cas 138402-11-6, Irbesartan | Articles data

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Improved synthesis of irbesartan, an antihypertensive active pharmaceutical ingredient
An improved synthesis of the antihypertensive drug irbesartan, based on the Suzuki reaction, has been described. Copyright Taylor & Francis, Inc.
Sumalatha, Bollikonda Satyanarayana Yasareni,Venkatraman, Sundram,Reddy, Ghanta Mahesh,Reddy, Padi Pratap
p. 1979 - 1982
(2005)
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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.
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Paragraph 0099; 0100; 0101; 0109

(2019/05/28)

One-pot method for preparing irbesartan
The invention discloses a one-pot method for preparing irbesartan. The method comprises the following steps: with 2-butyl-1,3-diazaspiro[4,4]non-1-ene-4-one hydrochloride and 2-cyano-4'-bromomethylbiphenyl as raw materials, performing a reaction in an aprotic solvent containing an alkaline solution, performing an alkylation reaction under the action of a phase transfer catalyst to obtain 2-butyl-3-[(2'-cyano-1,1'-biphenyl-4-yl)methyl]-1,3-diazaspiro[4,4]non-1-ene-4-one, and performing a cyclization reaction on the 2-butyl-3-[(2'-cyano-1,1'-biphenyl-4-yl)methyl]-1,3-diazaspiro[4,4]non-1-ene-4-one and sodium azide under the action of a cyclization catalyst to obtain the irbesartan. The method has the advantages of simple operation, a short reaction time, high yield, high purity and suitability for industrial production.
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Paragraph 0026-0034

(2018/12/13)

Nickel-Catalyzed Denitrogenative ortho-Arylation of Benzotriazinones with Organic Boronic Acids: an Efficient Route to Losartan and Irbesartan Drug Molecules
Denitrogenative ortho-arylation, vinylation and methylation of 1,2,3-benzotriazin-4-(3H)-ones with organic boronic acids catalyzed by nickel complexes to give a wide range of o-substituted benzamides were demonstrated. Further, the catalytic reaction is successfully applied to the synthesis of the popular hypertensive drugs losartan and irbesartan in high yields. (Figure presented.).
Thorat, Vijaykumar H.,Upadhyay, Nitinkumar Satyadev,Cheng, Chien-Hong
p. 4784 - 4789
(2018/11/10)

Syntheses of 5-substituted 1H-tetrazoles catalyzed by reusable Cu(II)-NaY zeolite from nitriles
Cu(II)-NaY heterogeneous catalyst is used for the synthesis of 5-substituted 1H-tetrazoles by [2+3]-cycloaddition of sodium azide and nitriles. The salient features of this process are low reaction times, mild reaction conditions and high yields. The catalyst is recovered and reused for several cycles with consistent activity.
Sudhakar,Purna Chandra Rao,Prem Kumar,Suresh,Ravi
p. 864 - 866
(2017/02/10)

Preparation method of irbesartan isomer and irbesartan intermediate
The invention relates to a preparation method of an irbesartan isomer and an irbesartan condensation compound isomer as an irbesartan intermediate. The method comprises the following steps: 1) a phase transfer catalyst and an organic solvent are added to an irbesartan ring compound hydrochloride and biphenyl bromide, a sodium hydroxide solution is added, a reaction liquid is filtered after sufficient reaction of the raw materials, a filter cake is subjected to column chromatographic separation, and the irbesartan condensation compound isomer is obtained; 2) triethylamine hydrochloride, sodium azide and an organic solvent A are added to the irbesartan condensation compound isomer, the materials are heated to 100-130 DEG C and reacted, the sodium hydroxide solution and an organic solvent B are added, the mixture is stirred, left to stand and subjected to organic layer removal, hydrochloric acid is added to an aqueous-layer solution to regulate pH to 3.5-6.0, the solution is stirred and filtered, a filter cake is subjected to recrystallization with an organic solvent C or subjected to column chromatographic separation, and the irbesartan isomer is obtained. The irbesartan isomer impurity and the irbesartan intermediate prepared with the method have higher purity and lower energy consumption and cost. Meanwhile, the preparation method is simple to operate and environment-friendly and has important value in irbesartan production and research.
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Paragraph 0031; 0033

