Facile and efficient synthesis of quinazoline-2,4(1H,3H)-diones through sequential hydrogenation condensation

被引:4
|
作者
Wang, Peng-Xu [1 ,2 ,3 ]
Wang, Ya-Nan [1 ,2 ]
Lin, Zi-Yun [1 ,2 ,3 ]
Li, Gang [1 ,2 ,3 ]
Huang, Hai-Hong [1 ,2 ,3 ]
机构
[1] Peking Union Med Coll, Inst Mat Med, State Key Lab Bioact Subst & Funct Nat Med, Beijing, Peoples R China
[2] Chinese Acad Med Sci, Beijing 100050, Peoples R China
[3] Peking Union Med Coll, Inst Mat Med, Beijing Key Lab Act Subst Discovery & Druggabil E, Beijing, Peoples R China
基金
中国国家自然科学基金;
关键词
Cascade reaction; heterocyclization; hydrogenation condensation; quinazoline-2,4(1H,3H)-dione; QUINAZOLINE; DERIVATIVES; ANTAGONISTS; INHIBITORS; SCAFFOLDS; RECEPTOR; DESIGN; POTENT;
D O I
10.1080/00397911.2018.1439173
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
The heterocyclizations from various methyl (2-nitrobenzoyl)carbamates to substituted quinazoline-2,4(1H,3H)-diones under hydrogenation conditions were investigated in this study. In the presence of p-toluenesulfonic acid monohydrate in methanol, various quinazoline-2,4(1H, 3H)-diones were obtained in good to excellent yields within 12h. The reaction was proposed to proceed through the cascade reactions of nitro reduction and condensation. [GRAPHICS] .
引用
收藏
页码:1183 / 1189
页数:7
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