cas 144701-48-4, Telmisartan | Articles data

Articles about 144701-48-4Total 56 be found

Article title
Article abstract
Author
Journal number and time
Download

Improved one-pot synthesis of telmisartan
Cost-effective and improved one-pot synthesis for telmisartan (1) is described that minimizes the reaction time and gives high-purity material. Copyright Taylor & Francis Group, LLC.
Rao, Challa Nageswar,Naresh, Tondepu,Satyanarayana, Komati,Reddy, Bojja Ramachandra,Reddy, Ghanta Mahesh
p. 530 - 534
(2010)
Read Online

An improved synthesis of telmisartan: Via the copper-catalyzed cyclization of o -haloarylamidines
A concise synthetic route was designed for making telmisartan. The key bis-benzimidazole structure was constructed via the copper-catalyzed cyclization of o-haloarylamidines. By adopting this approach, telmisartan was obtained in a 7-step overall yield of 54% starting from commercially available 3-methyl-4-nitrobenzoic acid, and the use of HNO3/H2SO4 for nitration and polyphosphoric acid (PPA) for cyclization in the reported literatures were avoided.
Li, Rui,Shen, Jingshan,Sun, Changliang,Zhang, Junchi,Zhu, Fuqiang
p. 13717 - 13721
(2020)
Read Online

A convergent approach to the total synthesis of telmisartan via a Suzuki cross-coupling reaction between two functionalized benzimidazoles
A direct and efficient total synthesis has been developed for telmisartan, a widely prescribed treatment for hypertension. This approach brings together two functionalized benzimidazoles using a high-yielding Suzuki reaction that can be catalyzed by either a homogeneous palladium source or graphene-supported palladium nanoparticles. The ability to perform the cross-coupling reaction was facilitated by the regio-controlled preparation of the 2-bromo-1-methylbenzimidazole precursor. This convergent approach provides telmisartan in an overall yield of 72% while circumventing many issues associated with previously reported processes.
Martin, Alex D.,Siamaki, Ali R.,Belecki, Katherine,Gupton, B. Frank
p. 1915 - 1919
(2015)
Read Online

Preparation method of telmisartan
The invention relates to a preparation method of telmisartan. According to the preparation method, 3-methyl-4-n-butylamide benzoic acid is used as a raw material, an intermediate (1) is prepared through cyaniding, nitration, reduction, ring closing and other reactions, the intermediate (1) and 4 '-bromomethyl biphenyl-2-methyl formate are subjected to condensation to generate an intermediate (2), the intermediate (2) and N-methyl o-phenylenediamine are subjected to condensation to prepare an intermediate (3), and finally the telmisartan is prepared through hydrolysis. The invention develops a new preparation method of telmisartan. The raw material 3-methyl-4-n-butyrylamide benzoic acid adopted by the method is easy to obtain and low in price; the method is mild in reaction condition, easy to operate and high in yield, the cyanation reaction avoids the use of toxic cyanide, the environmental pollution is small, and the method is suitable for industrial production.
-
(2021/08/28)

MANUFACTURING METHOD OF BIPHENYL-2-CARBOXYLIC ACID METHYL ESTER
PROBLEM TO BE SOLVED: To provide a manufacturing method of 4'-{[4-methyl-6-(1-methyl-1H-benzimidazole-2-yl)-2-propyl-1H-benzimidazole-1-yl]methyl}biphenyl-2-carboxylic acid methyl ester, capable of improving yield and quality, and enhancing efficiency of workability in an industrial scale. SOLUTION: There is provided a manufacturing method of 4'-{[4-methyl-6-(1-methyl-1H-benzimidazole-2-yl)-2-propyl-1H-benzimidazole-1-yl]methyl}biphenyl-2-carboxylic acid methyl ester by adding water to a reaction mixture containing an organic polar solvent and 4'-{[4-methyl-6-(1-methyl-1H-benzimidazole-2-yl)-2-propyl-1H-benzimidazole-1-yl]methyl}biphenyl-2-carboxylic acid methyl ester generated by mixing a mixture obtained by adding 2-n-propyl-4-methyl-6-(1'-methylbenzimidazole-2-yl)benzimidazole and a base to an organic polar solvent, and 4'-bromomethyl biphenyl-2-carboxylic acid methyl ester, to crystallize the methyl ester. SELECTED DRAWING: None COPYRIGHT: (C)2019,JPOandINPIT
-
Paragraph 0071-0076

