- A PROCESS FOR THE PREPARATION OF HIGHLY PURE VALSARTAN
-
Disclosed herein is a process for the preparation and purification of Valsartan. The process according to the invention is capable of removing the toxic nitroamine impurities and providing substantially pure Valsartan.
- -
-
Page/Page column 11-16
(2021/06/11)
-
- Valsartan without genotoxic impurity and preparation method thereof (by machine translation)
-
To, valsartan crude: is cyclised to obtain valsartan medoxomil (V), and the valsartan crude product (IV), is purified to obtain valsartan medoxomil (III), to obtain valsartan medoxomil (,) through hydrolysis pH, modulation (II), to obtain the valsartan crude product. pH. The valsartan crude product is obtained by cyclizing the valsartan medoxomil sodium, into salt to obtain valsartan medoxomil,and preparation method of the valsartan medoxomil prepared by the following steps N,N - refining to obtain valsartan medoxomil and, N,N -% of valsartan medoxomil. (by machine translation)
- -
-
-
- Synthesis of 5-Substituted 1 H-Tetrazoles from Nitriles by Continuous Flow: Application to the Synthesis of Valsartan
-
An efficient continuous flow process for the synthesis of 5-substituted 1H-tetrazoles is described. The process involves the reaction between a polymer-supported triorganotin azide and organic nitriles. The polymer-supported organotin azide, which is in situ generated with a polystyrene-supported triorganotin alkoxide and trimethylsilylazide, is immobilized in a packed bed reactor. This approach is simple, fast (it takes from 7.5 to 15 min), and guarantees a low concentration of tin residues in the products (5 ppm). The process was developed to aryl-, heteroaryl-, and also alkylnitriles and was applied for the synthesis of valsartan, an angiotensin II receptor antagonist.
- Carpentier, Florian,Felpin, Fran?ois-Xavier,Zammattio, Fran?oise,Le Grognec, Erwan
-
p. 752 - 761
(2020/03/13)
-
- Method for treating azide ions, non-genotoxic impurity Sartan raw material medicine and immediate thereof
-
The invention discloses a method for treating azide ions in a system and application thereof to the preparation of a compound with a tetrazolium group and without genotoxic impurities. The method is that the azide ions contained in the hydrogen peroxide treatment system are used. The method is used for preparing the compound with the tetrazolium group and comprises the following preparation steps:enabling a compound containing a cyano group to react with an azide, adding hydrogen peroxide after the reaction to quench and remove excessive sodium azide and further obtaining the compound with the tetrazolium group. The compound prepared by the method does not contain the genotoxic impurities. The method is simple in operation, mild in reaction conditions and suitable for industrial production.
- -
-
Paragraph 0104
(2019/05/28)
-
- A trityl protecting group by removing method of preparing losartan medicine
-
The invention discloses a method for preparation of a Sartan drug by removal of a triphenylmethyl protective group. The method includes: under the catalysis of an insoluble weak acid, subjecting a Sartan prodrug and methanol to deprotection reaction, and after complete reaction, conducting aftertreatment to obtain the Sartan drug. The method has the characteristics of low cost, few side product, high quality product, and simple aftertreatment. At the same time, montmorillonite can be taken as insoluble weak acid, and the cost is low, thus being convenient for industrial production.
