Diisopropylethylamine → HCID 71612386, compound

Participants

Reaction Steps

To a suspension of 147 mg 4-({2-[5-cyclopropyl-1-(4-ethoxy-2,6-difluorobenzyl)-4-methyl-1H-pyrazol-3-yl]-5-methoxypyrimidin-4-yl}amino)nicotinic acid 2-11-1 (0.27 mmol, 1.0 eq) and 67.5 mg 2-aminoethylmethyl sulfone (0.55 mmol, 2.0 eq) in 2.1 mL DMF were added 191 μL N,N-diisopropylethylamine (1.10 mmol, 4.0 eq) and 157 mg (benzotriazol-1-yloxy)tripyrrolidinophosphonium hexafluorophosphate (0.30 mmol, 1.1 eq). The resulting solution was stirred over night at rt and afterwards diluted with water. The precipitate was collected by filtration, washed with water and dried. The crude product was purified by preparative HPLC yielding 40 mg of analytically pure target compound (62 μmol, 22%).

Provenance & Evidence