2-BroMo-3-(trifluoroMethyl)phenol synthesis

Yield:1214323-39-3 3%

Reaction Conditions:

with bromine in dichloromethane at 20; for 18 h;

Steps:

TA

The appropriate phenol (1 eq.) was dissolved in dichloromethane and cooled a 0°C. Bromine (1 eq.) in dichloromethane was added. The reaction mixture was allowed to reach room temperature and kept under stirring for 18 hours. The reaction mixture was washed with aqueous Na₂S0₃, brine, dried over MgS0₄, filtered and evaporated. The residue was purified by chromatography on silica gel to provide the desired bromophenols with yields ranging from 3 to 76%.Bromination of 3-trifluoromethylphenol gave a mixture of isomers. Separation on silica gel afforded 2-bromo-3-trifluoromethylphenol, intermediate of Cpd.4-44 and 2-bromo-5- trifluoromethylphenol, intermediate of Cpd.4-73.This protocol was also used to prepare intermediates of Cpd.4-68, and Cpd.4-70.

References:

WO2013/45519,2013,A1 Location in patent:Page/Page column 52-53; 69