(2017/01/02)

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.
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(2015/09/23)

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.
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(2015/02/05)

Novel and efficient debenzylation of N-benzyltetrazole derivatives with the rosenmund catalyst
The Rosenmund catalyst (Pd/BaSO4) was found to efficiently catalyze debenzylation of N-benzyltetrazole derivatives with ammonium formate by catalytic transfer hydrogenation under mild conditions. The protocol has been applied to functionalized substrates to provide various angiotensin II receptor blockers in excellent yields.
Seki, Masahiko
p. 3249 - 3255
(2015/01/08)

AN IMPROVED PROCESS FOR PREPARATION OF IRBESARTAN
The present invention relates to an improved process for the preparation of 2-butyl-3-[[2'- (2H-tetrazol5yl[1,1'-biphenyl]-4-yl]methyl]-1,3-diazaspiro[4.4]non-1-en-4-one, the compound of formula I (Irbesartan) comprising reacting 4'-[(2-butyl-4-oxo-1,3- diazaspiro[4.4]non-1-en-3-yl)methyl]-[1,1'-biphenyl]-2-carbonitrile, the compound of formula II (cyano Irbesartan) with sodium azide, 1,8-Diazabicyclo[5.4.0]undec-7-ene (DBU) as a catalyst and triethylamine hydrochloride in an organic solvent at a temperature of 120- 140°C.
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Page/Page column 9

(2013/12/03)

NOVEL ZINC AZIDE COMPLEX AND A PROCESS FOR PREPARING TETRAZOLE DERIVATIVES USING THE SAME
The present invention relates to a novel zinc azide complex. The present invention also relates to a process for preparing 5-substituted-1H-tetrazole derivatives from nitrile derivatives by using the zinc azide complex. According to the present invention, in particular, pharmaceutically active compounds for treating hypertension or intermediates useful for preparation thereof can be prepared effectively.
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Page/Page column 13-14

(2012/11/13)

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
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Page/Page column 38-39

(2012/09/22)

PROCESS FOR THE PREPARATION OF IRBESARTAN
The present invention relates to a process for the preparation of 2-butyl-3-[[2′-(1H-tetrazol-5-yl)[1,1′-biphenyl]-4-yl]-1,3-diazaspiro[4,4]non-1-en-4-one by reaction of the corresponding nitrile with sodium azide and piperazine or its acid salt.
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Page/Page column 2

(2011/11/13)

PROCESS FOR IRBESARTAN SUBSTANTIALLY FREE OF DIMMER IMPURITY
The present invention provides a process for the preparation of irbesartan substantially free of 3-((2'-(1-((2'-(1H-tetrazol-5-yl)biphenyl-4-yl)methyl)-1H- tetrazol-5-yl)biphenyl-4-yl)methyl)-2-butyl-1,3-diazaspiro[4.4]non-1-en-4-one (or) 3- ((2'-(2-((2'-(1H-tetrazol-5-yl)biphenyl-4-yl)methyl)-2H-tetrazol-5-yl)biphenyl-4- yl)methyl)-2-butyl-1,3-diazaspiro[4.4]non-1-en-4-one impurity.
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Page/Page column 7

(2011/10/13)

Synthesis of amido-N-imidazolium salts and their applications as ligands in suzuki-miyaura reactions: Coupling of hetero- aromatic halides and the synthesis of milrinone and irbesartan
A new catalytic system based on palladium-amido-N-heterocyclic carbenes for Suzuki-Miyaura coupling reactions of heteroaryl bromides is described. A variety of sterically bulky, amido-N-imidazolium salts were synthesized in high yields from the corresponding anilines. This catalytic system effectively promoted Suzuki-Miyaura couplings of heteroaryl bromides and chlorides with a range of boronic acids to give the corresponding aryl compounds in high yield. The yield was increased with increasing steric bulkiness of the substituted group. Especially, 1-(2,6-diisopropylphenyl)-3-N-(2,4,6-tri-tert- butylphenylacetamido)imidazolium bromide (4bc) exhibited 850,000 TON in the coupling reaction of 2-bromopyridine and phenylboronic acid. In addition, pharmaceutical compounds such as milrinone and irbesartan were synthesized via Suzuki-Miyaura coupling using sterically bulky, amido-N-imidazolium salt (4bc) as a ligand. Copyright
Kumar, Manian Rajesh,Park, Kyungho,Lee, Sunwoo
experimental part
p. 3255 - 3266
(2011/02/23)

