Reaktion #88906

Reaktionsgleichung

5-(5-amino-3-tert-butyl-pyrazol-1-yl)-2-chloro-phenol

morpholino ethanol

Ph3P

DEAD

→

title compound

Ausbeute 80.0%

5-tert-Butyl-2-[4-chloro-3-(2-morpholin-4-yl-ethoxy)-phenyl]-2H-pyrazol-3-ylamine

Ausbeute 80.0%

Lösungsmittel

water

THF

Reaktionsbedingungen

Aufarbeitung

1. 1
   Extraktionextracted with DCM
2. 2
   SonstigeThe combined organics were dried
3. 3
   Einengenconcentrated in vacuo
4. 4
   SonstigeThe residue was purified by FCC

Vorschrift

To a stirred solution of 5-(5-amino-3-tert-butyl-pyrazol-1-yl)-2-chloro-phenol (WO2007/091152, which is incorporated herein by reference; 200 mg, 0.75 mmol), 2-N morpholino ethanol (137 μL, 1.13 mmol) and Ph3P (394 mg, 1.50 mmol) in THF (7.5 mL) at 0° C. was added DEAD (236 μL, 1.50 mmol). After 1 h, the reaction mixture was diluted with water and extracted with DCM. The combined organics were dried and concentrated in vacuo. The residue was purified by FCC, using 0-5% [2M NH3 in MeOH] in DCM, to give the title compound (228 mg, 80%). LCMS (Method 3): Rt 2.28 min, m/z 379 [MH+].

Quelle