- -
-
Paragraph 0032-0039; 0047-0051
(2018/07/30)
-
- Preparation and purification method of valsartan
-
The invention relates to the field of medicinal chemistry and discloses a preparation and purification method of valsartan. The method comprises the steps of (S1) adding L-valine and alcohol to a reaction kettle, slowly dropwise adding thionyl chloride, carrying out heating reflux reaction, adding isopropyl acetate for pulping, carrying out suction filtration to obtain an intermediate 1; (S2) carrying out nucleophilic reaction on the intermediate 1 and a starting material 2 in a solvent under an alkaline condition to obtain an intermediate 2; (S3) carrying out nucleophilic reaction on the intermediate 2 and valeryl chloride in the solvent under the alkaline condition to obtain an intermediate 3; and (S4) carrying out cyclization reaction on the intermediate 3, sodium azide and a catalyst ((-)-sparteine-Cu (II) complex) in the solvent, washing, crystallizing and drying to obtain the valsartan. The sodium azide and the catalyst ((-)-sparteine-Cu (II) complex) are used in the cyclization reaction, and the cyclization yield can reach 90%. According to the purification method, the purity of the raw materials of the valsartan is greater than 99.99%, the content of a solvent residue (ethyl acetate) is smaller than 0.5%, the content of a specific impurity is smaller than 0.1%, other unknown individual impurities are avoided and an enantiomer impurity is not detected.
- -
-
-
- A method of preparing the valsartan
-
The invention discloses a method for preparing valsartan. The method comprises the following steps: carrying out a first-step reaction on L-valine methyl-ester hydrochloride and 2-cyan-4'-bromomethyl biphenyl, of which the molar ratio is (1-2):1; carrying out a second-step reaction together with pentanoyl chloride; finally carrying out a third-step reaction, so as to obtain a valsartan crude product, wherein the first-step reaction comprises the following steps: by taking acetonitrile as a reaction solvent, carrying out neutral reaction on the L-valine methyl-ester hydrochloride and potassium carbonate; then adding the 2-cyan-4'-bromomethyl biphenyl to react; adding the 2-cyan-4'-bromomethyl biphenyl by 2-6 times, wherein the reaction temperature is 50-65 DEG C; the reaction time is 3-7 hours. By adopting the method for preparing the valsartan, the quantity of byproducts corresponding to valsartan impurities T in the product in the first step is controlled, so as to control the quantity of the valsartan impurities T; furthermore, the other conditions are correspondingly adjusted; generation of other unmanageable impurities also can be avoided. Thus, the high-purity valsartan product can be prepared.
- -
-
-
- DEPROTECTION METHOD FOR TETRAZOLE COMPOUND
-
The present invention relates to a method of deprotecting a tetrazole compound, useful as an intermediate for angiotensin II receptor blockers, and provides a novel production method of angiotensin II receptor blockers. Provided is a production method of a compound represented by the formula [3] or [4] or a salt thereof, including (i) reducing a compound represented by the formula [1] or [2] or a salt thereof in the presence of a metal catalyst and an alkaline earth metal salt, or (ii) reacting the compound with a particular amount of Br?nsted acid: wherein each symbol is as defined in the present specification.
- -
-
-
- COMPOSITIONS AND METHODS FOR DIAGNOSING AND TREATING SALT SENSITIVITY OF BLOOD PRESSURE
-
To characterize the urinary exosome miRNome, microarrays were used to identify the miRNA spectrum present within urinary exosomes from ten individuals that were previously classified for their salt sensitivity status. The present application discloses distinct patterns of selected exosomal miRNA expression that were different between salt-sensitive (SS), salt-resistant (SR), and inverse salt-sensitive (ISS) individuals. These miRNAs can be useful as biomarkers either individually or as panels comprising multiple miRNAs. The present invention provides compositions and methods for identifying, diagnosing, monitoring, and treating subjects with salt sensitivity of blood pressure. The applications discloses panels of miRNAs useful for comparing profiles, and in some cases one or more of the miRNAs in a panel can be used. The miRNAs useful for distinguishing SS and SR or ISS and SR subjects. One or more of the 45 miRNAs can be used. Some of the miRNAs have not been previously reported to be circulating. See those miRNAs with asterisks in FIG. 1 and below. The present invention encompasses the use of one or more of these markers for identifying and diagnosing SR, SS, and ISS subjects.