PROCESS FOR PURE IRBESARTAN
The present invention provides an improved and commercially viable process for preparation of irbesartan intermediate, 1-[(2′-cyanobiphenyl-4-yl)methyl]-2-n-butyl-4-spirocyclopentane-2-imidazolin-5-one, substantially free of 1-[(2′-cyanobiphenyl-4-yl)methyl]-2-n-propyl-4-spirocyclopentane-2-imidazolin-5-one impurity, thereby producing irbesartan substantially free of the undesired propyl analog impurity, namely 2-propyl-3-[[2′-(1H-tetrazol-5-yl)[1,1′-biphenyl]-4-yl]methyl]-1,3 -diazaspiro[4.4]non-1-en-4-one. The present invention also provides a process for preparation of irbesartan substantially free of tin content. The present invention further provides a commercially viable process for preparation of irbesartan in high purity and in high yield.
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Page/Page column 4

(2010/09/18)

A ONE POT PROCESS FOR PREPARING 2-BUTYL-3-[[2'-(1H-TETRAZOL-5-YL)[1,1'-BIPHENYL]-4-YL]METHYL]-1,3-DIAZASPIRO [4, 4] NON-1-EN-4-ONE (IRBESARTAN)
A one pot process for the synthesis of Irbesartan comprising reacting 2-n-Butyl-1, 3-Diazaspiro [4, 4] Non -1-en-4-one (Formula III) and Bromomethyl Cyanobiphenyl (Formula IV) in the presence of base and water with the optional use of PTC to give formula II from which Irbesartan is obtained by reacting with sodium azide and triethylamine hydrochloride in the presence of a non polar solvent.
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Page/Page column 10-11

(2010/11/03)

PROCESS FOR PURE IRBESARTAN
The present invention provides an improved and commercially viable process for preparation of irbesartan intermediate, 1-[(2''-cyanobiphenyl-4-yl)methyl]-2-n-butyl-4-spirocyclopentane-2-imidazolin-5-one, substantially free of 1-[(2''-cyanobiphenyl-4-yl)methyl]-2-n-propyl-4-spirocyclopentane-2-imidazolin-5-one impurity, thereby producing irbesartan substantially free of the undesired propyl analog impurity, namely 2-propyl-3-[[2''-(1H-tetrazol-5-yl)[1,1''-biphenyl]-4-yl]methyl]-1,3-diazaspiro[4.4]non-1-en-4-one. The present invention also provides a process for preparation of irbesartan substantially free of tin content. The present invention further provides a commercially viable process for preparation of irbesartan in high purity and in high yield.
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Page/Page column 9-10

(2009/07/17)

PROCESS FOR THE PREPARATION OF IRBESARTAN AND INTERMEDIATE PRODUCTS
The present invention relates to a new method for the production of irbesartan, having the chemical name 2-n-butyl-4-spirocyclopentane-1-[(2'-(tetrazol-5-yl)biphenyl-4-yl)methyl]-2- imidazolin-5-one, and pharmacologically acceptable salts thereof. Furthermore the invention relates to new (intermediate) compounds which are suitable for the production of irbesartan.
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Page/Page column 14-15

(2010/01/07)

IMPROVED PROCESS FOR PREPARING IRBESARTAN
Disclosed herein is an improved, commercially viable and industrially advantageous process for the preparation of Irbesartan, or a pharmaceutically acceptable salt thereof, in high yield and purity.
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Page/Page column 8-10

(2008/12/07)

A novel and improved process for the preparation of Irbesartan, an angiotensin-II receptor antagonist for the treatment of hypertension
2-Butyl-3-[[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-1,3-diaza-spiro[4,4]non-1-en-4-one (Irbesartan) is prepared by reacting 1-(2'-cyanobipehnyl-4-yl)methyl)-2-n-butyl-4-spirocyclopentane-2-imidazolin-5-one with sodium azide and zinc halide, in organic solvent.
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Page/Page column 3-4

