Reaktion #10424

Reaktionsgleichung

3-amino-1-cyclopropyl-6,7-difluoro-1H-quinazoline-2,4-dione

triethylamine

(S)-pyrrolidin-3-yl carbamic acid tert-butyl ester

→

title compound

Ausbeute 88.2%

3-Amino-7-[(S)-3-(tert-butoxycarbonylamino)pyrrolidin-1-yl]-1-cyclopropyl-6-fluoro-1H-quinazoline-2,4-dione

Ausbeute 88.2%

Lösungsmittel

acetonitrile

Reaktionsbedingungen

Aufarbeitung

1. 1
   TemperaturThe solution is refluxed for 18 hours
2. 2
   Sonstigethe solvent is removed under reduced pressure
3. 3
   Sonstigethe residue triturated with water
4. 4
   FiltrationThe solid is collected by filtration and air
5. 5
   Sonstigedried

Vorschrift

To a solution of 3-amino-1-cyclopropyl-6,7-difluoro-1H-quinazoline-2,4-dione (Example 24a) (50.0 mg, 0.20 mmol) and triethylamine (74 mg, 0.74 mmol) in acetonitrile (3 mL) is added (S)-pyrrolidin-3-yl carbamic acid tert-butyl ester (74 mg, 0.40 mmol). The solution is refluxed for 18 hours, the solvent is removed under reduced pressure, and the residue triturated with water. The solid is collected by filtration and air dried to afford 74 mg of the title compound. MS CI: m/z 420 (MH+).

Quelle