Cyclopropanesulfonyl chloride → HCID 51346984, compound

Participants

Reaction Steps

185 mg N-(3-{2-amino-5-fluoro-3-[(2-fluoro-4-iodophenyl)amino]phenoxy}-2-methylphenyl)ethanesulfonamide (0.33 mmol, 1 eq.) were dissolved in 3 mL pyridine, and treated with 49 mg cyclopropyl sulfonyl chloride (0.33 mmol, 1 eq.) and stirred at it for 16 h. Further 15 mg cyclopropyl sulfonyl chloride were added and stirring was continued for 4 h. Additional 15 mg cyclopropyl sulfonyl chloride were added and stirring was continued overnight. The reaction mixture was quenched with water, diluted with toluene and concentrated in vacuo. The residue was portioned between water and ethyl acetate, the aqueous layer reextracted with ethyl acetate, the combined organic layers dried, filtered and concentrated in vacuo. Flash column chromatography provided 150 mg of the target compound (64% yield).

Provenance & Evidence