Herein, we report a t-BuONa-promoted method for the site-selective silylation of 2H-indazoles.
Indazoles as privileged scaffolds; synthetic strategies; clinical trial compounds; biological activities: anti-tubercular, antifungal, antibacterial, antileishmanial, anti-Parkinson's, anti-inflammatory, antidiabetic, and anticancer.
The electrochemical intramolecular cyclization of ketimines via N–H/N–H dehydrogenation coupling has been established for the construction of 1H-indazole scaffolds.
A [3 + 2] cycloaddition reaction utilizing cyclic diaryl λ3-bromanes and α-diazo esters to deliver either N–H or N-Me indazoles in a controllable manner is reported. DFT calculations explain the regioselectivity and the mechanism.
The indazole scaffold, with its planar, π-conjugated structure, enables extensive derivatization and tunable luminescence. This makes it ideal for sensing, bioimaging, and materials science, including applications like cell staining and drug development.