(2008/12/04)

METHOD FOR PRODUCING PURE CRYSTALLINE FORM OF 2-N-BUTYL-3-((2-(1H-TETRAZOLE-5-YL) (1,1'-BIPHENYL)-4-METHYL)-1,3-DIAZAPSPIRO (4,4') NON -1- EN-4-ONE
Method for producing pure 2-n-Butyl-3-(2-(1H-tetrazole-5yl) (1,1'-biphenyl)-4-yl) methyl)-1,3-diazaspiro(4,4')non-1-en-4-one that is known as Irbesartan, in crystalline form A starting from crude Irbesartan, by controlling the cooling rate of the purification step.
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Page/Page column 5

(2008/06/13)

INTERMEDIATE COMPOUNDS FOR THE PREPARATION OF ANGIOTENSIN II ANTAGONISTS
The present invention relates to novel substituted biphenyltetrazole compounds useful as intermediates in the preparation of angiotensin II antagonists, to a process for the synthesis of them and to a process for the conversion thereof to said molecules.
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Page/Page column 33

(2010/11/30)

PROCESSES FOR THE SYNTHESIS OF 5-PHENYL -1 TRITYL-1H-TETRAZOLE
Provided are processes for the synthesis of 5 -phenyl- 1-trityl-lH-tetrazole, an intermediate useful in the synthesis of irbesartan.
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Page/Page column 21

(2010/11/30)

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)

INTERMEDIATE COMPOUNDS FOR THE PREPARATION OF ANGIOTENSIN II RECEPTOR ANTAGONISTS
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Page/Page column 16

(2008/12/05)

AN IMPROVED PROCESS FOR THE PREPARATION OF IRBESARTAN
The present invention relates to an improved process for the preparation of 2-n-butyl-3-[[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]-1,3-diazaspiro[4.4]non-1-en-4-one (Irbesartan)
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(2008/06/13)

Improved methods for the synthesis of irbesartan, an antihypertensive active pharmaceutical ingredient
New methods for the preparation of irbesartan 1 have been described. The dehydration and tetrazole formation in one step from substituted cyclopentane derivative 7 with tributyltin chloride and sodium azide is described. Selective hydrolysis of nitrile 3 with HCl has also been described in the preparation of N-acylaminocyclopentane-2-carboxylic acid 4, which is the key intermediate for the preparation of irbesartan. The impurity profiling of irbesartan has also been discussed. Copyright Taylor & Francis Group, LLC.
Rao, Korrapati V. V. Prasada,Dandala, Ramesh,Handa, Vijay K.,Rao, Inti V. Subramanyeswara,Rani, Ananta,Naidu, Andra
p. 2897 - 2905
(2008/02/13)

A novel approach for the conversion of primary amides into tetrazoles by using tributyltin chloride and sodium azide in the presence of DMF
A novel and efficient one-pot synthesis of tetrazole derivatives such as Irbesartan and its analogues has been described from the primary acid amide derivatives. Thus 2-alkyl-3-[p-(o-ami-dophenyl (benzyl]-1.3-diazaspiro[4.4]non- 1-en-4-one derivatives or 4-[α-(acylamino)cyclopentamidomethyl]-2′- carboxamidobiphenyl derivatives were treated with tributyltin chloride and sodium azide in o-xylene in the presence of DMF to afford irbesartan and its analogues without generation of nitriles. The synthesis of these new starting materials is also described, and two of the derivatives have been used as new intermediates in the preparation of irbesartan. Georg Thieme Verlag Stuttgart.
Prasada Rao, Korrapati V. V.,Dandala, Ramesh,Handa, Vijay K.,Subramanyeswara Rao, Inti V.,Rani, Ananta,Shivashankar, Sripelly,Naidu, Andra
p. 1289 - 1293
(2008/02/07)

PROCESS FOR THE PREPARATION OF PURE IRBESARTAN
A new process for the preparation of irbesartan was developed, which consist of converting irbesartan into salt, removing the impurities, and again converting into irbesartan to ensure purity greater than 99.7%.
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Page/Page column 10-11