(2019/12/25)

Preparation method of telmisartan
The invention discloses a preparation method of telmisartan. A compound 2 and a compound 3 are subjected to Suzuki coupling reaction so as to obtain the target product telmisartan. The method has moderate reaction conditions, the product cost is reduced, the yield can achieve 90 percent, and the preparation method has an industrialized enlargement potential.
-
Paragraph 0020; 0021; 0022; 0023; 0024; 0025-0028

(2018/03/01)

Solid dispersions comprising Telmisartan and the preparation method thereof
The solid dispersions comprising telmisartan and a manufacturing method thereof, according to the present invention, unlike conventional methods requiring a low yield, can manufacture telmisartan of a high yield through simple and short steps by using a relatively inexpensive raw material, can secure excellent quality through reduction of generation of decomposition products, and can manufacture the solid dispersions on a mass production basis to be commercially available. Therefore, the solid dispersions of novel crystalline polymorph of the telmisartan of the present invention has improved storage stability and solubility, and can be synthesized at a high yield, thereby being expected to be very useful in the manufacture of pharmaceuticals.COPYRIGHT KIPO 2018
-
Paragraph 0111; 0114; 0118

(2018/05/15)

4 ′ - [[2 a-n - (1 - methylbenzimidazole -2 - yl) - benzimidazole -1 - yl methyl propyl -4 - -6 -] - methyl] - biphenyl carboxylic acid ammonium salt crystals -2 - (by machine translation)
PROBLEM TO BE SOLVED: To provide a method for obtaining 4'-[[2-n-propyl-4-methyl-6-(1-methylbenzimidazole-2-yl)-benzimidazole-1-yl]-methyl]-biphenyl-2-carboxylic acid with high purity.SOLUTION: A method for purifying a compound of formula (1) below includes: a dissolution process of dissolving a crude substance of 4'-[[2-n-propyl-4-methyl-6-(1-methylbenzimidazol-2-yl)-benzimidazole-1-yl]-methyl]-biphenyl-2-carboxylic acid in a mixed solvent of water and a 2-12C alcohol by adding 2.0 to 30.0 mol of ammonia per mol of a composition of formula (1) below; a crystallization process of depositing an ammonium salt of the composition of formula (1) below by discharging ammonia from the solvent obtained in the process; and a process of separating and drying the ammonium salt.
-
Paragraph 0064-0067

(2017/06/23)

A synthetic method of telmisartan
The invention discloses a novel synthesis method of telmisartan. The method comprises the following steps: 2-n-propyl-4-methyl-6-(1-methyl-benzimidazole-2-base)-benzimidazole serving as a raw material is subjected to a substitution reaction with p-aminobenzyl bromide, then is subjected to a diazo-reaction, and finally is subjected to a condensation reaction with 2-sodium carboxybenzeneboronic acid under a palladium acetate catalytic system and the combined action of methyltetrahydrofuran/potassium carbonate/triphenylphosphine, so that telmisartan is produced. A synthetic route is brand new, has high innovativeness, is low in raw material price, mild in reaction conditions and small in environment pollution, and has great industrialized application prospect.
-
(2017/10/25)

Method for preparing telmisartan and intermediates thereof
Disclosed is a telmisartan preparation method, characterized in that: 2-n-propyl-4-methyl-6-(1-methyl benzimidazole-2-yl) benzimidazole (compound I) and 4'-halomethyl diphenyl-2-substituted compound (compound II) conduct a nucleophilic substitution reaction to obtain a compound III; when R is COOH, the compound III is telmisartan; and when R is COOR' or CN, the compound III can be hydrolyzed to obtain telmisartan.
-
Paragraph 0108-0109; 0111

(2017/08/31)

