An alternative synthesis of telmisartan one of the most important agents used in antihypertensive therapy is reported. Metalation of 4-bromo toluene provides the key boronic acid ester intermediate 14 for palladium catalysed biaryl coupling with 2-(2-bromophenyl)-4,4-dimethyl-2- oxazoline 16 via Suzuki coupling. The hydrolysis of oxazoline in telmisartan was realized in a convenient and economical manner, which is more suitable for industrial production. This methodology overcomes many of drawbacks associated with previously reported syntheses.
