148674-39-9

Basic information

• Product Name: SB 206328
• Synonyms: (Z)-Eprosartan;(Z)-α-[[2-Butyl-1-[(4-carboxyphenyl)Methyl]-1H-iMidazol-5-yl]Methylene]-2-thiophenepropanoic Acid;(αZ)-α-[[2-Butyl-1-[(4-carboxyphenyl)Methyl]-1H-iMidazol-5-yl]Methylene]-2-thiophenepropanoic Acid;SB 206328;Eprosartan USP RC F;Eprosartan related coMpound F;Eprosartan Related Compound F: Eprosartan Cis-Isomer
• CAS NO: 148674-39-9
• Molecular Formula: C23H24N2O4S
• Molecular Weight: 424.51266
• Product Categories: Aromatics;Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals;Sulfur & Selenium Compounds
• Mol File: 148674-39-9.mol

Chemical Properties

• Boiling Point: 660.6±55.0 °C(Predicted)
• Appearance: /
• Density: 1.26±0.1 g/cm3(Predicted)
• PKA: 3.10±0.37(Predicted)
• CAS DataBase Reference: SB 206328(CAS DataBase Reference)
• NIST Chemistry Reference: SB 206328(148674-39-9)
• EPA Substance Registry System: SB 206328(148674-39-9)

Safety Data

• Hazardous Substances Data: 148674-39-9(Hazardous Substances Data)

Usage

Uses

Used in Pharmaceutical Industry:
SB 206328 is used as an impurity in tablets for the production of (Z)-Eprosartan. SB 206328 serves as an important component in the development and manufacturing of pharmaceutical products, particularly in the context of tablets.
Used in Research and Development:
SB 206328 is also utilized in research and development settings, where it is employed to study the properties and effects of (Z)-Eprosartan. This application aids in the advancement of knowledge and understanding of the compound, which can lead to improvements in its use and potential applications.

Upstream product

• 133040-03-6 2-n-butyl-1-[(4-carbomethoxyphenyl)methyl]-1H-imidazol-5-carboxaldehyde 
• 143468-96-6 3-ethoxy-3-oxo-2-(thien-3-ylmethyl)propanoic acid 
• 1104528-98-4 (E)-α-[[2-butyl-1-[(4-carboxyphenyl)methyl]-1H-imidazol-5-yl]methylene]-2-thiophene propanoic acid acetate 
• 133486-13-2 ethyl (αE)-α-[[2-n-butyl-1-[[4-(methoxycarbonyl)phenyl]methyl]-1H-imidazol-5-yl]methylene-2-thiophene]propionate 
• 16862-05-8 methyl 3-(2-thienyl)propanoate 
• 68282-49-5 2-n-butyl-1H-imidazole-4-carbaldehyde 
• 148674-60-6 2-(thienylmethyl)cyanoacetic acid 
• 133040-05-8 4-[5-(1-Acetoxy-2-methoxycarbonyl-3-thiophen-2-yl-propyl)-2-butyl-imidazol-1-ylmethyl]-benzoic acid methyl ester 
• 133040-04-7 2-butyl-1-(4-carbomethoxybenzyl)-5-<2-carbomethoxy-1-hydroxy-3-(2-thienyl)propyl>imidazole 
• 133040-06-9 methyl (E)-3-<2-butyl-1-<(4-carbomethoxyphenyl)methyl>imidazol-5-yl>-2-(2-thienylmethyl)-2-propenoate 
• 133040-02-5 2-butyl-4-chloro-1-<(4-carbomethoxyphenyl)methyl>-1H-imidazole-5-carboxaldehyde 
• 83857-96-9 2-n-butyl-4-chloro-1H-imidazol-5-carboxaldehyde 
• 2417-72-3 Methyl 4-(bromomethyl)benzoate 
• 133040-01-4 eprosartan 

Relevant articles and documents

Multicomponent Pharmaceutical Adducts of α-Eprosartan: Physicochemical Properties and Pharmacokinetic Study

