Hydrochloric Acid → 1-(5-Amino-2,4-difluorophenyl)-8-chloro-6-fluoro-7-(2-hydroxy-1-methylethylamino)-4-oxo-1,4-dihydroquinoline-3-carboxylic Acid

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Reaktionsgleichung

[NH2:1][C:2]1[C:3]([F:26])=[CH:4][C:5]([F:25])=[C:6]([N:8]2[C:17]3[C:12](=[CH:13][C:14]([F:20])=[C:15](F)[C:16]=3[Cl:18])[C:11](=[O:21])[C:10]([C:22]([OH:24])=[O:23])=[CH:9]2)[CH:7]=1.[NH2:27][CH:28]([CH3:31])[CH2:29][OH:30].Cl>N1C=CC=CC=1>[NH2:1][C:2]1[C:3]([F:26])=[CH:4][C:5]([F:25])=[C:6]([N:8]2[C:17]3[C:12](=[CH:13][C:14]([F:20])=[C:15]([NH:27][CH:28]([CH3:31])[CH2:29][OH:30])[C:16]=3[Cl:18])[C:11](=[O:21])[C:10]([C:22]([OH:24])=[O:23])=[CH:9]2)[CH:7]=1

Komponenten

Reaktionsbedingungen

Temperatur: 50 °C

Versuchsvorschrift

1-(5-Amino-2,4-difluorophenyl)-8-chloro-6,7-difluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (200 mg) and 2-amino-1-propanol (200 mg) were added to pyridine (700 mg), and the mixture was stirred at 50° C. for 1.5 hours. Concentrated hydrochloric acid (200 mg) was added to the reaction mixture, and the resultant mixture was concentrated under reduced pressure. Ethanol (3 ml) was added to the residue, and deposits were collected by filtration and washed with ethanol and disopropyl ether in that order to obtain the title compound (167 mg) as a yellow powder.

Aufarbeitung

concentrationthe resultant mixture was concentrated under reduced pressure
additionEthanol (3 ml) was added to the residue, and deposits
filtrationwere collected by filtration
washwashed with ethanol and disopropyl ether in that order

Quellen und Nachweise

ORD-Eintrag: ord-e8b46cfcac8a49878c072d717252cf16
Quelldatensatz: uspto-grants-2000_10
DOI: 10.6084/m9.figshare.5104873.v1
Patentnummer: US06136823

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