Preparation of crystalline telmisartan A reduced acetate
PROBLEM TO BE SOLVED: To provide a method of easily reducing acetic acid contained in an A-type crystal of 4'-[[2-n-propyl-4-methyl-6-(1-methylbenzimidazole-2-yl)-benzimidazole-1-yl]-methyl]-biphenyl-2-carboxylic acid useful as a hypotensive agent.SOLUTION: There is provided a method of manufacturing an A-type crystal of 4'-[[2-n-propyl-4-methyl-6-(1-methylbenzimidazole-2-yl)-benzimidazole-1-yl]-methyl]-biphenyl-2-carboxylic acid having the content of acetic acid of less than 0.05 mass% including a process of mixing the A-type crystal of 4'-[[2-n-propyl-4-methyl-6-(1-methylbenzimidazole-2-yl)-benzimidazole-1-yl]-methyl]-biphenyl-2-carboxylic acid containing 0.05 to 10 mass% of acetic acid and a specific amount of a mixture of methanol and water.
-
Paragraph 0040; 0041; 0043; 0044

(2017/11/07)

METHOD FOR PRODUCING AMMONIUM SALT OF TELMISARTAN
PROBLEM TO BE SOLVED: To provide a method for producing an ammonium salt of telmisartan effective as a hypotensive agent with high purity. SOLUTION: The method for producing an ammonium salt of telmisartan comprises a dissolution step of dissolving a crude body of telmisartan by adding, in a mixed solvent of water, a 2-12C alcohol and ethyl acetate, ammonia in an amount of 2.0 to 30.0 mol based on 1 mol of the telmisartan at 0 to 30°C to form an ammonium salt of telmisartan and a crystallization step of depositing the ammonium salt of telmisartan from the solution produced in the dissolution step at 0 to 30°C and achieves reduction of specific impurities C and D. SELECTED DRAWING: None COPYRIGHT: (C)2016,JPOandINPIT
-
Paragraph 0052

(2017/02/23)

A CONVERGENT APPROACH TO THE TOTAL SYNTHESIS OF TELMISARTAN VIA A SUZUKI CROSS-COUPLING REACTION
Methods of synthesizing the angiotensin II receptor antagonist telmisartan in high yield and purity are provided. The methods involve the coupling of two structurally distinct benzimidazole units via a Suzuki cross-coupling reaction. Methods of regioselectively synthesizing one of the benzimidazole units are also provided.
-
(2016/06/28)

A Novel Method for Preparing of Telmisartan
The present invention relates to a method for preparing telmisartan used as an angiotensin-II receptor blocker (ARB)-based hypertension medicine and telmisartan prepared by the method. According to the method of the present invention, a condensation reaction for obtaining an intermediate during a telmisartan preparing procedure is conducted in a solvent containing an ionic liquid, thereby significantly shortening the reaction time by 1-2 hours compared with the conventional method; and a hydrolysis reaction of the intermediate for preparing telmisartan is conducted by controlling the ratio of water containing a hydroxyl group, thereby significantly improving filtering efficiency, the process rate, and process convenience and obtaining high-purity and high-yield telmisartan without further purification.
-
Paragraph 0069-0073

(2017/02/23)

ONE POT PROCESS FOR THE PREPARATION OF TELMISARTAN
A process for the preparation of bromine free telmisartan in one pot starting from 2-cyano-4′-methyl biphenyl. The process uses raw materials which are readily available to yield telmisartan, its salts and derivatives thereof, which are bromine free and potentially less genotoxic, since there is no bromine atom in any of the raw materials. The process can also be carried out in multiple steps by isolation of the intermediate compounds. The intermediate compound 4-chloromethyl-2′-cyanobiphenyl can also be used for the preparation of irbesartan and other sartans.
-
(2015/07/22)

