3-氨基-6-三氟甲基喹啉的合成  

Synthesis of 3-Amino-6-trifluoromethyl Quinoline

作　　者：赵丽芳 卢润轩 张玲 徐卫良 徐炜政 ZHAO Li-fang;LU Run-xuan;ZHANG Ling;XU Wei-liang;XU Wei-zheng(School of Pharmaceutical Science,Xuzhou Medical University,Xuzhou 221004,China;Suzhou Kangrun Pharmaceuticals Inc.,Suzhou 215000,China)

机构地区：[1]徐州医科大学药学院,江苏徐州221004 [2]苏州康润医药有限公司,江苏苏州215000

出　　处：《精细化工中间体》2022年第4期44-48,共5页Fine Chemical Intermediates

摘　　要：3-氨基-6-三氟甲基喹啉是具有潜在药用价值的医药中间体,以此为基础可以合成一系列具有广泛生物活性的候选药物分子。以2-溴-4-三氟甲基苯胺为原料,经过Skraup缩合、加氢脱溴、溴化反应、钯催化偶联和氨基脱保护等5步反应得到3-氨基-6-三氟甲基喹啉,总收率34.8%。其结构经^(1)H NMR、^(13)C NMR和LC-MS确证。该合成工艺操作简单,适合工业化生产。3-Amino-6-trifluoromethyl quinoline is a key pharmaceutical intermediate,and its derivatives could become drug candidates with a wide range of biological activities and potential medicinal values.3-Amino-6-trifluoromethyl quinoline was synthesized through 5 steps reactions including the Skraup condensation,debromination by hydrogenation,bromine substitution,palladium-catalyzed coupling and amino deprotection using 2-bromo-4-(trifluoromethyl)aniline as starting material in a total yield of 34.8%.The structure of the final product was confirmed by^(1)H NMR,^(13)C NMR and LC-MS.This multi-step synthetic process is relatively simple and suitable for industrial production.

关 键 词：3-氨基-6-三氟甲基喹啉 中间体 合成 

分 类 号：O626.323[理学—有机化学] TQ460.1[理学—化学]