Sodium borohydride → 1-(2-Hydroxy-ethyl)-cyclopropanesulfonic acid [7-(2-fluoro-4-iodo-phenylamino)-6-methyl-5-oxo-2,3-dihydro-5H-oxazolo[3,2-a]pyridin-8-yl]-amide

Participants

Reaction Steps

Sodium borohydride (0.1 g, 2.6 mmol) was added to a stirred solution of 1-(2-Oxo-ethyl)-cyclopropanesulfonic acid [7-(2-fluoro-4-iodo-phenylamino)-6-methyl-5-oxo-2,3-dihydro-5H-oxazolo[3,2-a]pyridin-8-yl]-amide (0.12 g, 0.21 mmol) in THF (5 mL) and MeOH (2 mL) at room temperature. The resulting mixture was stirred at room temperature for 1 hour. The reaction was monitored by TLC (10% MeOH in DCM). The reaction mixture was concentrated under reduced pressure and partitioned between ethylacetate and water. The organic layer was washed with water, brine solution, dried over Na2SO4, filtered and the filtrate was concentrated. Purification by column chromatography on silica gel (2-4% MeOH in DCM) afforded 70 mg of the product (58% yield).

Provenance & Evidence