Telmisartan alkyl ester (by machine translation)
PROBLEM TO BE SOLVED: To provide a method for stably and efficiently producing a high quality telmisartan alkyl ester. SOLUTION: The method for producing the telmisartan alkyl ester comprises mixing 2-n-propyl-4-methyl-6-(1'-methylbenzimidazol-2-yl)benzimidazole with a polar aprotic solvent and a base, and then sequentially adding an alkyl 4'-bromomethylbiphenyl-2-carboxylate solution thereto. Thus, the telmisartan alkyl ester little containing impurities can efficiently be produced. COPYRIGHT: (C)2011,JPO&INPIT
-
Paragraph 0045; 0046; 0047; 0048

(2018/10/31)

ONE POT PROCESS FOR THE PREPARATION OF TELMISARTAN
A process for the preparation of bromine free telmisartan in one pot starting from 2-cyano-4'- methyl biphenyl, a compound of the Formula (1). The compound of the Formula (1) is chlorinated to give 4-chloromethyl-2' -cyanobiphenyl, the compound of the Formula (2). The reaction of the compound of the Formula (2), with 2-n-propyl-4-methyl-6-(1'- methylbenzimidazol-2'-yl) benzimidazole, a compound of the Formula (3) yields the compound 2-cyano-4'-[2"-n-propyl-4"-methyl-6"-(1'"-methylbenzimidazol-2"'- yl) benzimidazol-1"- ylmethyl] biphenyl, a compound of the Formula (4) which on hydrolysis of the cyano group yields telmisartan a compound of the Formula (5).
-
(2014/03/22)

Highly practical and cost-efficient synthesis of telmisartan: An antihypertensive drug
A novel and cost-efficient strategy for synthesis of an antihypertensive drug telmisartan, a substituted bis-benzimidazole derivative, is described. The key strategy is the construction of bis-benzimidazole 4 by reductive cyclization of o-nitroanilines 11 with butyl aldehyde and cyclocondensation of aromatic aldehydes 9 with o-phenylenediamine, then N-alkylation is allowed to give the target compound telmisartan after hydrolysis. The simple operation and workup procedure, along with the low production costs, make it suitable for industrial production and will benefits those with cardiovascular disease.
Wang, Ping,Zheng, Guo-Jun,Wang, Ya-Ping,Wang, Xiang-Jing,Wei, He-Geng,Xiang, Wen-Sheng
p. 2509 - 2512
(2012/04/11)

AN IMPROVED PROCESS FOR THE PREPARATION OF TELMISARTAN
Methyl-4-(butyramido)-3-methyl-5-nitrobenzoate is treated with sulphur containing reducing agent to give methyl-4-methyl-2-propyl-lH-benzimidazole-6-carboxylate, which is further hydrolyzed to the corresponding acid, 2-n-propyl-4-methyl-6- carboxy benzimidazole. The critical intermediate l,4'-dimethyl-2'-propyl-lH,3'H- 2,6'-bisbenzimidazol (DMPBB) is prepared by treating the above acid with N- mehtyl-o-phenylenediamine dihydrochloride under acidic conditions. Reaction of 4'-halomethylbiphenyl-2-carboxylic acid alkyl ester with DMPBB in presence of base to give Telmisartan ester which is further converted to Telmisartan of Formula (I).
-
(2012/03/26)

AN IMPROVED PROCESS FOR PREPARING TELMISARTAN
The present invention relates to an improved process for preparing telmisartan from 4-methyl-6-(1-methyl-1H-benzimidazole-2-yl)-2-propyl-1H-benzimidazole and 2-[4-(bromomethyl)phenyl] benzoate by using condensation reaction and hydrolysis reaction wherein the condensation reaction is performed to prepare an intermediate by using mixed solvent of dimethyl sulfoxide and isopropanol as reaction solvent using dimethyl sulfoxide of 0.5~1.5 times and isopropanol of 1.5~4.5 times on the basis of the usage of 4-methyl-6-(1-methyl-1H-benzimidazole-2-yl)-2-prophyl-1H-benzimidazole and the hydrolysis reaction is performed to cause the reaction in mixed solvent of methanol of 7~9 times and purified water of 5~7 times on the basis of the intermediate. The process for preparing telmisartan according to the present invention provides a simple preparing process for mass production and improves a manufacturing yield with high purity by eliminating an additional process for removing an inorganic salt as a byproduct due to a base used in the condensation reaction and the hydrolysis reaction.
-
Page/Page column 13

