Version 2 2024-02-06, 18:26Version 2 2024-02-06, 18:26
Version 1 2024-02-05, 16:13Version 1 2024-02-05, 16:13
journal contribution
posted on 2024-02-06, 18:26authored byAnna Schoeggl Toledano, Jacqueline Bitai, David Covini, Jale Karolyi-Oezguer, Christian Dank, Helmut Berger, Andreas Gollner
Herein
we report a method for the synthesis of indazoles from readily
available 2-aminomethyl-phenylamines via N–N bond-forming oxidative
cyclization. Inspired by indazole formation initially observed as
a side product by N. Coskun et al. we developed a robust protocol
to access indazoles in all three tautomeric forms. The method selectively
gives access to various 2-substituted 2H-indazoles
which are frequently used in drug design, and we also demonstrated
its applicability to less studied 3H-indazoles.