Trifluoroacetic acid → 6-fluoro-1-(piperidin-4-yl)-1H-indazole

HRID 512863Notizen

Reaktionsgleichung

Reaktionsgleichung von HRID 512863
[F:1][C:2]1[CH:10]=[C:9]2[C:5]([CH:6]=[N:7][N:8]2[CH:11]2[CH2:16][CH2:15][N:14](C(OC(C)(C)C)=O)[CH2:13][CH2:12]2)=[CH:4][CH:3]=1.C(O)(C(F)(F)F)=O>C(Cl)Cl>[F:1][C:2]1[CH:10]=[C:9]2[C:5]([CH:6]=[N:7][N:8]2[CH:11]2[CH2:16][CH2:15][NH:14][CH2:13][CH2:12]2)=[CH:4][CH:3]=1

Komponenten

4

Edukt 2

HCID 6422Trifluoroacetic acidHCID 89614504tert-butyl 4-(6-fluoro-1H-indazol-1-yl)piperidine-1-carboxylate

Produkt 1

HCID 539239646-fluoro-1-(piperidin-4-yl)-1H-indazole

Reagenzien, Katalysatoren, Lösungsmittel 1

HCID 6344DichloromethaneLösungsmittel

Versuchsvorschrift

To tert-butyl 4-(6-fluoro-1H-indazol-1-yl)piperidine-1-carboxylate prepared as in STEP 1 above (998 mg, 3.10 mmol) in DCM (20 mL) at 0° C. was added TFA (10 mL). The resulting mixture was then stirred for 1 hour. The solvent was removed in vacuo. To the resulting residue was added 0.5N NaOH (15 mL), followed repeated extraction with CHCl3. The organic layer was dried with MgSO4 and filtered to yield 6-fluoro-1-(piperidin-4-yl)-1H-indazole.

Aufarbeitung

  1. customThe solvent was removed in vacuo
  2. additionTo the resulting residue was added 0.5N NaOH (15 mL)
  3. extractionextraction with CHCl3
  4. dry with materialThe organic layer was dried with MgSO4
  5. filtrationfiltered

Quellen und Nachweise

ORD-Eintrag
ord-05a761273e034f1fb71ef13db4eae075
Quelldatensatz
uspto-grants-2015_08
Patentnummer
US09102669B2

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