Triethylamine → 3-chloro-N-(3-(4-(1-(2-cyano-1-cyclopropylethyl)-1H-pyrazol-4-yl)-5-methoxypyrimidin-2-ylamino)phenyl)propane-1-sulfonamide

Participants

Reaction Steps

To a mixture of 3-(4-{2-[(3-aminophenyl)amino]-5-methoxypyrimidin-4-yl}-1H-pyrazol-1-yl)-3-cyclopropylpropanenitrile (prepared according to Example 345, 8.0 mg, 0.000021 mol) in 1,4-dioxane (0.1 mL, 0.002 mol) was added triethylamine (0.02 mL, 0.0001 mol), followed by 3-chloropropane-1-sulfonyl chloride (0.0039 mL, 0.000032 mol). The reaction was stirred at room temperature for 1 h, quenched with 1 N HCl. The mixture was extracted with EtOAc and the organic layer was separated. The combined organic layers were washed with brine, dried over MgSO4, and evaporated to dryness to provide the desired sulfonylated intermediate.

Provenance & Evidence