Sodium Chloride → tert-butyl 2-methyl-1-[(2R)-4-methyl-1-oxo-1-[2-oxo-8-(2-oxopyrrolidin-1-yl)-1-(thiophen-3-ylmethyl)-1,2,3,4-tetrahydroquinolin-3-ylamino]pentan-2-ylamino]-1-oxopropan-2-ylcarbamate
Reaktionsgleichung
[NH2:1][C@H:2]([CH2:29][CH:30]([CH3:32])[CH3:31])[C:3]([NH:5][CH:6]1[CH2:15][C:14]2[C:9](=[C:10]([N:16]3[CH2:20][CH2:19][CH2:18][C:17]3=[O:21])[CH:11]=[CH:12][CH:13]=2)[N:8]([CH2:22][C:23]2[CH:27]=[CH:26][S:25][CH:24]=2)[C:7]1=[O:28])=[O:4].[C:33]([O:37][C:38]([NH:40][C:41]([CH3:46])([CH3:45])[C:42](O)=[O:43])=[O:39])([CH3:36])([CH3:35])[CH3:34].ON1C2C=CC=CC=2N=N1.Cl.C(N=C=NCCCN(C)C)C.[Cl-].[Na+]>O1CCCC1>[CH3:46][C:41]([NH:40][C:38](=[O:39])[O:37][C:33]([CH3:36])([CH3:35])[CH3:34])([CH3:45])[C:42]([NH:1][C@H:2]([CH2:29][CH:30]([CH3:32])[CH3:31])[C:3](=[O:4])[NH:5][CH:6]1[CH2:15][C:14]2[C:9](=[C:10]([N:16]3[CH2:20][CH2:19][CH2:18][C:17]3=[O:21])[CH:11]=[CH:12][CH:13]=2)[N:8]([CH2:22][C:23]2[CH:27]=[CH:26][S:25][CH:24]=2)[C:7]1=[O:28])=[O:43]Komponenten
7
Edukt 5
Produkt 1
Reagenzien, Katalysatoren, Lösungsmittel 1
Versuchsvorschrift
To the tetrahydrofuran solution of (2R)-2-amino-4-methyl-N-[2-oxo-8-(2-oxopyrrolidin-1-yl)-1-(thiophen-3-ylmethyl)-1,2,3,4-tetrahydroquinolin-3-yl]pentanamide were sequentially added 2-(tert-butoxycarbonylamino)-2-methylpropanoic acid (20.4 g), 1-hydroxybenzotriazole (15.3 g), and 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride (19.2 g) under cooling on ice, and the mixture was stirred at room temperature for two hours. Saturated aqueous sodium chloride solution was added to the resultant mixture, and the organic layer was separated, whereby a solution of the title compound in tetrahydrofuran was yielded.
Aufarbeitung
- temperatureunder cooling on ice
- customthe organic layer was separated
Quellen und Nachweise
- ORD-Eintrag
- ord-2fac4af0a90747d4bb98ffbea6a12137
- Quelldatensatz
- uspto-grants-2012_10
- Patentnummer
- US08299255B2
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