(2011/09/19)

Novel process for the preparation of telmisartan
The present invention relates to a novel process for preparing Telmisartan by ester hydrolysis using a silanolate compound.
-
Page/Page column 7-8

(2011/04/25)

A NEW PROCESS FOR THE PREPARATION OF PURE TELMISARTAN
This invention provides a process for preparing pure telmisartan by condensing 2- n-propyl-4-methyl-6-(r-methylbenzimidazol-2'-yl) benzimidazole (I) with a compound of formula (II) to obtain the compound 2-cyano-4'-[2"-n-propyl-4"-methyl- 6"-(l"'-methylbenzimidazol-2"'-yl)benzimidazol-l"-ylmethyl] biphenyl (III), and subsequently hydrolyzing the isolated nitrile function group to obtain the telmisartan.
-
Page/Page column 7-8

(2011/07/09)

PROCESS FOR PREPARING TELMISARTAN
The present invention refers to an improved process for the preparation of telmisartan or a pharmaceutical acceptable salt thereof through hydrolysis compounds of formula general (I) wherein R is tert-butyl ester (Ia) or salts thereof. Preferably, the invention discloses the preparation of telmisartan through hydrolysis of novel organic salts of compounds of formula (I), particularly wherein R is tert-butyl ester (Ia). The invention also relates to a process for the preparation of these novel organic salts, in particular wherein R is tert-butyl ester (Ia) and its use in the preparation of telmisartan.
-
Page/Page column 15; 16

(2011/01/12)

Efficient and improved synthesis of Telmisartan
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.
Kumar, A. Sanjeev,Ghosh, Samir,Mehta, G. N.
experimental part

(2010/07/18)

A process for the preparation of telmisartan
The present invention relates to a process for the preparation of Telmisartan by hydroxycarbonylation of compound of formula (V), wherein X is a substituent which can be transformed into a carboxy group by hydroxycarbonylation. The invention also relates to intermediates for the synthesis of Telmisartan.
-
Page/Page column 12

(2010/03/02)

AN IMPROVED PROCESS FOR THE PREPARATION OF SUBSTANTIALLY PURE TELMISARTAN
The present invention relates to an improved process for the preparation of substantially pure Telmisartan in polymorphic form A.
-
Page/Page column 11

(2010/04/03)

PROCESS FOR THE PREPARATION OF PURE 4'-[4-METHYL-6-(1-METHYL-2-BENZIMIDAZOLYL)-2-PROPYL-1-BENZIMIDAZOLYL]METHYL]-2-BIPHENYLCARBOXYLIC ACID
The present invention relates to the purification of Telmisartan (I) from a mixture of water immiscible solvent and polar aprotic solvent, which results in the Telmisartan with the purity of above 99.5% by HPLC. Further, the precipitation process of the present invention improves flowability of crystallized product, ease of filtration from the crystalline medium, thereby increasing the yield, decreasing the cost and avoiding the drying problems.
-
Page/Page column 8-9

(2010/04/03)

A modification to the synthesis of Telmisartan: An antihypertensive drug
A highly efficient approach to the synthesis of Telmisartan is described. Directed ortho-metalation of 4,4-dimethyl-2-phenyl-4,5-dihydrooxazole provided the key organozinc intermediate for a palladium catalysed biaryl coupling with 3′-(4-bromobenzyl)-1,7′-dimethyl-2′-propyl-1 H,3′ H-2,5′-bibenzo[d]imidazole which was obtained from alkylation of 1,7′-dimethyl-2′-propyl-1 H,3′H-2,5′-bibenzo[d] imidazole. This methodology overcomes many of the drawbacks associated with previously reported syntheses.
Kumar, A. Sanjeev,Ghosh, Samir,Mehta
experimental part
p. 95 - 97
(2010/07/05)

