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0 °C

To a solution of 5-(2-fluoro-4-iodophenylamino)imidazo[1,5-a]pyridine-6-carboxylic acid methyl ester (1.5 g, 3.64 mmol) and O-(2-vinyloxyethyl)hydroxylamine (749 mg, 7.28 mmol) in THF (30 mL) at 0° C. was added lithium bis(trimethylsilyl)amide as a solution in THF (18 mL, 1M, 18 mmol) over 5 minutes. The reaction mixture was stirred at −0° C. for 1 hour before being quenched with saturated aqueous ammonium chloride. Volatile solvents were removed in vacuo and then diethyl ether (10 mL) and ethyl acetate (20 mL) added. The resultant mixture was sonicated causing a precipitate to form which was filtered off to give the title compound as a yellow solid (1.07 g, 61%). LCMS (Method B): RT=2.79 min, M+H+=483.

1. custombefore being quenched with saturated aqueous ammonium chloride
2. customVolatile solvents were removed in vacuo
3. additiondiethyl ether (10 mL) and ethyl acetate (20 mL) added
4. customThe resultant mixture was sonicated
5. customto form which
6. filtrationwas filtered off