Benzylamine → N-benzylpiperidin-4-amine
Reaktionsgleichung
[C:1]([BH3-])#[N:2].[Na+].[CH2:5]([NH2:12])[C:6]1[CH:11]=[CH:10][CH:9]=[CH:8][CH:7]=1>>[CH2:5]([NH:12][CH:6]1[CH2:5][CH2:1][NH:2][CH2:8][CH2:7]1)[C:6]1[CH:11]=[CH:10][CH:9]=[CH:8][CH:7]=1Komponenten
3
Versuchsvorschrift
The compounds of formula A and G are prepared as is described in Reaction Sequences 1 and 2. Compound G is then treated with sodium cyanoborohydride, optionally in the presence of benzylamine, to produce the 4-(benzyl)amino piperidine which is subsequently coupled with the compound of formula A to produce the benzyl derivative (formula G"). The compound of formula G" is then hydrogenated using, for instance, palladium-on-carbon catalyst to produce the compound of formula I.
Aufarbeitung
- customThe compounds of formula A and G are prepared
- customas is described in Reaction Sequences 1 and 2
Quellen und Nachweise
- ORD-Eintrag
- ord-746d12cd9afa47d7b19365652c6d5842
- Quelldatensatz
- uspto-grants-1985_02
- Patentnummer
- US04499100
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