- -
-
-
- PROCESS FOR THE PREPARATION OF ANGIOTENSIN II ANTAGONISTS AND INTERMEDIATES THEREOF
-
The present invention relates to an improved process for the preparation of angiotensin receptor antagonists and intermediates thereof. Particularly the present invention relates to an improved process for the preparation of N-(1-oxopentyl)-N-[[2′-(1H-tetrazol-5-yl)[1,1′-biphenyl]-4-yl]methyl]-L-valine of Formula 1 via a phosphite salt of Formula-4.H3PO3 preferably a phosphite salt of Formula-4′.H3PO3
- -
-
-
- PROCESS FOR THE PREPARATION OF VALSARTAN
-
The present invention relates to a process for the preparation of pure Valsartan (I) substantially free from impurities of formulae (Ia), (Ib), and (Ic), which comprises: (i) condensing 2-(4′-bromomethylphenyl)benzonitrile of formula (II) with L-valine methyl ester hydrochloride of formula (V) in the presence of a base in a solvent to produce N-[(2′-cyanobiphenyl-4-yl)methyl]-(L)-valine methyl ester of formula (VI); (ii) treating the compound VI of step (i) with acid followed by treating with base to produce pure compound VI substantially free from dimeric impurity of formula (Via); (iii) reacting the pure compound of formula (VI) with n-valeryl chloride in the presence of a base to produce pure N-valeryl-N-[(2′-cyanobiphenyl-4-yl)methyl]-(L)-valine methyl ester (VII) substantially free from alkene impurity of formula (Vila); (iv) reacting the compound of formula (VII) with trialkyltin chloride and a metal azide in a solvent at a reflux temperature to produce N-(1-oxopentyl)-N-[[2′-(2-tributyltinte-trazol-5-yl)-(1,1′-biphenyl)-4-yl]methyl]-(L)-valine methyl ester of formula (VHIb) free from thermal degradation impurity (Villa); (v) hydrolyzing the compound of formula (VHIb) in the presence of alkaline conditions to produce Valsartan (I).
- -
-
Paragraph 0062; 0063; 0064; 0065; 0066
(2013/06/26)
-
- AN IMPROVED PROCESS FOR THE PREPARATION OF ANGIOTENSIN II ANTAGONISTS AND INTERMEDIATES THEREOF.
-
The present invention relates to an improved process for the preparation of angiotensin receptor antagonists and intermediates thereof. Particularly the present invention relates to an improved process for the preparation of N-(l-oxopentyl)-N-[[2''-(lH-tetrazoI-5-yl) [1, 1 ''-biphenyl]-4-yl] methyl]-L- valine of Formula (1) Formula-1 Formula-4.H3P03 via a phosphite salt of Formula-4.H3P03 preferably a phosphite salt of Formula-4''.H3P03 Ph3C N-[2''-1 -triphenylmethyl-tetra zol-5-yl)biphenyl-4-yl)methyl ]-(L)-Valine Benzyl ester H3P03 salt Formula-4''.H3P03 salt.
- -
-
-
- AN IMPROVED PROCESS FOR THE PREPARATION OF VALSARTAN
-
The present invention relates to a process for the preparation of pure Valsartan (I) substantially free from impurities of formulae (la), (lb), and (Ic), which comprises: (i) condensing 2-(4'-bromomethylphenyl)benzonitrile of formula (II) with L-valine methyl ester hydrochloride of formula (V) in the presence of a base in a solvent to produce N-[(2'-cyanobiphenyl-4-yl)methyl]-(L)-valine methyl ester of formula (VI); (ii) treating the compound VI of step (i) with acid followed by treating with base to produce pure compound VI substantially free from dimeric impurity of formula (Via); (iii) reacting the pure compound of formula (VI) with n-valeryl chloride in the presence of a base to produce pure N-valeryl-N-[(2'-cyanobiphenyl-4-yl)methyl]- (L)-valine methyl ester (VII) substantially free from alkene impurity of formula (Vila); (iv) reacting the compound of formula (VII) with trialkyltin chloride and a metal azide in a solvent at a reflux temperature to produce N-(l-oxopentyl)-N-[[2'-(2- tributyltintetrazol-5-yl)-(l, l '-biphenyl)-4-yl]methyl]-(L)-valine methyl ester of formula (VHIb) free from thermal degradation impurity (Villa); (v) hydrolyzing the compound of formula (VHIb) in the presence of alkaline conditions to produce Valsartan (I).
