(3-Methyloxetan-3-yl)methanesulfonyl chloride → N-(7-(2-fluoro-4-iodophenylamino)-6-methyl-5-oxo-3,5-dihydro-2H-oxazolo[3,2-a]pyridin-8-yl)-1-(3-methyloxetan-3-yl)methanesulfonamide

Participants

Reaction Steps

Using the same reaction conditions and procedure as described for the preparation of Example 7A, 8-Amino-7-(2-fluoro-4-iodo-phenylamino)-6-methyl-2,3-dihydro-oxazolo[3,2-a]pyridin-5-one (I-7f: 0.2 g, 0.499 mmol) was reacted with (3-methyloxetan-3-yl)methanesulfonyl chloride (0.13 g, 0.748 mmol) in dry pyridine (3 mL) to afford the crude product. Purification by preparative HPLC afforded 25 mg of the product (9% yield).

Provenance & Evidence