Cyclopropanesulfonyl chloride → HCID 67083644, compound

Participants

Reaction Steps

To a solution of 5-amino-4-(2-fluoro-4-iodo-phenylamino)-indazole-1-carboxylic acid tert-butyl ester (200 mg, 0.43 mmol) in pyridine (2 mL) was added cyclopropyl sulfonyl chloride (0.218 mL, 2.14 mmol) and the mixture stirred at room temperature for 1 hour. The reaction mixture was concentrated in vacuo and the residue partitioned between ethyl acetate (100 mL) and water (100 mL). The organic layer was separated, washed with brine, then dried (Na2SO4), filtered and concentrated in vacuo. The resultant residue was subjected to flash chromatography (Si—PPC, gradient 10-35% ethyl acetate in cyclohexane) to yield the title compound (206 mg, 84%). LCMS (Method B): RT=4.17 min, [MH]+=573.

Provenance & Evidence