(2008/06/13)

Process for preparation of Irbesartan
A process for the preparation of Irbesartan of formula (I) using the steps of: (i) reacting 4′ aminomethyl-2-cyano biphenyl of formula (VI) with 1-veleramido cyclopentane carboxylic acid of formula (V) ?in an organic solvent and in the presence of an acid, without activating the —COOH group of compound of formula (V) to give 1-(2′cyanobiphenyl-4-yl-methylaminocarbonyl)-1-pentanoylamino cyclopentane of formula (VII). ?converting the compound of formula (VII) obtained in step (i) to Irbesartan of formula (I) by reacting the compound of the formula (VII) with tributyl tin azide in o-xylene to give Irbesartan of formula (I).
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Page/Page column 12-13

(2008/06/13)

AN IMPROVED PROCESS FOR PREPARATION OF IRBESARTAN
A process for the preparation of Irbesartan of formula (I): Formula (I) comprising the steps of: (i) reacting 4' aminomethyl-2-cyano biphenyl of formula (VI) with 1-veleramido cyclopentane carboxylic acid of formula (V): Formula (VI) and Formula (V) in an organic solvent and in the presence of an acid, without activating the -COOH group of compound of formula (V) to give 1-(2'cyanobiphenyl-4-yl-methylaminocarbonyl)-1-pentanoylamino cyclopentane of formula (VII). Formula (VII) converting the compound of formula (VII) obtained in step (i) to Irbesartan of formula (I) by reacting the compound of the formula (VII) with tributyl tin azide in o-xylene to give Irbesartan of formula (I).
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Page/Page column 20-21; 22; 23

(2008/06/13)

A PROCESS FOR THE PREPARATION OF IRBESARTAN FORM A
The present invention relates to a process for the preparation of Irbesartan Form-A by crystallization in water & water miscible solvent having the ratio 1 :99 to 99: 1.
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Page/Page column 5

(2008/06/13)

PROCESS FOR PRODUCING 2-(N-BUTYL)-3-[[2'-(TETRAZOL-5-YL)BIPHENYL- 4-YL]METHYL]-l,3-DIAZASPIRO[4.4] NON-1-EN-4-ONE
Disclosed herein a process for producing 2- (n-butyl) -3- [ [2’ - (tetrazol-5-yl)biphenyl-4-yl]methyl] -1,3 -diazaspiro [4.4] non-l-en-4 -one of formula (I) in pure form by using selective solvent system and cost efficient raw materials and reagents.
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Page/Page column 9

(2010/11/25)

Process for preparing an angiotensin II receptor antagonist
Process for preparing irbesartan, protected forms for the preparation thereof, or a pharmaceutically acceptable salt thereof, that comprises the reaction between a biphenylamino derivative and an oxazolone derivative.
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Page/Page column 8

(2010/11/25)

A new entry to antihypertensive active pharmaceutical ingredient, Irbesartan and its analogues
A new synthesis of Irbesartan, an antihypertensive active pharmaceutical ingredient and its analogues is reported.
Satyanarayana, Bollikonda,Sumalatha, Yasareni,Sridhar, Chaganti,Venkatraman, Sundaram,Reddy, Padi Pratap
p. 323 - 328
(2007/10/03)

Novel and expeditious microwave-assisted three-component reactions for the synthesis of spiroimidazolin-4-ones
Highly efficient methods for the syntheses of spiroimidazolinones via microwave-assisted three-component one-pot sequential reactions or one-pot domino reactions are described. The efficiency and utility of the methods have been demonstrated by quickly accessing the antihypertensive drug irbesartan (2).
Ye, Ping,Sargent, Katie,Stewart, Ethan,Liu, Ji-Feng,Yohannes, Daniel,Yu, Libing
p. 3137 - 3140
(2007/10/03)

Method for preparing irbesartan and intermediates thereof
A method for preparing irbesartan and intermediates thereof. Irbesartan has the structure of formula I,
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Page/Page column 3; 5

(2008/06/13)

