Triethylamine → 6-Chloro-2-[(pyridin-2-ylmethyl)amino]nicotinoyl fluoride

Participants

Reaction Steps

2.27 ml of triethylamine (16.31 mmol) and 1.65 ml of 2,4,6-trifluorotriazine (19.57 mmol) are added successively to a suspension of 4.3 g of 6-chloro-2-[(pyridin-2-ylmethyl)amino]nicotinic acid (16.31 mmol) in 90 ml of dichloromethane. The mixture is stirred for 1 hour at ambient temperature and then a dichloromethane/ice-cold water mixture is added. The organic phase is washed 3 times with ice-cold NaHCO3aq and then dried over Na2SO4, filtered, and concentrated under vacuum. 3.97 g of expected product are obtained in the form of an orange solid. Yield=92%.

Provenance & Evidence