文章摘要
林艳,万屏南,肖文杰,马广强,曹海泳,崔汉峰,樊浩.1-氯甲基磺酰胺类化合物的合成[J].精细化工,2019,36(6):
1-氯甲基磺酰胺类化合物的合成
Synthesis of the 1-Chloromethyl Sulfonamide Compounds
投稿时间:2018-11-14  修订日期:2019-02-20
DOI:
中文关键词: 磺酰化反应  氯甲基磺酰氯  芳香伯胺  精细化工中间体
英文关键词: sulfonylation  chloromethanesulfonyl chloride  aromatic primary amine  fine chemical intermediates
基金项目:
作者单位E-mail
林艳 江西中医药大学 linyan9945@sina.com 
万屏南 江西中医药大学  
肖文杰 江西中医药大学  
马广强 江西中医药大学  
曹海泳 江西中医药大学  
崔汉峰 江西中医药大学 cuihanfeng@126.com 
樊浩 江西中医药大学  
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中文摘要:
      磺酰胺类化合物具有广泛的生物活性。以吡啶为催化剂,实现了氯甲基磺酰氯和芳香伯胺的磺酰化反应。考察了催化剂、溶剂、物料比、反应温度等条件对反应产率的影响。结果表明,最优反应条件为:n(胺):n(磺酰氯) = 1:1.3,吡啶为催化剂,二氯甲烷为溶剂,先0℃再室温下反应,反应时间为4~8 h。在最优条件下,以42%~95%的产率合成了9种具有不同取代基的磺酰胺类化合物。利用IR、1HNMR、13CNMR对目标产物的结构进行了确征。
英文摘要:
      Sulfonamide is a special type of compound known for its versatile biological activity. The synthesis of these compounds has attracted manyattention of pharmaceutical chemists and organic chemists. Sulfonylation was accomplished between chloromethanesulfonyl chloride and aromatic primary amine in the presence of pyridine in this article. The reaction conditions such as catalyst, solvent, molar ratio of the material and reaction temperature were investigated.The results indicated that the optimized reaction conditions were determined as follows: n (amine) : n (chloromethanesulfonyl chloride) = 1 :1.3, pyridine as catalyst, dichloromethane as solvent , reaction at 0 ℃ to room temperature for 4~8 h. Under the optimized reaction conditions, a series of chloromethyl sulfonamide was obtained in 42%~95% yields. The structure of newly synthesized compounds was determined by IR, 1HNMR and 13CNMR.
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