Reacción #1174

Ecuación de reacción

K2CO3

1-Benzyloxycarbonyl-4-phthalimidylpiperidine

hydrazine monohydrate

→

4-amino-1-benzyloxycarbonylpiperidine

Rendimiento 85.0%

Disolventes

ethanol

Brine

Condiciones de reacción

Tratamiento posterior

1. 1
   Extracciónthe mixture was extracted with 5% MeOH/CHCl3 (3×)
2. 2
   LavadoThe combined extracts were washed with 2N aq. HCl, 2N aq. NaOH, brine solution
3. 3
   Secadodried over Na2SO4
4. 4
   Concentraciónconcentrated

Procedimiento

1-Benzyloxycarbonyl-4-phthalimidylpiperidine (1.50 g, 4.27 mmol), prepared in Example 16B, was taken up in 20 mL of ethanol. To this solution was added hydrazine monohydrate (35 mL, 700 mmol) and this mixture was heated at 100° C. for 3 h. Brine solution (40 mL) and 10% aq. K2CO3 (60 mL) were added and the mixture was extracted with 5% MeOH/CHCl3 (3×). The combined extracts were washed with 2N aq. HCl, 2N aq. NaOH, brine solution, dried over Na2SO4 and concentrated to give 0.847 g, (85%) of 4-amino-1-benzyloxycarbonylpiperidine. [1H]-NMR(CDCl3) consistent with structure.

Fuente