物進(jìn)行混合反應(yīng)，能迅速生成芐胺類(lèi)化合物。使用硼氫化鈉為還原劑，還原芐胺類(lèi)化合物。再加入碳酸鉀與2-氨基-4,6-二甲氧基嘧啶，加熱回流7小時(shí)后即可合成取代基不同的嘧啶芐胺化合物。此路線總收率較高, 操作簡(jiǎn)便。最終用1H NMR、LS-MS等對(duì)其結(jié)構(gòu)進(jìn)行表征。該類(lèi)化合物是一具有高效生物活性的冬油菜子萌后除草劑。

關(guān)鍵詞：一鍋連續(xù)反應(yīng)；嘧啶芐胺；生物活性；除草劑；

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