I2-catalyzed Oxidative Coupling Reactions of Hydrazones and Amines for the Synthesis of 1,3,5-Trisub

来源 :中国化学会第十三届全国有机合成化学学术研讨会 | 被引量 : 0次 | 上传用户:jhyyxz
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  1,2,4-Triazoles,as highly privileged heterocyclic scaffolds,have found extensive applications in biological and pharmaceutical fields as well as materials science.Several potent biological activities,such as antihypertensive,antifungal and antibacterial activities,have aroused considerable attention among medicinal chemists.Therefore,the development of one-pot regioselective approach for the efficient construction of 1,2,4-triazole structure is highly desirable.We have disclosed a general and expeditious approach for the metal-free mediated synthesis of 1,3,5-trisubstituted 1,2,4-triazoles from hydrazones and aliphatic amines under aerobic oxidative conditions.The methodology features readily accessible starting reagents,general and convenient operating conditions,broad substrate scope and high efficiency,and can be easily scaled up to gram scale.The reaction proceeds through cascade C-H functionalization,double C-N bonds formation and oxidative aromatization sequence.
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