PROCESS FOR THE SYNTHESIS OF TETRAZOLES
A process for the synthesis of tetrazol derivative has been developed which starts from a tetrazole derivative where acidic hydrogen atom has been replaced by a protecting group and the deprotection is performed with a catalytic amount of organic acid and can proceed in an aqueous solvent.
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Page/Page column 9

(2008/06/13)

IRBESARTAN POLYMORPHS
The present invention relates to novel hydrate of irbesartan, amorphous irbesartan hydrate and pharmaceutical compositions containing them. The present invention also relates to novel processes for preparing crystalline form-A, crystalline form-B and amorphous form of irbesartan. Thus, for example, irbesartan and water are stirred for 15 minutes, cooled to 5°C and pH is adjusted to 10.5 to 11 with 10% sodium hydroxide solution, the contents are stirred at 5°C - 10°C for 3 hours and the resulting solution is washed with methylene chloride, the aqueous solution is cooled to 5°C and the pH is adjusted to 5.0 with 10% HCl solution at 5°C - 10°C, and then the separated solid is filtered, washed with chilled water and dried to give amorphous irbesartan hydrate.
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Page/Page column 8

(2010/02/15)

PROCESS FOR THE PREPARATION OF IRBESARTAN HYDROCHLORIDE
The present invention is concerned with a process for the preparation of 2n-butyl-4-spirocyclopentane-1-[(2'-(tetrazol-5-yl)biphenyl-4-yl) methyl]-2-imidazolin-5-one hydrochloride, irbesartan hydrochloride, novel hydrated and anhydrous crystalline forms thereof, amorphous irbesartan hydrochloride, formulations containing the same, therapeutic uses thereof and methods of treatment employing the same. The process of the present invention is a one-pot process which comprises reacting intermediate compounds 2n-butyl-1, 3-diazaspiro [4,4] non-1-en-4-one and 5-(4' -bromomethyl-biphenyl-2-yl)-1-trityl-lH-tetrazole.
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Page/Page column 28-29

(2008/06/13)

PROCESS FOR PRODUCING BIPHENYL-TETRAZOLE COMPOUNDS
A process for producing biphenyl-tetrazole compounds in pure form by deprotecting compounds of the following formula (II): proposes to use acids in an alcohol-ketone-water mixture and/or a mixture of alcohol-alcohol-keton-water to remove the Ph3C-protecting group.
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Page/Page column 12-14

(2008/06/13)

METHOD FOR PRODUCING BIPHENYL-TETRAZOLE COMPOUNDS
A method for producing biphenyl-tetrazole compounds by deprotecting compounds of the formula (II) proposes to use hydroxylammonium salts to remove the Ph3C-protecting group.
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Page/Page column 14-15

(2008/06/13)

PREPARATION OF TETRAZOLE DERIVATIVE
The present invention relates to a process for the preparation of irbesartan or its pharmaceutically acceptable salts comprising a synthesis of trityl irbesartan by a reaction of 5-(4-(bromomethyl)biphenyl-2-yl)-1-(triphenylmethyl)tetrazole and 2-n-butyl-4-cyclopentane-2-imidazolin-5-one or a salt therof in an organic solvent in the presence of a phase transfer catalyst and a base, a removal of the protecting group and an isolation of irbesartan or its pharmaceutically acceptable salt.
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Page/Page column 10-11

(2008/06/13)

PROCESS FOR PREPARING IRBESARTAN
A process for preparing irbesartan comprises pentanoylation of cycloleucine in the presence of sodium hydroxide to form n-pentanoyl cycloleucine, condensing this product with 2-(4-aminomethyl phenyl) benzonitrile using dicyclohexyl carbodiimide and 1-hydroxy benzotriazole as a catalyst to form the 4-(?-N-pentanoyl amino) cyclopentamido methyl-2'-cyano biphenyl compound, and then cyclizing using trifluroacetic acid in the presence of an aromatic solvent to form cyano irbesartan. Cyano irbesartan is converted to irbesartan by reaction with tributyltin chloride and sodium azide in the presence of an aromatic solvent.
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Page/Page column 11-12

(2008/06/13)