- -
-
Page/Page column 15-16
(2012/01/14)
-
- PROCESS FOR PRODUCTION OF BIPHENYL DERIVATIVE
-
The invention provides a production method of a biaryltetrazole derivative useful as an intermediate for an angiotensin II receptor antagonist. The method comprises reacting an aryltetrazole derivative with a benzene derivative, deprotecting or reducing the resulting compound, and halogenating the deprotected or reduced compound
- -
-
Page/Page column 36
(2012/09/22)
-
- An efficient and telescopic process for valsartan, an angiotensin II Receptor Blocker
-
An efficient, telescopic, and scalable process for an antihypertensive drug substance, valsartan with an overall yield of 58%, and ~99.9% purity is described. A simple, and safe process is developed for the recovery of tributyltin chloride from the tributyltin hydroxide, byproduct formed in the tetrazole ring construction, and reused in the synthesis of valsartan.
- Aalla, Sampath,Gilla, Goverdhan,Bojja, Yakambram,Anumula, Raghupathi Reddy,Vummenthala, Prabhakar Reddy,Padi, Pratap Reddy
-
experimental part
p. 682 - 686
(2012/08/07)
-
- AN IMPROVED PROCESS FOR THE PREPARATION OF N-PENTANOYL-N-[[2'-(1H-TETRAZOL-5-YI)[1,1'-BIPHENYL]-4-YI]METHYL]-L-VALINE
-
Disclosed herein is an improved process for the preparation of pure N-Pentanoyl-N-[[2'- (1h-Tetrazol-5-Y1)[1,1'-Biphenyl]-4-Yl]Methyl]-L-Valine employing highly active carbon.
- -
-
-
- An improved synthesis of valsartan
-
Biphenyltetrazole group, an important component of sartans, is usually formed in excellent yield by the reaction of 4′-alkylbiphenyl-2- carbonitrile with excessive organotin azide. However, it is restricted in industrial scale because of the difficult post-treatment. In this article, an improved synthetic method for valsartan and the quantitative recovery of tri-n-butyltin chloride are reported. During this process, the tetrazole-Sn complex and excessive organotin azide were decomposed by HCl to furnish tri - n-butyltin chloride, and then reacted with NaF to lead to filterable polymer tributyltin fluoride which was converted again to tributyltin chloride by HCl in ethyl acetate. This approach is facile for the efficient manufacture of sartans using organotin azide to form the tetrazole group and is valuable for industry readers.
- Wang, Guo-Xi,Sun, Bao-Ping,Peng, Cong-Hu
-
experimental part
p. 986 - 988
(2011/12/16)
-
- Synthesis of angiotensin II receptor blockers by means of a catalytic system for C-H Activation
-
A highly efficient catalytic system for C-H activation has been worked out that involves inexpensive RuCl3·xH2O and a specific amount of PPh3. This procedure has been successfully applied to a practical synthesis of angiotensin II receptor blockers (ARBs). The residual ruthenium that existed in the reaction mixture was thoroughly removed by treatment with properly selected metal scavengers. The new process permits ready access to the important class of drugs in a highly atom-economical and sustainable manner (Figure presented).
- Seki, Masahiko,Nagahama, Masaki
-
p. 10198 - 10206
(2012/02/03)
-
- IMPROVED PROCESS FOR PREPARING VALSARTAN
-
The invention relates to an improved process for the preparation of valsartan wherein the cycloaddition reaction is performed is an ether as reaction solvent, with a metal salt azide and in the present of zinc halides.
- -
-
-
- PROCESS FOR THE MANUFACTURE OF ORGANIC COMPOUNDS
-
The present invention relates to processes for the manufacture of an angiotensin receptor blocker (ARB; also called angiotension Il receptor antagonist or AT1 receptor antagonist) and salts thereof, to novel intermediates and process steps.
