Alternative Synthesis of Telmisartan via Suzuki Coupling 

By A.Sanjeev Kumar, Samir Ghosh and G. N. Mehta 

ABSTRACT

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. 

Keywords: Telmisartan, antihypertensive drug, Suzuki coupling, oxazoline hydrolysis.

Click here to download the complete article in PDF Format