Reacción #439616

Ecuación de reacción

hydrochloric acid

1-benzyl-4-methylaminopiperidine

cyclopropane carboxaldehyde

sodium cyanoborohydride

→

1-benzyl-4-(cyclopropylmethyl-methyl-amino)-piperidine

Rendimiento 95.0%

Disolventes

methanol

Condiciones de reacción

Tratamiento posterior

1. 1
   workup.WAITfor about 16 hours at ambient temperature
2. 2
   Otroevaporated to dryness in vacuo
3. 3
   LavadoIt is washed with ether
4. 4
   Extracciónextracted with ether/ethyl acetate
5. 5
   ExtracciónThe organic extract
6. 6
   Secadois dried over sodium sulphate

Procedimiento

18.9 g of 1-benzyl-4-methylaminopiperidine in the form of the oil prepared in a) are taken up in 250 ml of methanol, combined with 8.3 g of cyclopropane carboxaldehyde and 11.3 g of sodium cyanoborohydride. The mixture is stirred for 5 hours at 40-50° C., then for about 16 hours at ambient temperature. It is then acidified with 2 N hydrochloric acid, evaporated to dryness in vacuo and the residue is taken up in water. It is washed with ether, made alkaline with concentrated sodium hydroxide solution and extracted with ether/ethyl acetate. The organic extract is dried over sodium sulphate and freed from solvents in vacuo. 22.7 g of 1-benzyl-4-(cyclopropylmethyl-methyl-amino)-piperidine are obtained as a yellowish oil.

Fuente