- -
-
-
- Process for the manufacture of organic compounds
-
The present invention relates to a process for the manufacture of an angiotensin receptor blocker (ARB: also called angiotension II receptor antagonist or AT1 receptor antagonist) and salts, thereof, to novel intermediates and process steps.
- -
-
-
- PREPARATION OF VALSARTAN
-
Processes for preparing valsartan and essentially amorphous valsartan are described.
- -
-
Page/Page column 18-19
(2010/08/18)
-
- METHOD OF REMOVING THE TRIPHENYLMETHANE PROTECTION GROUP
-
The present invention relates to a method of removing triphenylmethane protection group. The method for preparing biphenyl benzoic acid derivatives of the present invention is economically advantageous and very excellent in the aspect of improving process in that: process safety is secured by using acidic ion exchange resin in the presence of organic solvent instead of using highly corrosive acid; the reaction takes much less time than do the conventional reactions which use only anhydrous methanol and few sub-reaction does occur; and the ion-exchange resin of the present invention is excellent for mass-processing because the resin can be collected and recycled only by filtration after being used.
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Page/Page column 20
(2010/07/02)
-
- A short and efficient synthesis of valsartan via a Negishi reaction
-
An efficient synthesis of the angiotensin-II inhibitor valsartan (Diovan) is presented. Directed ortho-metalation of 5-phenyl-1-trityl-1H- tetrazole (6) and its Negishi coupling with aryl bromide 5 are the key steps of the synthesis. This method overcomes
- Ghosh, Samir,Kumar, A. Sanjeev,Mehta, G. N.
-
experimental part
(2010/07/18)
-
- New and improved manufacturing process for valsartan
-
A new and improved industrially viable manufacturing process for valsartan, an antihypertension drug, is described.
- Kumar N, Senthil,Reddy, Shankar B.,Sinha, Brajesh Kumar,Mukkanti, Kagga,Dandala, Ramesh
-
scheme or table
p. 1185 - 1189
(2010/04/22)
-
- PROCESS FOR PREPARATION OF VALSARTAN INTERMEDIATE
-
The present invention provides a process for preparation of a key intermediate of valsartan in a pure form and use of this intermediate for the preparation of valsartan or a pharmaceutically acceptable salt in pure form.
- -
-
-
- PROCESSES FOR THE PREPARATION OF INTERMEDIATES OF VALSARTAN
-
The present invention relates to processes for the preparation of intermediates of valsartan.
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Page/Page column 7
(2009/08/18)
-
- Processes for the preparation of intermediates of valsartan
-
The present invention relates to processes for the preparation of intermediates of valsartan.
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-
Page/Page column 13
(2009/09/05)
-
- Unusual detritylation of tritylated tetrazole in Sartan molecules
-
Tritylated tetrazole of 2a underwent unusual detritylation under basic reaction condition during the synthesis of methyl ether of olmesartan medoxomil 1. The unusual detritylation was found to be a common feature in the case of all tetrazole containing Sartan molecules (3-7).
- Srimurugan, Sankareswaran,Suresh, Paulsamy,Babu, Balaji,Hiriyanna, Salmara Ganeshbhat,Pati, Hari Narayan
-
p. 383 - 384
(2008/09/20)
-
- PROCESS FOR PREPARING VALSARTAN
-
An N-[(2'-(1-triphenyl methyl tetrazole-5-yl) biphenyl]-4-yl] methyl]-L-valine benzyl ester organic salt of formula (IVA) wherein A represents an organic carboxylic acid, a process for its preparation and its use in the synthesis of valsartan or salts thereof.
- -
-
-
- AN IMPROVED PROCESS FOR THE PREPARATION OF VALSARTAN
-
The present invention relates to an improved process for the preparation of valsartan compound of formula-1 through novel intermediate compounds. It also relates to a novel process for the preparation of amorphous form of valsartan.
