Sulfuryl chloride → HCID 46195835, compound

Participants

Reaction Steps

In analogy to GP 6b, 100 mg of 2-(5-Amino-pyridin-3-yloxy)-4-fluoro-6-(2-fluoro-4-iodo-phenylamino)-benzamide (Intermediate 3.1; 0.21 mmol, 1 eq.) were dissolved in 1.5 mL pyridine and treated with 37 mg iso-propylsulfonyl chloride (0.26 mmol, 1.25 eq., dissolved in 0.5 mL pyridine). The reaction mixture was stirred at rt overnight, treated with another 1.25 eq. sulfonylchloride (in 0.2 mL pyridine) and stirring was continued at rt overnight. After addition of further 1.25 eq. sulfonylchloride (in 0.2 mL pyridine) and further stirring at rt for 3 days, the resulting mixture diluted with ethyl acetate, washed with water and the organic layers dried. Concentration in vacuo was followed by prepurification by chromatography and subsequent HPLC purification to provide the desired compound.

Provenance & Evidence