Triethylamine → HCID 46186796, compound

Participants

Reaction Steps

In analogy to GP 6a, 240 mg of 2-(3-amino-phenoxy)-4-fluoro-6-(2-fluoro-4-iodo-phenylamino)-benzamide (Intermediate 1.4; 0.5 mmol, 1 eq.) were dissolved in 8 mL THF and treated with 0.1 mL triethylamine (0.75 mmol, 1.5 eq.) and 71 μL ethylsulfonyl chloride (0.75 mmol, 1.5 eq.). The reaction mixture was stirred at rt overnight, diluted with ethyl acetate, washed with saturated NaHCO3 solution, dried and concentrated in vacuo. HPLC purification of the residue provided 123 mg (0.22 mmol, 48% yield) of the desired compound.

Provenance & Evidence