Diisopropylethylamine → (S)-4-{6-Chloro-2-[1-(4-fluorophenyl)ethylamino]pyrimidin-4-yl}piperazine-2,6-dione
Reaktionsgleichung
Cl[C:2]1[CH:7]=[C:6]([Cl:8])[N:5]=[C:4]([NH:9][C@H:10]([C:12]2[CH:17]=[CH:16][C:15]([F:18])=[CH:14][CH:13]=2)[CH3:11])[N:3]=1.[NH:19]1[C:24](=[O:25])[CH2:23][NH:22][CH2:21][C:20]1=[O:26].C(N(CC)C(C)C)(C)C>O1CCCC1.CN(C)C=O.C(OCC)(=O)C>[Cl:8][C:6]1[N:5]=[C:4]([NH:9][C@H:10]([C:12]2[CH:17]=[CH:16][C:15]([F:18])=[CH:14][CH:13]=2)[CH3:11])[N:3]=[C:2]([N:22]2[CH2:23][C:24](=[O:25])[NH:19][C:20](=[O:26])[CH2:21]2)[CH:7]=1Komponenten
7
Edukt 3
Produkt 1
Reagenzien, Katalysatoren, Lösungsmittel 3
Reaktionsbedingungen
- Temperatur
- 80 °C
Versuchsvorschrift
182 mg of (S)-4,6-dichloro-N-[1-(4-fluorophenyl)ethyl]pyrimidine-2-amine (Reference Example 1) and 80 mg of piperazine-2,6-dione were dissolved in 2 ml of tetrahydrofuran and 2 ml of N,N-dimethylformamide, and 122 μl of N,N-diisopropylethylamine was added thereto, and the mixture was stirred at 80° C. for 32 hours. The reaction solution was air-cooled to room temperature, and then diluted with ethyl acetate. The solution was washed with water and then dried over magnesium sulfate. The solvent was distilled off under reduced pressure to obtain 136 mg of the objective compound as white powder.
Aufarbeitung
- temperatureThe reaction solution was air-cooled to room temperature
- washThe solution was washed with water
- dry with materialdried over magnesium sulfate
- distillationThe solvent was distilled off under reduced pressure
Quellen und Nachweise
- ORD-Eintrag
- ord-a79bdee204fa4a10b4da810c19c19701
- Quelldatensatz
- uspto-grants-2014_03
- Patentnummer
- US08673891B2
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