Triethylamine → Ethyl 1-(4-morpholin-4-ylbutyryl)4-piperidinecarboxylate

Participants

Reaction Conditions

Reaction Steps

0.95 g of N-(3-dimethylaminopropyl)-N′-ethylcarbodiimide in solution in 20 cm3 of dichloromethane is added, at 20° C., to 1.0 g of 4-morpholinobutyric acid, 0.78 g of ethyl isonipecotate, 2.1 cm3 of triethylamine and 20 mg of hydroxybenzotriazole hydrate, in solution in 80 cm3 of dichloromethane. After stirring for 20 hours at 20° C., the reaction mixture is washed with 20 cm3 of water. The organic phase is dried over magnesium sulfate, filtered and concentrated to dryness under reduced pressure (2.7 kPa) to give a pale yellow oil which is purified by chromatography on a CBT1 alumina column [eluent: dichloromethane/methanol (97/3 by volume)]. 1.30 g of ethyl 1-(4-morpholin-4-ylbutyryl)-4-piperidinecarboxylate are thus obtained in the form of a pale yellow oil.

Provenance & Evidence