Water → N-(4,5-Difluoro-6-(2-fluoro-4-iodophenylamino)benzo[d]oxazol-7-yl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide

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Reaction Steps

Following the procedure set forth in Example 1I, 1-allyl-cyclopropanesulfonic acid [4,5-difluoro-6-(2-fluoro-4-iodo-phenylamino)benzoxazol-7-yl]-amide (7 g, 0.0127 mol) in THF (150 mL) was reacted with N-methyl morpholine-N-oxide (2.23 g, 0.019 mol), osmium tetroxide (0.32 g, 0.00127 mol) and water (15 mL) to afford the crude product. Purification by column chromatography on silica gel (0-2.5% methanol in DCM), followed by separation of the optical isomers using chiral HPLC afforded 1 g of the product

Provenance & Evidence