4-Piperidinecarboxylic acid → 1-(5-Cyano-2-pyridinyl)-4-piperidinecarboxylic acid

Participants

Reaction Conditions

Reaction Steps

A suspension of 1.8 g of 6-bromonicotinic acid nitrile, 1.3 g of 4-piperidinylcarboxylic acid and 1.06 g of sodium carbonate in 15 ml of dimethylformamide is stirred for 2 hours at 120° C. After cooling, the suspension is diluted with water. 2.0 g of ammonium chloride are added and the aqueous phase is extracted with ethyl acetate. The organic phase is washed with saturated saline solution, dried over sodium sulphate and the solvent is removed under reduced pressure. Yield: 1.2 g (52% of theory), Rf value: 0.29 (silica gel; methylene chloride/methanol/conc. ammonia=4:1:0.25)

Provenance & Evidence