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-
Page/Page column 20
(2010/11/29)
-
- PROCESS FOR THE PREPARATION OF VALSARTAN AND INTERMEDIATE PRODUCTS
-
The present invention relates to a new method for the production of valsartan, a valine derivative having the chemical name is (S)-N-(1 -carboxy-2-methylprop-1 -yl)-N-pentanoyl-N- [2'-(1 H-tetrazol-5-yl)-biphenyl-4-ylmethyl]amine, and pharmacologically ac
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-
Page/Page column 12; 19-20
(2008/12/06)
-
- PROCESS FOR THE PREPARATION OF VALSARTAN
-
The present invention relates to a process for preparing valsartan from a compound of general formula (I), wherein R is cumyl, trityl or t-butyl. The process comprises a first step, wherein the protective group is eliminated and thereafter the oxazolidinone ring is opened by catalytic hydrogenationin the presence of an organic base. Finally, Valsartanor a pharmaceutically acceptable salt thereofis isolated.
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Page/Page column 10; 12
(2009/01/20)
-
- INTERMEDIATES AND PROCESSES FOR THE PREPARATION OF VALSARTAN
-
It comprises a preparation process of Valsartan from new salts of Valsartan having the tetrazole moiety protected with a protective group. The process leads to the elimination of the typical impurities due to the preparation process while avoiding its rac
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Page/Page column 26-27
(2010/11/27)
-
- A PROCESS FOR PURIFICATION OF VALSARTAN
-
The present invention relates to a process for purification of Valsartan comprising steps of: (i) crystallizing from an organic solvent (ii) washing the crystallized product obtained in step (i) with a solvent selected from a group consisting of aliphatic
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-
Page/Page column 6
(2008/06/13)
-
- A process for the preparation of angiotensin II antagonistic compounds
-
A process for the preparation of angiotensin II antagonists and novel intermediates useful for the synthesis thereof.
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-
Page/Page column 7
(2008/06/13)
-
- PROCESS FOR THE PREPARATION OF ANGIOTENSIN II ANTAGONISTIC COMPOUNDS
-
A process for the preparation of angiotensin II antagonists and novel intermediates useful for the synthesis thereof.
- -
-
Page/Page column 5
(2010/11/26)
-
- Synthesis of valsartan via decarboxylative biaryl coupling
-
(Chemical Equation Presented) An efficient synthesis of the angiotensin II inhibitor valsartan (Diovan) is presented. Two routes were evaluated, both making use of an advanced version of our decarboxylative coupling for the construction of the biaryl moiety. Thus, in the presence of a catalyst system consisting of copper(II) oxide, 1,10-phenanthroline, and palladium(II) bromide, 2-cyanocarboxylic acid was coupled with 1-bromo(4-dimethoxymethyl)benzene in 80% yield and with 4-bromotoluene in 71% yield. The valsartan synthesis using 1-bromo(4-dimethoxymethyl)benzene was completed in four steps overall with a total yield of 39%, via a novel route that presents substantial economical and ecological advantages over the literature process, as it is more concise and stoichiometric amounts of expensive organometallic reagents are avoided.
- Goossen, Lukas J.,Melzer, Bettina
-
p. 7473 - 7476
(2008/02/12)
-
- Process for obtaining a valsartan salt useful for obtaining valsartan
-
The invention relates to a new salt of Valsartan, in particular to the high-purity dilithium salt of Valsartan, its polymorphs and solvates or hydrates thereof, useful for obtaining Valsartan with a high yield. The process for obtaining the dilithium salt of Valsartan (I) comprises i) Coupling of the intermediate (II) with the 2-(1H-tetrazole-5-il)-phenylboronic acid of formula (III), wherein said coupling takes place in the presence of a lithium base, and a mixture of water and water-miscible organic solvent and a palladium catalyst, to give the dilithium salt of Valsartan of formula (I).