Pharmaceutical adducts of α-eprosartan (EPR) with nicotinamide (NIC) and p-hydroxy benzoic acid (PHB) were prepared by a liquid assisted grinding technique. Prior to conducting this study, the single crystal structure of EPR was determined. This study was designed to improve the pH-dependent solubility and dissolution rate of EPR and hence its oral absorption across the gastrointestinal tract. Initially, differential scanning calorimetry and powder X-ray diffractometry were used as a screening tool for rapid cocrystal or eutectic mixture screening. The eutectic mixture of EPR with PHB in a 1:3 stoichiometry ratio shows a better solubility and dissolution rate in all aqueous buffers as compared to EPR/NIC cocrystals and pure EPR. The EPR/NIC cocrystal in a 1:1 stoichiometry ratio shows a better dissolution rate initially as compared to pure EPR but does revert back to EPR within the first 30 min in pH 1.2 and 6.8. Absorption and desorption profile of EPR adducts are reversible, suggesting no solid state transformation under experimental conditions. A significant increase in oral bioavailability in overnight fasted Sprague-Dawley rats is achieved with the EPR/NIC cocrystal (2.4-fold) and EPR/PHB eutectics (6.1-fold), even when the cocrystal transformation is suspected based on in vitro studies.

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 EPROSARTAN

Disclosed herein is an improved novel synthetic process for the preparation of Eprosartan, which comprises treating 2-n-butyl-4-formylimidazole of formula (II) with N-protecting group selected from the group consisting of C1-C4 alkyl ester derivative of m

AN IMPROVED PROCESS FOR THE PREPARATION OF PURE EPROSARTANAND ITS PHARMACEUTICAL ACCEPTABLE SALTS

The present invention relates to an improved process for preparation of pure Eprosartan and its pharmaceutical acceptable salts comprising the steps of: a) treating the Eprosartan with hydrochloric acid; b) suspending the resulted Eprosartan hydrochloride

PROCESS FOR EPROSARTAN INTERMEDIATE

The present invention provides an improved process for preparation of (E)-α-[[2-butyl-1-[[4-(methoxycarbonyl)phenyl]methyl]-1H-imidazole-5-yl]methylene]-2-thiophene propanoic acid ethyl ester in high purity and in high yield. Thus, for example, 4-[[2-buty

PHARMACEUTICAL FORMULATION CONTAINING ANGIOTENSIN-II RECEPTOR BLOCKER

The present invention provides a pharmaceutical formulation containing an angiotensin-II receptor blocker and a release-control material as a pharmacologically active ingredient and a pharmaceutical formulation comprising an immediate-release compartment and an extended-release compartment. The immediate-release compartment contains an agent as a pharmacologically active ingredient for preventing and inhibiting hepatitis and the extended-release compartment has an angiotensin-II receptor blocker as a pharmacologically active ingredient. The formulation of the present invention maximizes the effectiveness on pharmacologically and clinically lowering blood pressure and preventing complications when taking the formulation, helps to avoid interaction with a drug which is metabolized by the same enzyme in the liver, and prevents and inhibits the incidence of drug-induced hepatitis which is caused by drug administration for a long time.

AN IMPROVED PROCESS FOR THE PREPARATION OF EPROSARTAN

The present invention provides an improved process for the preparation of Eprosartan or its pharmaceutically acceptable salt comprising the steps of: condensing compound of formula (a) with compound of formula (b) in presence of a catalyst, in a solvent to get a compound of formula (c), and hydrolyzing the compound of formula (c) to get Eprosartan and optionally converting Eprosartan to its pharmaceutically acceptable salt. The present invention also relates to process for the preparation of compound of formula (c) by condensing compound of formula (a) with compound of formula (b) in presence of dehydrating agent.

Synthesis and biological evaluation of [carboxyl-11C]eprosartan

Essential hypertension occurs in approximately 25% of the adult population and one cause of hypertension is primary aldosteronism. Targeting the angiotensin II AT1 receptor using PET and an appropriate tracer may offer a diagnostic method for a

EPROSARTAN MESYLATE CRYSTALLINE PARTICLES AND A PROCESS FOR PREPARING PURE EPROSARTAN

The present invention relates to eprosartan mesylate particles having relatively larger surface area, to the methods for the manufacture of said crystalline particles, and to pharmaceutical compositions comprising said crystalline particles. The present i

IMPROVED PROCESS FOR EPROSARTAN INTERMEDIATE

The present invention provides an improved process for preparation of (E)-α-[[2-butyl-1-[[4-(methoxycarbonyl)phenyl]methyl]-1 H-imidazole-5-yl] methylene]-2-thiophene propanoic acid ethyl ester in high purity and in high yield. Thus, for example, 4-[[2-bu