Methanol → Cyclopropanesulfonic acid [7-(2-fluoro-4-iodo-phenylamino)-6-methyl-5-oxo-2,3-dihydro-5H-thiazolo[3,2-a]pyridin-8-yl]-amide

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Reaction Steps

Cyclopropane sulfonyl chloride (34 mg, 0.23 mmol) was added to a solution of 8-amino-7-(2-fluoro-4-iodo-phenylamino)-6-methyl-2,3-dihydro-thiazolo[3,2-a]pyridin-5-one (0.09 g, 0.21 mmol) in pyridine (1 mL) at 0° C. The resulting mixture was stirred at room temperature overnight. The reaction was monitored by TLC (5% MeOH in CHCl3). The reaction mixture was partitioned between ethylacetate and water. The organic layer was washed with 2N HCl, brine solution, dried over Na2SO4 and concentrated. Purification by column chromatography on silica gel (1% MeOH in CHCl3), followed by preparative HPLC afforded 25 mg of the product (22% yield).

Provenance & Evidence