A Scalable and Metal-Free Synthesis of Indazoles from 2-Aminophenones and In Situ Generated De-Boc-Protected O-Mesitylsulfonyl Hydroxylamine Derivatives

A one-pot metal-free protocol to access indazoles from easily available 2-aminophenones and hydroxylamine derivatives has been achieved. The reaction is operationally simple, mild, and insensitive to air and moisture. A broad range of indazoles were prepared in good to excellent yield (up to 97% yield), and the reaction displayed a broad functional group tolerance. The reaction was performed at gram scale, and its synthetic application was exhibited through the rapid and efficient preparation of bioactive molecule YC-3 and FDA-approved drug axitinib.