Chlorosulfonic acid → 5-fluoro-1-{[2-(3-fluorophenyl)pyrimidine-5-carbonyl]amino}-1H-indole-3-sulfonyl chloride

Participants

Reaction Steps

A solution of 2-(3-fluorophenyl)pyrimidine-5-carboxylic acid-(5-fluoroindol-1-yl)amide (0.35 g,) in dry CH3CN (20 mL) is treated with chlorosulfonic acid (0.5 mL) and stirred at rt for 24 h. The reaction mixture is poured onto ice/water (150 mL) and extracted with EtOAc. The organic layer is washed with water, brine and dried (MgSO4), filtered and concentrated in vacuo to afford 5-fluoro-1-{[2-(3-fluorophenyl)pyrimidine-5-carbonyl]amino}-1H-indole-3-sulfonyl chloride (0.43 g, 95%). MS: 449 (M+H).

Provenance & Evidence