吡咯酰胺催化合成吡唑啉酮衍生物  

Synthesis of Pyrazolone Derivatives Catalyzed by Pyrrole Amide

作　　者：王文琛[1] 杨志翔[1] 王金娟[1] 黄克俊 陈治明[1] WANG Wen-chen;YANG Zhi-xiang;WANG Jin-juan;HUANG Ke-jun;CHEN Zhi-ming(Key Laboratory of Functional Materials Chemistry of Guizliou Province,School of Chemistry and Materials Science,Guizhou Normal University,Guiyang 550001,China)

机构地区：[1]贵州师范大学化学与材料科学学院贵州省功能材料重点实验室,贵州贵阳550001

出　　处：《合成化学》2018年第5期337-342,共6页Chinese Journal of Synthetic Chemistry

基　　金：国家自然科学基金资助项目(21362006)

摘　　要：探究了绿色高效合成医药价值较高的吡唑啉酮衍生物的方法,即:以吡咯酰胺催化吡唑啉酮与硝基烯进行Michael反应,高收率地合成了系列吡唑啉酮衍生物,其结构经~1H NMR和^(13)C NMR确证。并考察了催化剂及其用量、溶剂和温度对反应的影响。结果表明;在室温下,CH_2Cl_2体系中,在10 mmol%催化剂E存在下,吡唑啉酮与硝基烯烃能有效进行Michael反应,收率80%~91%。A green and highly efficient method for synthesizing pyrazolone derivatives with higher medicinal value was explored. A series of pyrazolone derivatives were synthesized by reaction of pyrazolone with nitroolefins catalyzed by the pyrroliamide catalysts. The structures were confirmed by 1H NMR and 13C NMR. The effects of catalyst and its amount,solvent and temperature on the reaction were investigated. The results showed that the reaction was effcciently performed in the presence of catalyst E（10 mmol%） at room temperature in CH2Cl2 with the yields of 80% 91%.

关 键 词：吡唑啉酮 吡唑啉酮衍生物 硝基烯烃 MICHAEL反应 合成 

分 类 号：O626[理学—有机化学]