New strategy for the synthesis of telmisartan: An antihypertensive drug
An improved, convergent and industrially useful process suitable for large-scale production of telmisartan has been described. The key steps are Suzuki coupling for the preparation of key intermediate 4,4-dimethyl-2-(4′-methanesulfonyloxymethylbiphenyl-2-yl)oxazoline of telmisartan, N-alkylation and oxazoline hydrolysis.
Venugopal,Ramanatham,Devanna,Sanjeev Kumar,Ghosh, Samir,Soundararajan,Kale, Bhima,Mehta
experimental part
p. 2767 - 2773
(2010/11/03)

PROCESS FOR THE PREPARATION OF TELMISARTAN
The invention relates to processes for preparing telmisartan or a pharmaceutically acceptable salt thereof as well as to a process for preparing a telmisartan cyano intermediate. Moreover, the invention relates to a multilayer pharmaceutical tablet comprising (a) at least one first tablet layer comprising 1 to 50 wt. -% telmisartan or a pharmaceutically acceptable salt thereof by weight of the first tablet layer and (b) at least one second tablet layer comprising 1 to 50 wt.-% of a diuretic and 50 to 99 wt.-% of at least one filler by weight of the second tablet layer, wherein the combined weight of the diuretic and the at least one filler is at least 87 wt.-% by weight of the second tablet layer. The invention also relates to a process for the preparation of a multilayer pharmaceutical tablet.
-
Page/Page column 37-38

(2010/12/31)

METHOD OF MANUFACTURING 4'-[[4-METHYL-6-(1-METHYL-1H-BENZIMIDAZOL-2-YL)-2-PROPYL-1H-BENZIMIDAZOL-1YL]METHYL]BIPHENYL-2-CARBOXYLIC ACID (TELMISARTAN)
A carboxylic acid of the general formula R1COOH, wherein R1 is the hydrogen atom or a C1-C4 alkyl, is added to a solution of the potassium salt of telmisartan in an alcohol of the formula R2OH with the water content lower than 2%, wherein R2 is ethyl or methyl.
-
Page/Page column 3

(2010/09/07)

Catalyzed carbonylation in the synthesis of angiotensin ii antagonists
One embodiment disclosed in the invention is the efficient synthesis of halogenated biaryl starting material via Grignard chemistry and the use thereof. Another embodiment of the invention is the reaction of catalyzed carbonylation of the 3'-(2'-halo-biphenyl-4-ylmethyl)-1,7'-dimethyl-2'-propyl-1H,3'H-[2,5']bibenzoimidazolyl (TLMH) using either gaseous carbon monoxide in a solvent mixture containing water; or formic acid salts optionally together with acetic acid in anhydrous solvent.
-
Page/Page column 8-9

(2009/10/01)

2'-Halobiphenyl-4-yl intermediates in the synthesis of angiotensin II antagonists
A process for obtaining 2'-halo-4-methylbiphenyls is described, which comprises reacting 4-halotoluene with a 1,2-dihalobenzene in the presence of elemental metal such as magnesium, lithium or zinc, wherein 0 to 0.9 molar, particularly 0 to 0.2 molar excess of 4-halotoluene in regard to 1,2-dihalobenzene is used, and arised organometal intermediates are quenched by elemental halogen. In addition, the coupling of arised 2'-halo-4-methylbiphenyls with 2-(1-propyl)-4-methyl-6-(1'-methylbenzimidazole-2-il)benzimidazole to afford 3'-(2'-halo-biphenyl-4-ylmethyl)-1,7'-dimethyl-2'-propyl-1H,3'H-[2,5']bibenzoimidazolyl, which can be further converted to organometallic compound and said organometallic compound is further reacted with formic acid derivative, such as N,N-dimethylformamide, alkylformiate or carbon dioxide to obtain telmisartan, is also described. Further described is use of in line analytics for monitoring the aforementioned reactions.
-
Page/Page column 11

(2009/10/01)

