Reaktionsgleichung
C(N)(=O)CCC(N)=O.[C:9]1([NH:15][C:16](=[O:21])[CH2:17][C:18](O)=O)[CH:14]=[CH:13][CH:12]=[CH:11][CH:10]=1.NC1C=CC=CC=1.ClCC(=O)C[C:33]([O:35]C)=[O:34].[OH-].[Li+]>>[C:9]1([NH:15][C:16](=[O:21])[CH2:17][CH2:18][C:33]([OH:35])=[O:34])[CH:14]=[CH:13][CH:12]=[CH:11][CH:10]=1Komponenten
6
Versuchsvorschrift
The synthesis of the succinamide analogs 29, 30, 31, 32, and 33 are described in Schemes 12, 13, and 14. N-Phenyl-succinamic acid was prepared via a two step reaction sequence analogous to the preparation of the N-phenyl-malonamic acid: 1) reaction of aniline with methyl 4-chloro-3-oxobutyrate followed by 2) treatment with lithium hydroxide. Coupling of N-phenyl-succinamic acid with 1-(2-methylamino-(S)-2-phenyl-ethyl)-pyrrolidin-(S)-3-ol, 1-(3-methyl-(S)-2-methylamino-butyl)-pyrrolidin-(S)-3-ol or 1-piperidin-(S)-2-ylmethyl-pyrrolidin-(S)-3-ol afforded 29, 30 and 31, respectively.
Quellen und Nachweise
- ORD-Eintrag
- ord-af277b7469404150b416483520c15498
- Quelldatensatz
- uspto-grants-2007_01
- Patentnummer
- US07160902B2
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