Phosphorus oxychloride → Ethyl 4-chloro-6-methoxyquinazoline-2-carboxylate
Reaction equation
[CH2:1]([O:3][C:4]([C:6]1[NH:15][C:14](=O)[C:13]2[C:8](=[CH:9][CH:10]=[C:11]([O:17][CH3:18])[CH:12]=2)[N:7]=1)=[O:5])[CH3:2].O=P(Cl)(Cl)[Cl:21]>>[CH2:1]([O:3][C:4]([C:6]1[N:15]=[C:14]([Cl:21])[C:13]2[C:8](=[CH:9][CH:10]=[C:11]([O:17][CH3:18])[CH:12]=2)[N:7]=1)=[O:5])[CH3:2]Participants
3
Conditions
- Temperature
- 100 °C
Procedure
To 6-methoxy-4-oxo-3,4-dihydro-quinazoline-2-carboxylic acid ethyl ester (1.38 g, 5.438 mmol) was added POCl3 (25 mL) and the solution was heated at 100° C. for 1.5 h. The solution was concentrated under reduced pressure and the residue was dissolved in EtOAc and washed with water, brine, dried (Na2SO4) and concentrated under reduced pressure to give 1.22 g of 4-chloro-6-methoxy-quinazoline-2-carboxylic acid ethyl ester.
Workup
- concentrationThe solution was concentrated under reduced pressure