1-[2-(4-Aminopiperidin-1-yl)ethyl]-2-oxo-1,2-dihydroquinoline-7-carbonitrile → 4-[2-(4-Aminopiperidin-1-yl)ethyl]-6-fluoro-2H-1,4-benzoxazin-3(4H)-one

HRID 1644331Notizen

Reaktionsgleichung

Reaktionsgleichung von HRID 1644331
C(OC(=O)[NH:7][CH:8]1[CH2:13][CH2:12][N:11]([CH2:14][CH2:15][N:16]2[C:21]3[CH:22]=[C:23]([F:26])[CH:24]=[CH:25][C:20]=3[O:19][CH2:18][C:17]2=[O:27])[CH2:10][CH2:9]1)(C)(C)C.NC1CCN(CCN2C3C(=CC=C(C#N)C=3)C=CC2=O)CC1>>[NH2:7][CH:8]1[CH2:9][CH2:10][N:11]([CH2:14][CH2:15][N:16]2[C:21]3[CH:22]=[C:23]([F:26])[CH:24]=[CH:25][C:20]=3[O:19][CH2:18][C:17]2=[O:27])[CH2:12][CH2:13]1

Komponenten

3

Edukt 2

HCID 602009201-[2-(4-Aminopiperidin-1-yl)ethyl]-2-oxo-1,2-dihydroquinoline-7-carbonitrileHCID 86642612tert-Butyl {1-[2-(6-fluoro-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)ethyl]piperidin-4-yl}carbamate2×

Produkt 1

HCID 667743534-[2-(4-Aminopiperidin-1-yl)ethyl]-6-fluoro-2H-1,4-benzoxazin-3(4H)-one

Versuchsvorschrift

tert-Butyl{1-[2-(6-fluoro-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)ethyl]piperidin-4-yl}carbamate (Intermediate 55) (640 mg, 1.56 mmol) was reacted as described for Intermediate 14. The crude trifluoro acetate of the title compound was used without further purification for the next step (quantitative yield).

Aufarbeitung

  1. customThe crude trifluoro acetate of the title compound was used without further purification for the next step (quantitative yield)

Quellen und Nachweise

ORD-Eintrag
ord-b8de42c9f0f845109d7ffdac7bf20fef
Quelldatensatz
uspto-grants-2012_02
Patentnummer
US08124602B2

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