Triethylamine → HCID 71522920, compound

Participants

Reaction Conditions

Reaction Steps

To a solution of 1-[5-(trifluoromethyl)-3-vinylpyridin-2-yl]piperidin-2-one a18-2 (310 mg, 1.147 mmol, 1 eq) and 2-pyrrolidin-3-yl pyridine (221 mg, 1.491 mmol, 1.3 eq) in ethanol (10 ml) is added triethylamine (348 mg, 479 μl, 3.441 mmol, 3 eq). The reaction mixture is stirred at 90° C. for 7 hours, then heated overnight at 85° C. The reaction mixture is evaporated to dryness and retaken in dichloromethane. This organic phase is washed with aqueous NH4Cl (1 time), saturated aqueous NaHCO3 (2 times), then dried over MgSO4, filtered and evaporated to dryness. The residue obtained is purified by flash chromatography over silicagel (12 g; gradient: from dichloromethane/MeOH 100/0 to 94/6), dried under vacuum to afford 91.4 mg of 1-[3-{2-[3-(pyridin-2-yl)pyrrolidin-1-yl]ethyl}-5-(trifluoromethyl)pyridin-2-yl]piperidin-2-one 110.

Provenance & Evidence