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US 2006/0135780 A1Published application
Novel synthesis of irbesartan
AssigneeTeva Pharmaceutical Industries Ltd.
InventorsGennady Nisnevich, Igor Rukhman, Boris Pertsikov, Julia Kaftanov, Ben-Zion Dolitzky
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Abstract
Provided are a method of making irbesartan via a Suzuki coupling reaction and a novel intermediate, 2-butyl-3-(4′-bromobenzyl)-1,3-diazaspiro[4.4]non-1-ene-4-one, for such process. The novel process includes the step of reacting such intermediate with a protected imidazolephenylboronic acid.
Claims3
A process of making 2-(1-trityl-1H-tetrazol-5-yl)phenylboronic acid comprising the steps of:
- a) combining 5-phenyl-1H-tetrazole with chlorotriphenylmethane in the presence of a solvent and a first base;
- b) combining the product of step a with a borate, in the presence of a solvent and a second base;
- and
- c) recovering 2-(5-tetrazoyl)phenylboronic acid.
1 more element
Dependencies are inferred from the claim text.