Process for the Preparation of Telmisartan
AssigneeMatrix Laboratories Limited
InventorsSatyanarayana Chava, Seeta Ramanjaneyulu Gorantla, Sai Prasanna Ginjupalli
Life of this patent
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Abstract
The present invention encompasses a method for the preparation of Telmisartan comprises, through Telmisartan dihydrochloride comprises i) Condensing 4-Methyl-2-n-propyl-1H-benzimidazole-6-carboxylic acid with N-Methyl-O-phenylenediamine dihydrochloride to yields 4-methyl-6 (1-methyl benzimidazol-2-yl)-2-n-propyl 1H-benzimidazole ii) Treating 4-methyl-6-(1-methylbenzimidazol-2-yl)-2-n-propyl-1H-benzimidazole with 4′-(bromomethyl)-2-biphenyl-2-carboxylate in presence of a base in an organic solvent and isolating the ester as acid addition salt iii) Converting ester acid addition salt to Telmisartan dihydrochloride and iv) Converting Telmisartan dihydrochloride to Telmisartan.
Claims10
A process for the preparation of Telmisartan comprising steps
- Condensing 4-Methyl-2-n-propyl-11H-benzimidazole-6-carboxylic acid with N-Methyl-O-phenylenediamine dihydrochloride in the presence of polyphosphoric acid (PPA) yields 4-methyl-6 (1-methyl benzimidazol-2-yl)-2-n-propyl 1H-benzimidazole
- Treating 4-methyl-6-(1-methyl benzimidazol-2-yl)-2-n-propyl-1H-benzimidazole with 4′-(bromomethyl)-2-biphenyl-2-carboxylate in presence of a base in an organic solvent followed by treatment with mineral acid yields acid addition salt of 4′-[4-Methyl-6-(1-methyl-1H-benzimidazol-2-yl)-2-n-propyl-1H-benzimidazol-1-yl-methyl]biphenyl-2-carboxylate ester
- Treating 4′-[4-Methyl-6-(1-methyl-1H-benzimidazol-2-yl)-2-n-propyl-1H-benzimidazol-1-yl-methyl]biphenyl-2-carboxylate ester acid addition salt with aqueous hydrochloric acid yields Telmisartan dihydrochloride
- Converting Telmisartan dihydrochloride to Telmisartan
4′-[4-Methyl-6-(1-methyl-1H-benzimidazol-2-yl)-2-n-propyl-1H-benzimidazol-1-yl-methyl]biphenyl-2-carboxylate ester acid addition salts
Telmisartan dihydrochloride
Dependencies are inferred from the claim text.