Methanol → 8-[1-(2,3-Dihydroxy-propyl)-cyclopropanesulfonylamino]-7-(2-fluoro-4-iodo-phenylamino)-6-methyl-5-oxo-2,3-dihydro-5H-imidazo[1,2-a]pyridine-1-carboxylic acid tert-butyl ester

Participants

Reaction Steps

OsO4 (0.004 g, 0.00002 mol) was added to a stirred solution of 8-(1-allyl-cyclopropanesulfonylamino)-7-(2-fluoro-4-iodo-phenylamino)-6-methyl-5-oxo-2,3-dihydro-5H-imidazo[1,2-a]pyridine-1-carboxylic acid tert-butyl ester (125 mg, 0.0002 mol) and N-methylmorpholine-N-oxide (34 mg, 0.0003 mol) in water and THF (3 mL). The resulting mixture was stirred at room temperature for 3 hours. The reaction was monitored by TLC (10% MeOH in CHCl3). The reaction mixture was partitioned between ethylacetate and water. The organic layer concentrated to afford 80 mg of the crude product which was used in the next step without further purification.

Provenance & Evidence