Boron Trichloride → 3-Hydroxy-cyclobutanesulfonic acid [7-(2-fluoro-4-iodo-phenylamino)-6-methyl-5-oxo-2,3-dihydro-5H-oxazolo[3,2-a]pyridin-8-yl]-amide

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Reaction Steps

3-Benzyloxy-cyclobutanesulfonic acid [7-(2-fluoro-4-iodo-phenylamino)-6-methyl-5-oxo-2,3-dihydro-5H-oxazolo[3,2-a]pyridin-8-yl]-amide (180 mg, 0.288 mmol) in DCM (10 mL) was reacted with 1M BCl3 (0.86 mL, 0.864 mmol) at −78° C. The resulting mixture was stirred at room temperature for 1 hour. Purification by column chromatography on silica gel (4% MeOH in DCM), followed by preparative HPLC afforded 45 mg of the product (30% yield).

Provenance & Evidence