Teva Pharmaceutical Industries Limited

Julia Kaftanov

Gennady Nisnevich

Igor Rukhman

Ben-Zion Dolitzky

Boris Pertsikov

Shlomit Wizel

Ben Zion Dolitzky

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.

Synthesis of irbesartan

This invention relates to novel amorphous losartan potassium, novel losartan potassium in a crystalline form that is a hydrate, novel crystalline losartan potassium Form IV and solvates thereof, novel crystalline losartan potassium Form V and solvates thereof, to processes for their preparation, to compositions containing them and to their use in medicine. This invention further relates to a novel process for preparing crystalline losartan potassium Form I and Form II.

Amorphous and crystalline forms of losartan potassium and process for their preparation

Provided is a novel method of making 2-butyl-3-[[2'(1-trityl-1H-tetrazol-5-yl)biphen-4-yl]methyl]-1,3-diazaspiro[4.4]non-1-ene-4-one, which can be converted to irbesartan. Also provided are methods of making irbesartan.

Synthesis of 2-butyl-3-(1-trityl-1H-tetrazol-5-YL)biphenyl-4-YL)-1,3-diazaspiro[4,4]- non-ene-4-one

Intermediates for the synthesis of irbesartan

Synthesis of 2-butyl-3-(2'-(1-trityl-1H-tetrazol-5-yl)biphenyl-4-yl)-1,3-diazaspiro[4.4]-non-ene-4-one

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Haifa, Israel

Julia Kaftanov