PROCESSES FOR THE PREPARATION OF HIGHLY PURE IRBESARTAN
The present invention relates to processes for synthesis of highly pure irbesartan or pharmaceutically acceptable salts thereof.
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Page/Page column 8; 9; 11

(2010/02/11)

CONVERSION OF AROMATIC NITRILES INTO TETRAZOLES
The present invention relates to the conversion of aromatic nitriles to tetrazoles, comprising treatment of the cyano compound with trialkyltin chloride and sodium azide optionally in the presence of a phase transfer catalyst. The process is particularly useful in the perparation of Irbesartan,Candesartan, Losartan and Valsartan.
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Page/Page column 17

(2008/06/13)

Phenyltetrazole compounds
Novel phenyltetrazole compounds useful as intermediates in the preparation of angiotensin II antagonists and the processes for the conversion thereof to biologically active molecules.
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Page/Page column 6-7

(2010/02/12)

A METHOD OF REMOVING THE TRIPHENYLMETHANE PROTECTING GROUP
A method of removing the triphenylmethane protecting group from 1-triphenylmethyl-5-(4'-subst. methyl-1,1‘-biphenyl-2-yl)-1H-tetrazoles of general formula I wherein R represents the groups of formulae and where R1, R2 and R3 can be H, a halogen, an unbranched or branched C1-C5 alkyl, C1-C5 hydroxyalkyl, Cl-C5 alkoxy, C1-C5 alkoxymethyl or benzyl, or wherein R2 and R3 can form together a saturated or unsaturated C5-C7 ring, optionally an unsubstituted or substituted aromatic ring, is carried out by solvolysis in a simple anhydrous Cl to C5 alcohol in a neutral or slightly basic medium. The method is suitable for the preparation of drugs, such as the potassium salts of losartan, irbesartan or valsartan or candesartan cilexetil.
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Page/Page column 14-15

(2008/06/13)

PROCESS FOR PRODUCTION OF TETRAZOLYL COMPOUNDS
The present invention relates to processes for the production of tetrazolyl compounds including removing protective groups from an N-protected tetrazolyl compound with organic acids, giving a high yield of the tetrazolyl compound. The compounds produced in accordance with the processes provided can be useful as therapeutic aspects for hypertension, circulatory diseases, such as heart failure, strokes, cerebral apoplexy, nephropathy and nephritis.
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Page/Page column 13

(2008/06/13)

Chemical Properties

Appearance/Colour :white crystalline powder
Melting Point: 180-181 °C
Boiling Point: 648.6 °C at 760 mmHg
Flash Point:346 °C
Density: 1.3 g/cm³
Solubility:DMSO: >25mg/mL
Storage Temp.:-20°C Freezer
Vapor Pressure: 1.05E-16mmHg at 25°C
Refractive Index: 1.689
PKA: 4.16±0.10(Predicted)
Merck: 14,5083
PSA: 87.13000
LogP: 4.15090

Global suppliers and manufacturers of 138402-11-6total 286 suppliers on LookChem

Company Name
Business Type
Min Order
FOB Price
Main Products
Contact

Nanjing Yuance Industry&Trade Co., Ltd.
Business Type:Manufacturers
Min Order:1 Metric Ton
FOB Price:No Data
Main Products:23
Country:

Zhejiang Huili Pharmaceutical Co., Ltd
Business Type:Trading Company
Min Order:1 Kilogram
FOB Price:No Data
Main Products:27
Country:

Sinoway Industrial Co., Ltd.
Business Type:Trading Company
Min Order:1 Kilogram
FOB Price:No Data
Main Products:105
Country:

Kono Chem Co.,Ltd
Business Type:Other
Min Order:1 Kilogram
FOB Price:USD $ 10.0-100.0 / Kilogram
Main Products:86
Country:

Hangzhou JINLAN Pharm-Drugs Technology Co., Ltd
Business Type:Manufacturers
Min Order:1 Gram
FOB Price:No Data
Main Products:86
Country:

Hebei yanxi chemical co.,LTD.
Business Type:Manufacturers
Min Order:1 Metric Ton
FOB Price:USD $ 1.0-3.0 / Metric Ton
Main Products:84
Country:

Wuhan Fortuna Chemical Co.,Ltd
Business Type:Trading Company
Min Order:25 Kilogram
FOB Price:USD $ 110.0-120.0 / Kilogram
Main Products:51
Country:

Ality Chemical Corporation
Business Type:Other
Min Order:1
FOB Price:No Data
Main Products:165
Country:

Xi'an Xszo Chem Co., Ltd.
Business Type:Manufacturers
Min Order:1 Gram
FOB Price:USD $ 0.1-0.1 / Gram
Main Products:108
Country:

Enke Pharma-tech Co.,Ltd. （Cangzhou, China ）
Business Type:Manufacturers
Min Order:1 Kilogram
FOB Price:USD $ 1.0-1.0 / Kilogram
Main Products:53
Country:

Shandong Jiulong Hisince Pharmaceutical Co.,Ltd.
Business Type:Manufacturers
Min Order:1 Kilogram
FOB Price:No Data
Main Products:29
Country:

COLORCOM LTD.
Business Type:Manufacturers
Min Order:1 Metric Ton
FOB Price:No Data
Main Products:32
Country:

Dayang Chem (Hangzhou) Co.,Ltd.
Business Type:Lab/Research institutions
Min Order:1 Kilogram
FOB Price:USD $ 3.0-3.0 / Kilogram
Main Products:994
Country:

Chemwill Asia Co., Ltd.
Business Type:Manufacturers
Min Order:5 Kiloliter
FOB Price:USD $ 1.2-5.0 / Kiloliter
Main Products:56
Country:

LIDE PHARMACEUTICALS LIMITED
Business Type:Lab/Research institutions
Min Order:1 Kilogram
FOB Price:USD $ 0.9-1.0 / Kilogram
Main Products:56
Country:

Hebei Nengqian Chemical Import and Export Co., LTD
Business Type:Trading Company
Min Order:1 Kilogram
FOB Price:USD $ 1.0-10.0 / Kilogram
Main Products:165
Country:

Henan Tianfu Chemical Co., Ltd.
Business Type:Lab/Research institutions
Min Order:1 Kilogram
FOB Price:No Data
Main Products:67
Country:

Zhuozhou Wenxi import and Export Co., Ltd
Business Type:Trading Company
Min Order:1 Kilogram
FOB Price:USD $ 139.0-210.0 / Kilogram
Main Products:1
Country:

Hebei Sankai Chemical Technology Co., Ltd
Business Type:Trading Company
Min Order:1 Kilogram
FOB Price:USD $ 7.0-10.0 / Kilogram
Main Products:11
Country:

Henan Sinotech Import&Export Corporation
Business Type:Other
Min Order:1 Metric Ton
FOB Price:USD $ 1.0-1.0 / Metric Ton
Main Products:21
Country:

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Article Database

138402-11-6

Articles about 138402-11-6Total 57 be found

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Chemical Properties

Appearance/Colour :white crystalline powder

Melting Point: 180-181 °C

Boiling Point: 648.6 °C at 760 mmHg

Flash Point:346 °C

Density: 1.3 g/cm³

Solubility:DMSO: >25mg/mL

Storage Temp.:-20°C Freezer

Vapor Pressure: 1.05E-16mmHg at 25°C

Refractive Index: 1.689

PKA: 4.16±0.10(Predicted)

Merck: 14,5083

PSA: 87.13000

LogP: 4.15090

Global suppliers and manufacturers of 138402-11-6total 286 suppliers on LookChem

Article Database

138402-11-6

Articles about 138402-11-6Total 57 be found

More Articles about upstream products of 138402-11-6

Chemical Properties

Appearance/Colour :white crystalline powder

Melting Point: 180-181 °C

Boiling Point: 648.6 °C at 760 mmHg

Flash Point:346 °C

Density: 1.3 g/cm3

Solubility:DMSO: >25mg/mL

Storage Temp.:-20°C Freezer

Vapor Pressure: 1.05E-16mmHg at 25°C

Refractive Index: 1.689

PKA: 4.16±0.10(Predicted)

Merck: 14,5083

PSA: 87.13000

LogP: 4.15090

Global suppliers and manufacturers of 138402-11-6total 286 suppliers on LookChem

Density: 1.3 g/cm³