Direct Synthesis of Benzo[f]indazoles from Sulfonyl Hydrazines and 1,3-Enynes by Copper-Catalyzed Annulation
作者单位：Department of ChemistryHuaibei Normal University 淮北师范大学
会议名称：《中国化学会·第十六届全国有机合成化学学术研讨会》
会议日期：2019年
学科分类：081704[工学-应用化学] 07[理学] 08[工学] 0817[工学-化学工程与技术] 070303[理学-有机化学] 0703[理学-化学]
关 键 词：cascade cyclization 1,4-arylmigration 1,3-enyne benzo[f]indazole sulfonyl hydrazine
摘 要：Indazole moiety is a privileged N-heterocyclic structure in medicinal chemistry due to its pronounced biological and therapeutic activities,and especially,tricyclic 1 H-benzo-indazole plays increasingly important role in drug discovery. In the past few decades,a number of impressive methods have been reported for the construction of indazole frameworks, yet synthetic protocols to benzo[f]indazole are severely scarce,which have hampered their biomedical *** our work,a novel and efficient strategy for the direct synthesis of benzo[f]indazoles via copper-catalyzed cascade reaction of sulfonyl hydrazides with 1,3-enynes under mild conditions has been *** method achieves the formation of two C-N bonds and one C-C bond in one pot,providing a series of benzo[f]indazoles in good yields with good functional group tolerance and remarkable regioselectivity.