2-Naphthylalanine → 1-{2-[1-(4-Fluoro-benzyl)-6,8-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl]-ethyl}-3-(2-methyl-quinolin-4-yl)-urea
Reaktionsgleichung
[F:1][C:2]1[CH:22]=[CH:21][C:5]([CH2:6][CH:7]2[C:16]3[C:11](=[CH:12][C:13]([O:19][CH3:20])=[CH:14][C:15]=3[O:17][CH3:18])[CH2:10][CH2:9][NH:8]2)=[CH:4][CH:3]=1.Cl[CH2:24][CH2:25][NH:26][C:27]([NH:29][C:30]1[C:39]2[C:34](=[CH:35][CH:36]=[CH:37][CH:38]=2)[N:33]=[C:32]([CH3:40])[CH:31]=1)=[O:28].N[C@H](C(O)=O)CC1C=C2C(C=CC=C2)=CC=1>C1COCC1>[F:1][C:2]1[CH:3]=[CH:4][C:5]([CH2:6][CH:7]2[C:16]3[C:11](=[CH:12][C:13]([O:19][CH3:20])=[CH:14][C:15]=3[O:17][CH3:18])[CH2:10][CH2:9][N:8]2[CH2:24][CH2:25][NH:26][C:27]([NH:29][C:30]2[C:39]3[C:34](=[CH:35][CH:36]=[CH:37][CH:38]=3)[N:33]=[C:32]([CH3:40])[CH:31]=2)=[O:28])=[CH:21][CH:22]=1Komponenten
5
Edukt 3
Produkt 1
Reagenzien, Katalysatoren, Lösungsmittel 1
Reaktionsbedingungen
- Temperatur
- 75 °C
Versuchsvorschrift
To a solution of 1-(4-fluoro-benzyl)-6,8-dimethoxy-1,2,3,4-tetrahydro-isoquinoline (example A1, 50 mg, 0.16 mmol) in anhydrous THF (2.5 mL) is added 1-(2-chloro-ethyl)-3-(2-methyl-quinolin-4-yl)-urea (example D1, 43.8 mg, 0.16 mmol), TEA (34.6 μL, 0.25 mmol) and Nal (2.5 mg, 0.017 mmol). The mixture is stirred at 75° C. for five days in a sealed flask. The reaction mixture is evaporated, and the residue is purified by preparative HPLC to provide the title compound.
Aufarbeitung
- customThe reaction mixture is evaporated
- customthe residue is purified by preparative HPLC
Quellen und Nachweise
- ORD-Eintrag
- ord-b10086768987492e9db8d3923b980bcc
- Quelldatensatz
- uspto-grants-2004_11
- Patentnummer
- US06815451B2
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