Direct C-H Alkenylation of Functionalized Indazoles under High-speed Ball-milling Conditions
作者单位：Collaborative Innovation Center of Yangtze River Delta Region Green Pharmaceuticals Zhejiang University of Technology 浙江工业大学
会议名称：《中国化学会·第十五届全国有机合成化学学术研讨会》
会议日期：2018年
学科分类：1007[医学-药学(可授医学、理学学位)] 10[医学]
关 键 词：indazoles C-H activation alkenylation ball milling
摘 要：Transition metal-catalyzed alkenylation of heteroarene C-H bonds has regained considerable attention over recent years .These reactions can potentially provide concise routes for constructing various drugs and drug *** an important class of heteroarenes, indazole motifs are embedded in numerous pharmaceuticals with a broad range of biological activities , including axitinib, pazopanib, benzydamine, granisetron, and ***, the installation of alkenyl groups onto the indazole ring has had limited success, particularly for(1H) indazole which confront with formidable challenge due to lack of *** two examples of alkenylation of(1H) indazole have been reported so far .However, these methods are more or less suffered from harsh reaction conditions such as noble metal oxidant, environmentally unfriendly solvent, or high ***, both their yields and substrate scope remain to be substantially ***, we developed a highly efficient and mild catalytic system for the C-3 alkenylation of(1H) indazole through C-H activation under high-speed ball-milling(HSBM) conditions with wide substrate scope and good yields.