室温下氨基磺酸催化合成喹噁啉衍生物  

Synthesis of Quinoxaline Derivatives Catalyzed by Sulfamic Acid at Room Temperature

作　　者：李维思[1] 孙颖杰[1] 任星华[1] 李振江[1] 石玉瑚[1] 欧阳平凯[1] 

机构地区：[1]南京工业大学制药与生命科学学院,江苏南京210009

出　　处：《精细化工》2007年第6期577-580,共4页Fine Chemicals

基　　金：国家973计划资助项目(2003CB716004)~~

摘　　要：用廉价、无毒、易得的氨基磺酸作为催化剂,以二氯甲烷为溶剂,用芳香、杂环及脂肪1,2-二酮分别与1,2-二胺在室温下进行缩合反应得到喹噁啉衍生物。考察了溶剂、催化剂用量、反应时间对产物收率的影响,优化的工艺条件为:n(二酮)∶n(二胺)∶n(氨基磺酸)=1∶1∶0.15,反应温度25℃,反应时间6 h,产物最终收率均超过75%。该反应放大200倍后,即在1 L溶剂中,用1 mol的反应物反应时,在优化的工艺条件下产率仍然可以达到70%。氨基磺酸可以循环使用5次而产率保持稳定。Several aromatic, heteroaromatic as well as aliphatic 1,2-diketones were subjected to condensation with various aromatic 1,2-diamines using the inexpensive, nontoxic and readily available sulfamic acid as catalyst in dichloromethane to afford quinoxaline derivatives. The optimal reaction conditions were n （diketone） ： n （ diamine ） ： n （ sulfamic acid ） = 1 ： 1：0. 15, reaction time 6 h and reaction temperature 25 ℃. The product yield exceeded 75%. When the reaction was magnified 200 times with 1 mol reactants in 1 L solvent under the optimal conditions,the yield still reached 70%. Sulfamic acid can be used five times with recycle without any loss in yield.

关 键 词：氨基磺酸 1 2-二酮 1 2-二胺 喹噁啉 缩合 

分 类 号：TQ247.56[化学工程—有机化工] TQ253.23