Reaktion #610241

Reaktionsgleichung

Cs2CO3

3-chloro-6-(1H-pyrazol-4-yl)isoquinoline

3,6-dioxabicyclo[3.1.0]hexane

→

title compound

Ausbeute 46.0%

4-(4-(3-Chloroisoquinolin-6-yl)-1H-pyrazol-1-yl)tetrahydrofuran-3-ol

Ausbeute 46.0%

Lösungsmittel

DMF

Reaktionsbedingungen

Aufarbeitung

1. 1
   TemperaturThe reaction was cooled
2. 2
   Einengenconcentrated in vacuo
3. 3
   Sonstigepurified
4. 4
   Wascheneluting with 50-75% EtOAc/cyclohexane

Vorschrift

A mixture of Cs2CO3 (34 mg, 0.105 mmol), 3-chloro-6-(1H-pyrazol-4-yl)isoquinoline (16 mg, 0.070 mmol) and 3,6-dioxabicyclo[3.1.0]hexane (Preparation 37, 24 mg, 0.279 mmol) in DMF (3 mL) was stirred at 120° C. under microwave irradiation for 60 minutes. The reaction was cooled, concentrated in vacuo and purified using Biotage silica gel column chromatography eluting with 50-75% EtOAc/cyclohexane to give the title compound as white solid (10 mg, 46%).

Quelle