A general one-pot synthesis of 2H-indazoles using an organophosphorus-silane system
Authors
- J. Schoene
- H. Bel Abed
- P. Schmieder
- M. Christmann
- M. Nazaré
Journal
- Chemistry - A European Journal
Citation
- Chemistry 24 (36): 9090-9100
Abstract
A simple and direct approach for the regioselective construction of the privileged 2H‐indazole scaffold is described. The developed one‐pot strategy involves phospholene‐mediated N−N bond formation to access 2H‐indazoles. The amount of organophosphorus reagent was minimized by recycling the phospholene oxide with organosilane reductants. Starting from functionalized 2‐nitrobenzaldehydes and primary amines, a mild reductive cyclization, involving the use of commercially available phospholene oxide and silanes, delivered a wide variety of substituted 2H‐indazoles in good to excellent yields.