Synthesis of Polycyclic Imidazoles via α-C–H/N–H Annulation of Alicyclic Amines

Abstract

Secondary alicyclic amines are converted into their corresponding ring-fused imidazoles in a simple procedure consisting of oxidative imine formation followed by a van Leusen reaction. Amines with an existing α-substituent undergo regioselective ring-fusion at the α′-position. This method was utilized in a synthesis of fadrozole.

Key words

C–H bond functionalization - amines - annulation - imidazoles - heterocycles

• References


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