(2Z)-3-(5-chloro-6-{[(3R)-1-cyclopentyl-3-pyrrolidinyl]amino}-3-pyridinyl)-2-fluoro-N-(tetrahydro-2H-pyran-2-yloxy)acrylamide → (2Z)-3-(5-chloro-6-{[(3R)-1-cyclopentyl-3-pyrrolidinyl]amino}-3-pyridinyl)-2-fluoro-N-hydroxyacrylamide dihydrochloride
Reaktionsgleichung
[Cl:1][C:2]1[CH:3]=[C:4](/[CH:19]=[C:20](\[F:31])/[C:21]([NH:23][O:24]C2CCCCO2)=[O:22])[CH:5]=[N:6][C:7]=1[NH:8][C@@H:9]1[CH2:13][CH2:12][N:11]([CH:14]2[CH2:18][CH2:17][CH2:16][CH2:15]2)[CH2:10]1>CCO>[ClH:1].[ClH:1].[Cl:1][C:2]1[CH:3]=[C:4](/[CH:19]=[C:20](\[F:31])/[C:21]([NH:23][OH:24])=[O:22])[CH:5]=[N:6][C:7]=1[NH:8][C@@H:9]1[CH2:13][CH2:12][N:11]([CH:14]2[CH2:15][CH2:16][CH2:17][CH2:18]2)[CH2:10]1Komponenten
3
Edukt 1
Produkt 1
Reagenzien, Katalysatoren, Lösungsmittel 1
Reaktionsbedingungen
- Temperatur
- 22.5 °C
Versuchsvorschrift
A solution of 2NHCl-EtOH solution (3.4 ml) was added to a mixture of (2Z)-3-(5-chloro-6-{[(3R)-1-cyclopentyl-3-pyrrolidinyl]amino}-3-pyridinyl)-2-fluoro-N-(tetrahydro-2H-pyran-2-yloxy)acrylamide (620 mg) in EtOH (5 ml) and stirred at 20-25° C. for 2 hours. IPE (20 ml) was added to a reaction mixture and the resultant mixture was stirred at ambient temperature for 20 minutes. The precipitate was collected by filtration to give (2Z)-3-(5-chloro-6-{[(3R)-1-cyclopentyl-3-pyrrolidinyl]amino}-3-pyridinyl)-2-fluoro-N-hydroxyacrylamide dihydrochloride (500 mg).
Aufarbeitung
- additionIPE (20 ml) was added to a reaction mixture
- filtrationThe precipitate was collected by filtration
Quellen und Nachweise
- ORD-Eintrag
- ord-40843c4cc0b541cf8778c8cbac7eb960
- Quelldatensatz
- uspto-grants-2009_07
- Patentnummer
- US07557127B2
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