Azetidine → HCID 57378391, compound

Participants

Reaction Conditions

Reaction Steps

A mixture of 5-(2-((2-fluoroethyl)(methyl)amino)-[1,2,4]triazolo[1,5-a]pyridin-7-ylcarbamoyl)-1-methyl-1H-pyrazole-4-carboxylic acid (100 mg, 277 μmol), azetidine (74.6 μl, 1.11 mmol) and propylphosphonic anhydride (50% in ethyl acetate, 408 μl, 692 μmol) in tetrahydrofuran (5 ml) was stirred for 18 hours at 25° C. The solvent was evaporated, the residue was triturated with sodium hydrogencarbonate solution. The precipitated solid was filtered off, washed with water and dried in vacuo affording 4-(azetidine-1-carbonyl)-2-methyl-2H-pyrazole-3-carboxylic acid {2-[(2-fluoro-ethyl)-methyl-amino]-[1,2,4]triazolo[1,5-a]pyridin-7-yl}-amide (93 mg, 83.9%) as a white solid. mp: 236-237° C., MS: m/z=401.1 (M+H+)

Provenance & Evidence