2-BROMO-4-CHLORO-1-(DIFLUOROMETHYL)BENZENE synthesis

Yield:1261476-50-9 80%

Reaction Conditions:

with diethylamino-sulfur trifluoride in dichloromethane at 0 - 20;

Steps:

19

To a solution of 2-bromo-4-chlorobenzaldehyde (1 g, 4.56 mmol) in DCM (15 mL) was added DAST (0.903 mL, 6.83 mmol) at 0 °C. The reaction was allowed to warm to rt and stir overnight. The reaction mixture was diluted with EtOAc, washed with sat NaHCC^ and brine. The organic phase was dried over magnesium sulfate, filtered and concentrated to give Intermediate 19A (0.88g. 80% yield) as a clear oil. MS (ESI) m/z: 261.2 (M+Na)+.

References:

WO2011/100401,2011,A1 Location in patent:Page/Page column 146