摘要
以1-(2-甲基丙基)-4-氯-1H-咪唑并[4,5-c]喹啉(Ⅰ)为原料与哌啶反应合成了1-(2-甲基丙基)-4-[哌啶-1-基]-1H-咪唑并[4,5-c]喹啉(Ⅱ),当用甲苯为溶剂,n(Ⅰ)∶n(哌啶)∶n(K2CO3)=1∶2∶0.3时,Ⅱ的收率为88.5%;Ⅰ与三倍过量的吗啉反应合成1-(2-甲基丙基)-4-[吗啉-4-基]-1H-咪唑并[4,5-c]喹啉(Ⅲ),收率86.5%;Ⅰ与三倍过量的哌嗪在体积分数50%的1,4-二氧六环水溶液中反应合成1-(2-甲基丙基)-4-[哌嗪-1-基]-1H-咪唑并[4,5-c]喹啉(Ⅳ),收率59%。Ⅱ、Ⅲ、Ⅳ的合成工艺均较简单。
1-( 2-Methylpropyl ) -4-( piperidin-l-yl ) -1H- imidazo [ 4, 5-c ] quinoline ( 11 ) was synthesized by the reaction of 1 -(2-methylpropyl) -4-chloro -1H- imidazo [ 4,5-c ] quinoline ( I ) with piperidine,when toluene was used as solvent and the molar ratio of Ⅰ ,piperidine and K2CO3 was 1:2: 0.3. The yield was 88.5%. 1-( 2-Methylpropyl ) -4-( morpholin-4-yl ) -1H-imidazo [ 4,5-c ] quinoline ( Ⅲ) was synthesized in 86.5% yield by the reaction of I with three fold excess of morpholine. 1-(2- Methylpropyl) -4-(piperazin-l-yl) -1 H- imidazo [ 4,5-c ] quinoline ( Ⅳ ) was obtained in 59% yield by the reaction of Ⅰwith three fold excess of piperazine using 50% water solution of 1,4-dioxane as solvent.
出处
《精细化工》
EI
CAS
CSCD
北大核心
2007年第3期304-307,共4页
Fine Chemicals
基金
广东省重点科技攻关项目(2003C104043)