One Pot Procedure for Trisubstituted 1,2,4-Triazoles

Scientists at Genentech, San Francisco, have recently reported (Staben S T et al, Angew Chem Int Ed, 2010, 49, 325-8) a synthesis of triazoles that relies initially on a carbonylation of aromatic halides with CO and an amidine, the intermediate then being trapped by a hydrazine.

The procedure has been used in a one-pot synthesis of Deferasirox, the active ingredient in the drug Exjade, used as a chelator for patients with chronic iron overload.