An Improved Synthesis of Telmisartan: An Antihypertensive Drug

Research Article

Srinivas Ambati, Hanumantha Ra

Abstract

An improved synthesis of the angiotensin II receptor antagonist telmisartan is described. It involves Suzuki coupling of 4-formylphenylboronic acid with 2-(2-bromophenyl)-4,4-dimethyl-2- oxazoline followed by construction of benzimidazole moiety regioselectively though a reductive amination-condensation sequence, replacing the earlier alkylation of the preformed benzimidazole route. This methodology overcomes many drawbacks of the reported syntheses.

Relevant Publications in Der Chemica Sinica