Reaktion #1491798

Reaktionsgleichung

tert-butyl 4-[4-(1-{[(E)-(2,6-dichloro-3-fluorophenyl)methylidene]amino}-1H-pyrrolo[3,2-b]pyridin-6-yl)-1H-pyrazol-1-yl]piperidine-1-carboxylate

HCl

→

desired intermediate

Ausbeute 53.0%

N-[(E)-(2,6-dichloro-3-fluorophenyl)methylidene]-6-[1-(piperidin-4-yl)-1H-pyrazol-4-yl]-1H-pyrrolo[3,2-b]pyridin-1-amine

Ausbeute 53.0%

Lösungsmittel

MeOH

Reaktionsbedingungen

Aufarbeitung

1. 1
   SonstigeSolvents were removed
2. 2
   workup.ADDITIONthe residue was treated with aqueous NaHCO3
3. 3
   Extraktionextracted with ethyl acetate
4. 4
   SonstigeThe organic layer was dried
5. 5
   Sonstigeevaporated

Vorschrift

A solution of tert-butyl 4-[4-(1-{[(E)-(2,6-dichloro-3-fluorophenyl)methylidene]amino}-1H-pyrrolo[3,2-b]pyridin-6-yl)-1H-pyrazol-1-yl]piperidine-1-carboxylate (15 mg, 0.027 mmol) in MeOH (0.5 mL) was treated with HCl (4.0M solution in dioxane, 2.0 mL) at room temperature for 2 h. Solvents were removed and the residue was treated with aqueous NaHCO3, and extracted with ethyl acetate. The organic layer was dried, evaporated to afford the desired intermediate as a yellowish solid (6.5 mg, yield 53%).

Quelle