تفاعل #1174

معادلة التفاعل

K2CO3

1-Benzyloxycarbonyl-4-phthalimidylpiperidine

hydrazine monohydrate

→

4-amino-1-benzyloxycarbonylpiperidine

المردود 85.0%

المذيبات

ethanol

Brine

ظروف التفاعل

المعالجة

1. 1
   استخلاصthe mixture was extracted with 5% MeOH/CHCl3 (3×)
2. 2
   غسيلThe combined extracts were washed with 2N aq. HCl, 2N aq. NaOH, brine solution
3. 3
   تجفيفdried over Na2SO4
4. 4
   تركيزconcentrated

الإجراء التجريبي

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.

المصدر