p-Toluenesulfonic acid → 6-Bromo-2-(4-(trifluoromethyl)phenyl)benzo[d]oxazole

Participants

Reaction Conditions

Reaction Steps

Intermediate 53 (940 mg, 2.6 mmol) was dissolved in xylene (25 ml) and added p-Toluenesulphonic acid (991 mg, 5.22 mmol). This mixture was refluxed to 160° C. for 12 h under a dean-stork condenser. Xylene removed from the reaction mixture and basified the residue with aq. NaHCO3 (30 ml). Work up (EtOAc/H2O) followed by purification with combiflash using a gradient mixture of EtOAc and Petether (5:95) as eluent to afford the titled compound (650 mg) as an Off-White solid.

Provenance & Evidence