A highly efficient, convergent approach to the synthesis of the angiotensin II receptor antagonist losartan (1) is described. Directed ortho-metalation of 2-trityl-5-phenyltetrazole provides the key boronic acid intermediate 10 for palladium-catalyzed biaryl coupling with bromide 5 obtained from the regioselective alkylation of the chloroimidazole 2. This methodology overcomes many of the drawbacks associated with previously reported syntheses.
|Original language||English (US)|
|Number of pages||4|
|Journal||Journal of Organic Chemistry|
|State||Published - Oct 1 1994|
All Science Journal Classification (ASJC) codes
- Organic Chemistry