3-(4-甲氧基苯基)-4-甲基-5-异噻唑胺的合成及表征  

Synthesis and Characterization of 3-(4-Methoxyphenyl)-4-methyl-5-isothiazolamine

作　　者：冯柏成[1] 郭超[1] 

机构地区：[1]青岛科技大学化工学院,山东青岛266042

出　　处：《青岛科技大学学报（自然科学版）》2018年第1期18-21,共4页Journal of Qingdao University of Science and Technology:Natural Science Edition

基　　金：山东省自然科学基金项目(ZR2015BL025)

摘　　要：以对甲氧基苯甲醛为起始原料,经过肟化-脱水、交叉偶联、亲核加成和氧化闭环4步反应合成了目标产物3-(4-甲氧基苯基)-4-甲基-5-异噻唑胺,并且总收率可达47.15%。通过工艺条件优化,得到了盐酸羟胺和硫代乙酰胺的最佳用量。目标化合物的结构通过GC-MS和~1H NMR进行了鉴定。实验结果表明:该反应条件温和,产品收率高,后处理简单,三废较少,具有良好的工业应用前景。Utilize p-methoxybenzaldehyde as a starting material,after oximation-dehydration,cross-coupling,nucleophilic addition and oxidation closed-loop four-step reactions synthesized target product 3-（4-methoxy-phenyl）-4-methyl-5-isothiazoleamine,and the total yield is up to 47.15%.By optimizing the process conditions obtained the optimum dosage of hydroxylamine hydrochloride and thioacetamide.The structure of the target product was confirmed by GC-MS and ^1H NMR.The experimental results show that the reaction condition is mild,product yield is high,simple workup,less three wastes,and with good prospects for industrial applications.

关 键 词：对甲氧基苯甲醛 苯甲腈 异噻唑 mGluR1拮抗剂 

分 类 号：O626.29[理学—有机化学]