2,4-Dichloro-6-(4-fluorophenyl)quinazoline synthesis

Yield:-

Reaction Conditions:

with N-ethyl-N,N-diisopropylamine;trichlorophosphate for 16 h;Heating / reflux;

Steps:

53
2,4-Dichloro-6-(4-fluorophenyl)-quinazoline:; A mixture of 6-(4-Fluoro-phenyl)-quinazoline-2,4-diol (760 mg, 2.95 mmol), POCI₃ (20 ml) and N,N-di-isopropyl ethyl amine (DIEA, 2 ml) was heated to reflux for 16 hours. The POCI₃ was removed by concentration under reduced pressure and the residue was dissolved in EtOAc. The organic solution was extracted with brine three times, then dried over sodium sulfate and concentrated to provide crude product (700 mg), which used without further purification.

References:

GILEAD SCIENCES, INC. WO2008/9078, 2008, A2 Location in patent:Page/Page column 80