3-(Benzyloxy)cyclobutane-1-sulfonyl chloride → 3-Benzyloxy-cyclobutanesulfonic acid [7-(2-fluoro-4-iodo-phenylamino)-6-methyl-5-oxo-2,3-dihydro-5H-thiazolo[3,2-a]pyridin-8-yl]-amide

Participants

Reaction Steps

Using the same reaction conditions and workup as described for the preparation of Example 19A, 8-amino-7-(2-fluoro-4-iodo-phenylamino)-6-methyl-2,3-dihydro-thiazolo[3,2-a]pyridin-5-one (I-19f: 0.15 g, 0.35 mmol) in pyridine (2 mL) was reacted with 3-benzyloxy-cyclobutanesulfonyl chloride (0.1 g, 0.39 mmol) to afford the crude product. Purification by column chromatography on silica gel (50% ethylacetate in hexane) afforded 0.1 g of the product (43% yield).

Provenance & Evidence