NOVEL INTERMEDIATES AND METHOD FOR SYNTHESIS OF 4'-[(1,4'-DIMETHYL-2'-PROPYL-[2,6'- BI-1HBENZIMIDAZOL]-L-YL)METHYL]-1,1-BIPHENYL]-2-CARBOXYLIC ACID.
Disclosed herein is a method for synthesis of 4'-[(1,4'-dimethyl-2'-propyl-[2,6'-bi- 1H]benzimidazol]-l-yl)methyl]-[1,1-biphenyl]-2-carboxylic acid or its derivatives, and novel intermediate compounds useful in the synthesis.
-
(2009/10/22)

New and improved synthesis of telmisartan: An antihypertensive drug
An improved, cost-effective, and industrially advantageous process suitable for large-scale production of telmisartan 1 has been described. The key steps include Suzuki coupling for the preparation of key intermediate 2-(4'-chloromethyl-biphenyl-2-yl)-4,4
Kumar, A. Sanjeev,Ghosh, Samir,Mehta,Soundararajan,Sarma,Bhima, Kale
experimental part
p. 4149 - 4157
(2010/01/13)

A process for the preparation of Telmisartan.
The present invention relates to a process for the preparation of Telmisartan esters and Telmisartan and intermediates for the synthesis thereof.
-
Page/Page column 13

(2009/12/07)

PROCESS FOR PREPARATION OF TELMISARTAN
A process for preparation of telmisartan comprises: (i) oxidation of compound of formula (a), wherein R2 is a hydrogen atom or a substituent of formula (b), in which R1 is a protecting group for the carboxyl function, to an aldehyde of formula (c), in which R2 is defined as in the formula (a), and, optionally, (ii) in case R2 in the compound (c) thus obtained is a hydrogen atom, iV-alkylation of the compound (c) with a biphenyl derivative, (iii) treatment of the compound (c) thus obtained with N- methyl- o-nitroaniline in a cyclocondensation reaction, and (iv) cleavage of the protecting group R1.
-
Page/Page column 19-20

(2009/10/30)

Pharmaceutically acceprable salts of aporphine compounds of carboxyl group-containing agents and methods for preparing the same
The present invention discloses novel pharmaceutically acceptable salts of aporphine compounds and carboxyl-group containing agents. Also, the present invention discloses methods for preparing the pharmaceutically acceptable salts. These pharmaceutically acceptable salts are suitable for use in treating and/or preventing hyperglycemic disease and/or several oxidative stress related diseases.
-
(2009/12/28)

PROCESS FOR PREPARING TELMISARTAN
Novel processes for preparing a telmisaitan nitrile intermediate (4'-[{2-n-propyl-4- methyI-6-f l-methyJbenzimidazol-2-yl)-benzimidazol- l -yl)-methyl]-biphenyl-2-nitrile) and further converting it to telmisaitan and/or salts thereof are disclosed.
-
Page/Page column 44-45

(2009/03/07)

Concise synthesis of telmisartan via decarboxylative cross-coupling
(Chemical Equation Presented) An efficient synthesis of the angiotensin II receptor antagonist telmisartan is presented involving a decarboxylative cross-coupling of isopropyl phthalate (1) with 2-(4-chlorophenyl)-1,3-dioxolane (2c) as the key step (85% yield). The benzimidazole moiety is constructed regioselectively via a reductive animation-condensation sequence, replacing the previously published route via alkylation of the preformed benzimidazole. The product is obtained in an overall yield of 35% in a convergent synthesis with the longest sequence consisting of eight steps.
Goossen, Lukas J.,Knauber, Thomas
supporting information; experimental part
p. 8631 - 8634
(2009/04/11)

A PROCESS FOR THE PREPARATION OF TELMISARTAN
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.
-
Page/Page column 6; 12-13

(2008/06/13)

An efficient and impurity-free process for telmisartan: An antihypertensive drug
Telmisartan (1), a substituted dibenzimidazole derivative, is an antihypertensive drug, essentially used to control blood pressure. An improved, cost-effective, and impurity-free process for telmisartan (1) suitable for large-scale production is described here by addressing various process development issues. The overall yield obtained from this newly developed process is around 50% (over five steps) compared to the literature reported process (21%, over eight steps).
Reddy, Kikkuru Srirami,Srinivasan, Neti,Reddy, Chinta Raveendra,Kolla, Naveenkumar,Anjaneyulu, Yerremilli,Venkatraman, Sundaram,Bhattacharya, Apurba,Mathad, Vijayavitthal T.
p. 81 - 85
(2012/12/26)

