Efficient Synthesis of 1‐Aryl‐1H‐indazole Derivatives via Copper(I)‐Catalyzed Intramolecular Amination Reaction

Abstract

A copper(I)‐catalyzed intramolecular amination reaction using CuI, KOH, and 1,4‐dioxane at 105°C for the preparation of 1‐aryl‐1H‐indazole derivatives was described. The method was applied to a wide scope of substrates and afforded indazole products in high yields.

Keywords:

• arylhydrazones
• copper(I) iodide
• indazole
• intramolecular amination
• 1,10‐phenanthroline

Acknowledgment

This work was partially supported by the National Natural Science Foundation of China (Grants 20472062 and 20672079) and the Natural Science Foundation of Jiangsu Province (No. BK2006048).