Trifluoroacetic acid → HCID 178461788, Verbindung

HRID 1175995Notizen

Reaktionsgleichung

Reaktionsgleichung von HRID 1175995
FC(F)(F)C(O)=O.[N:8]1([C:12]([C:14]2[N:15]=[CH:16][C:17]([O:20][C:21]3[CH:22]=[C:23]([C:35]([NH:37][C:38]4[CH:42]=[CH:41][N:40](C(OC(C)(C)C)=O)[N:39]=4)=[O:36])[CH:24]=[C:25]([O:27][C@@H:28]([CH3:34])[CH2:29][O:30][CH:31]([F:33])[F:32])[CH:26]=3)=[N:18][CH:19]=2)=[O:13])[CH2:11][CH2:10][CH2:9]1>C(Cl)Cl>[N:8]1([C:12]([C:14]2[N:15]=[CH:16][C:17]([O:20][C:21]3[CH:22]=[C:23]([CH:24]=[C:25]([O:27][C@@H:28]([CH3:34])[CH2:29][O:30][CH:31]([F:33])[F:32])[CH:26]=3)[C:35]([NH:37][C:38]3[CH:42]=[CH:41][NH:40][N:39]=3)=[O:36])=[N:18][CH:19]=2)=[O:13])[CH2:9][CH2:10][CH2:11]1

Komponenten

4

Edukt 2

HCID 6422Trifluoroacetic acidHCID 591271291,1-dimethylethyl 3-({[3-{[5-(azetidin-1-ylcarbonyl)pyrazin-2-yl]oxy}-5-({(1S)-2-[(difluoromethyl)oxy]-1-methylethyl}oxy)phenyl]carbonyl}amino)-1H-pyrazole-1-carboxylate

Produkt 1

HCID 178461788HCID 178461788, VerbindungAusbeute 112 %

Reagenzien, Katalysatoren, Lösungsmittel 1

HCID 6344DichloromethaneLösungsmittel

Versuchsvorschrift

Trifluoroacetic acid (2 mL) was added to a solution of 1,1-dimethylethyl 3-({[3-{[5-(azetidin-1-ylcarbonyl)pyrazin-2-yl]oxy}-5-({(1S)-2-[(difluoromethyl)oxy]-1-methylethyl}oxy)phenyl]carbonyl}amino)-1H-pyrazole-1-carboxylate (115 mg, 0.17 mmol) in DCM (16 mL) and stirred at RT for 2 hours. The solvent was removed in vacuo, DCM (20 mL) added and the mixture washed with water (20 mL), a saturated solution of sodium bicarbonate (20 mL), brine (20 mL), dried (MgSO4), filtered and reduced in vacuo to give the desired compound as a white foam (93 mg).

Aufarbeitung

  1. customThe solvent was removed in vacuo, DCM (20 mL)
  2. additionadded
  3. washthe mixture washed with water (20 mL)
  4. dry with materiala saturated solution of sodium bicarbonate (20 mL), brine (20 mL), dried (MgSO4)
  5. filtrationfiltered

Quellen und Nachweise

ORD-Eintrag
ord-962736c5c4e542e8a83fe5ce4a65670f
Quelldatensatz
uspto-grants-2010_11
Patentnummer
US07842694B2

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