Methylamine → 5-{6-[(methylamino)methyl]3H-imidazo[4,5-c]pyridin-3-yl}-3-{(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy}thiophene-2-carboxamide

Participants

Reaction Steps

A solution of 75 mg of crude [3-(5-carbamoyl-4-{(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy}-2-thienyl)-3H-imidazo[4,5-c]pyridin-6-yl]methyl methanesulfonate (example 49, step 1) and 0.32 ml methylamine (2 M solution in methanol) in 1.5 ml methanol is stirred in a microwave vial at 120° C. for 6 h in the microwave cavity. The reaction mixture is concentrated to dryness and the resulting residue is purified by preparative HPLC (ammonium formate buffer/acetonitrile, elution gradient 97/3 to 0/100 (v/v)) to obtain the title product.

Provenance & Evidence