137862-87-4

Usage

Uses

Used in Pharmaceutical Industry:
Valsartan is used as an active pharmaceutical ingredient for the treatment of hypertension (high blood pressure). It functions as an angiotensin II receptor blocker, which helps in relaxing blood vessels and reducing blood pressure.
Used in Cardiovascular Applications:
In the field of cardiology, valsartan is utilized as a therapeutic agent for the management of heart failure and post-myocardial infarction (heart attack). Its ability to block angiotensin II receptors aids in improving heart function and reducing the risk of further cardiovascular events.
Used in Research and Development:
Valsartan is also used as a research compound in the development of new drugs and therapies related to hypertension and cardiovascular diseases. Its chemical properties and mechanism of action provide valuable insights for scientists working on novel treatments for these conditions.

InChI:InChI=1/C24H29N5O3/c1-4-5-10-21(30)29(22(16(2)3)24(31)32)15-17-11-13-18(14-12-17)19-8-6-7-9-20(19)23-25-27-28-26-23/h6-9,11-14,16,22H,4-5,10,15H2,1-3H3,(H,31,32)(H,25,26,27,28)/t22-/m1/s1

Upstream product

• 195062-57-8 p-tolylboronic pinacol ester 
• 138500-85-3 4-bromomethylphenylboronic acid pinacol ester 
• 137863-20-8 (S)-N-(1-benzyloxycarbonyl-2-methyl-prop-1-yl)-N-pentanoyl-N-[2'-(1H-tetrazol-5-yl)-biphenyl-4-ylmethyl]-amine 
• 676129-92-3 desvaleroyl valsartan 
• 638-29-9 n-valeryl chloride 
• 137864-44-9 N-[(2'-(1-triphenylmethyl-tetrazol-5-yl)biphenyl-4-yl)methyl]-N-valeroyl-(L)-valine benzyl ester 
• 443093-86-5 N-((2'-(cyano)-[1,1'-biphenyl]-4-yl)methyl)-N-pentanoyl-L-valine 
• 867022-57-9 (S)-2-[(4-bromo-benzyl)-pentanoyl-amino]-3-methyl-butyric acid 
• 943019-61-2 N-[4-(5,5-dimethyl-[1,3,2]dioxaborinan-2-yl)phenyl-4-yl-methyl]-N-pentanoyl-L-valinate 
• 143945-72-6 N-trityl-5-(2-bromophenyl)tetrazole 
• 137864-22-3 (S)-2-[(2'-cyanobiphenyl-4-ylmethyl)pentanoylamino]-3-methylbutyric acid benzyl ester 
• 1298055-63-6 C₂₉H₃₆N₂O₃ 
• 512182-37-5 1-(o-methoxybenzyl)-5-phenyl-1H-tetrazole 
• 1301606-99-4 1-((2'-(1-(2-methoxybenzyl)-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)oxy)propan-2-one 

Downstream Products

• 58-93-5 6-chloro-3,4-dihydro-2H-1,2,4-benzothiadiazine-7-sulfonamide 1,1-dioxide 
• 137863-43-5 (S)-N-((2'-(1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-N-(3-methyl-1-morpholino-1-oxobutan-2-yl)pentanamide 
• 1378237-69-4 (S)-2-((S)-2-(N-((2'-(1H-tetrazol-5-yl)biphenyl-4-yl)methyl)pentanamido)-3-methylbutanamido)-3-phenylpropanoic acid 

Relevant academic research and scientific papers

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.

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.

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)

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.

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.

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.

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.

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.