Triethylamine → 2-{2,5-Difluoro-4-[2-((1S,2R)-2-{1-[5-(methoxymethyl)pyrimidin-2-yl]piperidin-4-yl}cyclopropyl)ethoxy]phenyl}-N,N-dimethylacetamide

Participants

Reaction Steps

To a solution of 2-(2,5-difluoro-4-{2-[(1S,2R)-2-piperidin-4-ylcyclopropyl]ethoxy}phenyl-)-N,N-dimethylacetamide (40.0 mg, 0.109 mmol) in 1 ml anhydrous DMF at RT was added triethylamine (0.046 ml, 0.33 mmol) and 2-chloro-5-(methoxymethyl)pyrimidine (20.8 mg, 0.131 mmol). The mixture was stirred at RT for 2 hours. The mixture was filtered and purified by reverse-phase HPLC (SunFire Prep C18 OBD Sum 19×100 mm column; 35-65% acetonitrile in 0.1% formic acid in water gradient) to afford the title compound. LC/MS (m/z): 489.5 (M+H)+. Human EC50: 1.6 nM

Provenance & Evidence