An Efficient, Facile, and General Synthesis of 1H-Indazoles by 1,3-Dipolar Cycloaddition of Arynes with Diazomethane Derivatives

摘要

1H-Indazoles are pharmaceutically important compounds that display a wide range of pharmacological activities, including antifertility, antiarthritic, anti-inflammatory, and contraceptive activity, as well as antagonistic activity towards the 5-HT3 receptor. Because of this usefulness, considerable effort has been devoted to the development of efficient methods for the construction of indazole frameworks (Scheme 1).