3-(Benzyloxy)cyclobutane-1-sulfonyl chloride → 8-(3-Benzyloxy-cyclobutanesulfonylamino)-7-(2-fluoro-4-iodo-phenylamino)-6-methyl-5-oxo-2,3-dihydro-5H-imidazo[1,2-a]pyridine-1-carboxylic acid tert-butyl ester

Participants

Reaction Steps

Using the same reaction conditions and workup as described for the preparation of Intermediate (I-5d), 8-Amino-7-(2-fluoro-4-iodo-phenylamino)-6-methyl-5-oxo-2,3-dihydro-5H-imidazo[1,2-a]pyridine-1-carboxylic acid tert-butyl ester (I-5c: 350 mg, 0.7 mmol) in pyridine (3 mL) was reacted with 3-benzyloxy-cyclobutanesulfonyl chloride (273 mg, 1.05 mmol) to afford the crude product. Purification by column chromatography on silica gel (80% ethylacetate in hexane) afforded 250 mg of the product (45.3% yield).

Provenance & Evidence