PREPARATION OF TELMISARTAN SALTS
New salts of telmisartan, in amorphous and crystalline forms, together with two new polymorphic forms of telmisartan potassium, have been prepared by crystallization, evaporation of solvent, spray-drying or lyophilization and were included into a pharmaceutical formulation.
-
Page/Page column 30

(2008/06/13)

A SYNTHESIS OF 4-BROMOMETHYL-2'-FORMYLBIPHENYL AND 4-BROMOMETHYL-2'- HYDROXYMETHYLBIPHENYL AND ITS USE IN PREPARATION OF ANGIOTENSIN II ANTAGONISTS
4-bromomethyl-2'-formylbiphenyl and 4-bromomethyl-2'-hydroxymethylbiphenyl are useful starting material for the preparation various angiotenzin II antagonists, which are prepared from 4-bromomethyl-2'-cyanobiphenyl or 4'- bromomethylbiphenylcarboxyilic derivatives using selected hydride reagent.
-
Page/Page column 11; 18

(2008/06/13)

Telmisartan production process
The present invention provides an intermediate and a process for preparing Telmisartan, which overcomes the drawbacks of conventional methods and produces Telmisartan in high purity and yield.
-
Page/Page column 4

(2008/06/13)

PROCESS FOR PREPARING TELMISARTAN
A process for preparing telmisartan and intermediates formed in the process.
-
Page/Page column 27-29

(2008/06/13)

Processes of preparing highly pure telmisartan form A, suitable for pharmaceutical compositions
Processes are disclosed for preparing Telmisartan form A, which is free-flowing and which does not contain electrostatic charge and is thus industrially process-able. The free-flowing Telmisartan form A is prepared by crystallization from a polar organic solvent e.g., DMSO, DMF, DMA, NMP, or water and is suitable for use in pharmaceutical compositions. A process is also disclosed for preparing highly-pure Telmisartan form A by precipitation from aqueous solutions.
-
Page/Page column 7

(2008/06/13)

Process for the preparation of angiotensin receptor blockers and intermediates thereof
A process for the preparation of a biphenyl-containing compound of general formula I: wherein R1 is a C3-6 carbonyl containing compound; R2 is a substituted or unsubstituted, straight or branched C3-6 alkyl group, or R1 and R2 together with the nitrogen atom to which they are bonded are joined together to form a substituted heterocyclic group selected from the group consisting of substituted or unsubstituted imidazoles, substituted or unsubstituted benzimidazoles and substituted or unsubstituted 1,3-diazaspiro[4,4]non-1-en-4-one; and R3 is a carboxylic acid ester, cyano, a substituted or unsubstituted 1H-tetrazolyl group or a substituted or unsubstituted group which may be converted in vivo into a carboxy group is provided, the process comprising reacting a compound of general formula II: wherein R1 and R2 have the aforestated meanings with a compound of general formula III: wherein Z is a leaving group and R3 has the aforestated meaning in a biphasic solvent system in the presence of a phase transfer catalyst.
-
Page/Page column 5-6

(2008/06/13)

PROCESS FOR PREPARING TELMISARTAN
Provided are processes for preparing telmisartan alkyl ester and telmisartan using environmentally friendly organic solvents that are easily removed from the reaction mixture, wherein a telmisartan alkyl ester is isolated and hydrolyzed to form telmisartan or the telmisartan is prepared using a synthesis in a single reaction vessel.
-
Page/Page column 16-17

(2008/06/13)

SUBSTANTIALLY PURE MICRONIZED PARTICLES OF TELMISARTAN AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME
The present invention provides micronized particles of substantially pure telmisartan or a pharmaceutically acceptable salt, ester or derivative thereof. Also provided are pharmaceutical compositions containing the micronized particles of substantially pure telmisartan or a pharmaceutically acceptable salt, ester or derivative thereof.
-
Page/Page column 17

(2008/06/13)