Efficient and improved synthesis of Telmisartan
Keyword(s):
An efficient synthesis of the angiotensin II receptor antagonist Telmisartan (1) is presented involving a cross coupling of 4-formylphenylboronic acid 10 with 2-(2-bromophenyl)-4,4-dimethyl-2-oxazoline (11) as the key step (90% yield). The benzimidazole moiety 15 was constructed regioselectively via a reductive amination-condensation sequence, replacing the alkylation of the preformed benzimidazole step in the previously published route. This methodology overcomes many of drawbacks associated with previously reported syntheses.
2010 ◽
Vol 24
(9)
◽
pp. 749-758
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A highly efficient synthesis of RWJ 47639: a novel orally active angiotensin II receptor antagonist.
1993 ◽
Vol 3
(8)
◽
pp. 1523-1526
◽
1994 ◽
Vol 59
(21)
◽
pp. 6391-6394
◽
1998 ◽
Vol 31
(2)
◽
pp. 33A