Reaktion #627378

Reaktionsgleichung

2,4-dichloro-6-methylquinazoline

oxetane-3,3-diyldimethanamine

triethylamine

→

desired product

Ausbeute 43.4%

N-{[3-(Aminomethyl)oxetan-3-yl]methyl}-2-chloro-6-methylquinazolin-4-amine

Ausbeute 43.4%

Lösungsmittel

dichloromethane

dichloromethane

water

Reaktionsbedingungen

Aufarbeitung

1. 1
   Extraktionextracted with dichloromethane
2. 2
   WaschenThe organic layer was washed with brine
3. 3
   Trocknendried over anhydrous sodium sulfate
4. 4
   Einengenconcentrated in vacuo
5. 5
   SonstigeThe residue was purified by flash column chromatography (eluting with 10% methanol in dichloromethane)

Vorschrift

To a mixture of oxetane-3,3-diyldimethanamine (1.16 g, 10.0 mmol) and triethylamine (1.4 mL, 10 mol) in dichloromethane (15 mL) was added dropwise of a solution of 2,4-dichloro-6-methylquinazoline (500 mg, 2.36 mmol) in dichloromethane (5 mL). After being stirred at room temperature overnight, the resulting mixture was diluted with water (50 mL), and extracted with dichloromethane. The organic layer was washed with brine, dried over anhydrous sodium sulfate, and concentrated in vacuo. The residue was purified by flash column chromatography (eluting with 10% methanol in dichloromethane) to afford 300 mg of the desired product as a white solid.

Quelle