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Page/Page column 6-7
(2008/06/13)
-
- Process for the Preparation of Valsartan and its Intermediates
-
The present invention concerns a process for preparing valsartan of Formula I: comprising purifying intermediate benzyl valsartan of Formula IV by crystallizing said benzyl valsartan of lower purity from a first solvent which is a ternary mixture comprising a hydrophilic solvent, a non-polar protic solvent and water; recovering benzyl valsartan from said ternary mixture followed by crystallizing benzyl valsartan from a second solvent comprising a non-polar aprotic solvent or polar aprotic solvent or their mixture; and recovering benzyl valsartan substantially free of organotin impurity; and converting said benzyl valsartan of into valsartan
- -
-
Page/Page column 3; 9-10
(2008/06/13)
-
- Efficient synthesis of valsartan, a nonpeptide angiotensin II receptor antagonist
-
A highly efficient and convergent approach to the synthesis of the angiotensin II receptor antagonist valsartan (1), one of the most important agents used in antihypertensive therapy today, is described. Directed ortho-metalation of 4-bromotoluene provides the key boronic acid intermediate 11 which was subjected to palladium-catalyzed Suzuki coupling. This method overcomes many of the drawbacks associated with the previously reported syntheses. The saponification of the methyl ester in valsartan was realized in a convenient and economical manner, which is more suitable for industrial production. Georg Thieme Verlag Stuttgart.
- Zhang, Chen,Zheng, Guojun,Fang, Lijing,Li, Yulin
-
p. 475 - 477
(2007/10/03)
-
- A process for the synthesis of valsartan
-
This invention relates to an improved process for preparing a valsartan, or a pharmaceutically acceptable salt thereof, or pharmaceutical preparation containing either entity wherein a compound of formula (II) or a salt thereof, is reacted with valine or
- -
-
Page/Page column 13
(2010/11/08)
-
- PROCESS FOR THE PREPARATION OF TETRAZOLE DERIVATIVES FROM ORGANO BORON AND ORGANO ALUMINIUM AZIDES
-
The present invention relates to a method for preparing substituted tetrazoles, compounds obtained according to this method, new reactants and new tetrazole derivatives.
- -
-
Page/Page column 56
(2008/06/13)
-
- A process for the preparation of valsartan and intermediates thereof
-
A novel process for the preparation of valsartan and novel intermediates useful in the preparation thereof.
- -
-
Page/Page column 8
(2010/02/11)
-
- PROCESS FOR THE PREPARATION OF VALSARTAN AND PRECURSORS THEREOF
-
This invention relates to a process for preparing intermediates useful in preparing Valsartan and to a process for preparing the latter, together with synthesis intermediates of formula (IV), (V) and (VI), useful for manufacturing a medicament for the treatment of arterial hypertension or heart failure. The process for preparing Valsartan permits it to be prepared on an industrial scale with high yields and without racemisation problems, in addition to using simple and available starting products. The invention also provides a process for preparing the intermediate of formula (VI), from an intermediate of formula (V) that does not require protection of the carboxylic acid prior to N-acylation.
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Page/Page column 28-29
(2008/06/13)
-
- PROCESS FOR PREPARATION OF BIPHENYL TETRAZOLE
-
The present invention relates to processes for the preparation of pure valsartan. Also provided is a barium salt of valsartan, and a pharmaceutical composition thereof.
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-
Page/Page column 11-12
(2008/06/13)
-
- Process for the preparation of valsartan and intermediates thereof
-
A novel process for the preparation of valsartan and novel intermediates useful in the preparation thereof.
- -
-
Page/Page column 5
(2010/02/12)
-
- PROCESS FOR THE MANUFACTURE OF VALSARTAN
-
The present invention relates to a process for the manufacture of Valsartan, an angiotensin receptor blocker (ARB; also called angiotension II receptor antagonist or AT1 receptor antagonist) and salts thereof, to novel intermediates and process steps.
- -
-
-
- POLYMORPHIS OF VALSARTAN
-
Provided are crystalline and amorphous form of valsartan, and processes for their preparation.
- -
-
-