Trifluoroacetic acid → 4-Chloro-5,7-difluoro-3-methyl-2-(piperazin-1-yl)quinoline 2,2,2-trifluoroacetate

HRID 1431645Notizen

Reaktionsgleichung

Reaktionsgleichung von HRID 1431645
[Cl:1][C:2]1[C:11]2[C:6](=[CH:7][C:8]([F:13])=[CH:9][C:10]=2[F:12])[N:5]=[C:4]([N:14]2[CH2:19][CH2:18][N:17](C(OC(C)(C)C)=O)[CH2:16][CH2:15]2)[C:3]=1[CH3:27].[F:28][C:29]([F:34])([F:33])[C:30]([OH:32])=[O:31]>ClCCl>[F:28][C:29]([F:34])([F:33])[C:30]([OH:32])=[O:31].[Cl:1][C:2]1[C:11]2[C:6](=[CH:7][C:8]([F:13])=[CH:9][C:10]=2[F:12])[N:5]=[C:4]([N:14]2[CH2:19][CH2:18][NH:17][CH2:16][CH2:15]2)[C:3]=1[CH3:27]

Komponenten

4

Edukt 2

HCID 6422Trifluoroacetic acidHCID 59631055Tert-butyl 4-(4-chloro-5,7-difluoro-3-methylquinolin-2-yl)piperazine-1-carboxylate

Produkt 1

HCID 866495114-Chloro-5,7-difluoro-3-methyl-2-(piperazin-1-yl)quinoline 2,2,2-trifluoroacetate

Reagenzien, Katalysatoren, Lösungsmittel 1

HCID 6344DichloromethaneLösungsmittel

Reaktionsbedingungen

Temperatur
0 °C

Versuchsvorschrift

The tert-butyl 4-(4-chloro-5,7-difluoro-3-methylquinolin-2-yl)piperazine-1-carboxylate (370 mg, 0.93 mmol) was dissolved in dichloromethane (3.0 mL) and cooled to 0° C. The trifluoroacetic acid (0.50 mL, 6.5 mmol) was added and the mixture was stirred for 2 h while warming to rt. The mixture was then cond and triturated with EtOAc. The slurry was filtered to give 4-chloro-5,7-difluoro-3-methyl-2-(piperazin-1-yl)quinoline 2,2,2-trifluoroacetate. Mass Spectrum (ESI) m/e=298.1 (M+1).

Aufarbeitung

  1. temperaturewhile warming to rt
  2. customcond and triturated with EtOAc
  3. filtrationThe slurry was filtered

Quellen und Nachweise

ORD-Eintrag
ord-5b0424d490af4a17afc9b565a1b6a4eb
Quelldatensatz
uspto-grants-2015_01
Patentnummer
US08940724B2

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