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1. (WO2007010558) A PROCESS FOR THE PREPARATION OF TELMISARTAN
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2007/010558 International Application No.: PCT/IN2006/000257
Publication Date: 25.01.2007 International Filing Date: 19.07.2006
IPC:
C07D 403/04 (2006.01) ,C07D 235/20 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
403
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
02
containing two hetero rings
04
directly linked by a ring-member-to-ring- member bond
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
235
Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
02
condensed with carbocyclic rings or ring systems
04
Benzimidazoles; Hydrogenated benzimidazoles
20
Two benzimidazolyl-2 radicals linked together directly or via a hydrocarbon or substituted hydrocarbon radical
Applicants:
MATRIX LABORATORIES LIMITED [IN/IN]; 1-1-151/1,IV Floor Sairam Towers, Alexander Road Secunderabad, 500 003, IN (AllExceptUS)
CHAVA, Satyanarayana [IN/IN]; IN (UsOnly)
GORANTLA, Seeta, Ramanjaneyulu [IN/IN]; IN (UsOnly)
GINJUPALLI, Sai, Prasanna, Bhagya, Lakshmi [IN/IN]; IN (UsOnly)
Inventors:
CHAVA, Satyanarayana; IN
GORANTLA, Seeta, Ramanjaneyulu; IN
GINJUPALLI, Sai, Prasanna, Bhagya, Lakshmi; IN
Agent:
RAO, Ramana, V.; Matrix Laboratories Ltd Plot No. 38, Phase-IV IDA, Jeedimetla Hyderabad 500 055, IN
Priority Data:
957/CHE/200519.07.2005IN
Title (EN) A PROCESS FOR THE PREPARATION OF TELMISARTAN
(FR) PROCEDE DE PREPARATION DU TELMISARTAN
Abstract:
(EN) The present invention encompasses a method for the preparation of Telmisartan comprises, through Telmisartan dihydrochloride comprises i) Condensing 4-Methyl-2-n-propyl-lH- benzimidazole-6-carboxylic acid with N-Methyl-O-phenylenediamine dihydrochloride to yields 4-methyl-6 (1 -methyl benzimidazol-2-yl)-2-n-propyl lH-benzimidazole ii) Treating 4- methyl-6-(l -methyl benzimidazol-2-yl)-2-n-propyl-lH-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.
(FR) La présente invention concerne un procédé de préparation du telmisartan qui consiste à, au moyen d'un dihydrochlorure de telmisartan, i) condenser l'acide 4-méthyl-2-n-propyl-1H- benzimidazole-6-carboxylique avec un dihydrochlorure de N-méthyl-O-phénylènediamine pour produire 4-méthyl-6(1-méthyl benzimidazol-2-yl)-2-n-propyl 1H-benzimidazole; ii) traiter 4-méthyl-6-(1-méthyl benzimidazol-2-yl)-2-n-propyl-1H-benzimidazole avec 4`- (bromométhyl)-2-biphényl-2-carboxylate en présence d'une base dans un solvant organique et isoler l'ester sous forme d'un sel d'addition acide; iii) convertir le sel d'addition d'acide ester en dihydrochlorure de telmisartan et iv) convertir le dihydrochlorure de telmisartan en telmisartan.
Designated States: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BW, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LV, LY, MA, MD, MG, MK, MN, MW, MX, MZ, NA, NG, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RS, RU, SC, SD, SE, SG, SK, SL, SM, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HU, IE, IS, IT, LT, LU, LV, MC, NL, PL, PT, RO, SE, SI, SK, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)
Also published as:
EP1912975US20090023932