Both 1,5-benzodiazepine and quinoxaline derivatives are important heterocycles in pharmaceuticals. We describe an efficient and clean method for the synthesis of 1,5-benzodiazepines from o-phenylenediamine and ketones...Both 1,5-benzodiazepine and quinoxaline derivatives are important heterocycles in pharmaceuticals. We describe an efficient and clean method for the synthesis of 1,5-benzodiazepines from o-phenylenediamine and ketones catalyzed by sodium tetrachloroaurate(Ⅲ) dihydrate under mild conditions. The catalyst was shown to be equally effective for the synthesis of quinoxalines from o-phenylenediamine and α-bromo ketones under the similar reaction conditions. This method produced good yields.展开更多
基金Project supported by the Natural Science Foundation of Zhejiang Province (No. Y407168)the Foundation of Education of Zhejiang Province (No. Z200803599)the Opening Foundation of Zhejiang Provincial Top Key Discipline (No. 56310101634), China
文摘Both 1,5-benzodiazepine and quinoxaline derivatives are important heterocycles in pharmaceuticals. We describe an efficient and clean method for the synthesis of 1,5-benzodiazepines from o-phenylenediamine and ketones catalyzed by sodium tetrachloroaurate(Ⅲ) dihydrate under mild conditions. The catalyst was shown to be equally effective for the synthesis of quinoxalines from o-phenylenediamine and α-bromo ketones under the similar reaction conditions. This method produced good yields.