139481-58-6

Basic information

• Product Name: Ethyl -2-ethoxy-1-[[(2-(1Htetrazol-5-yl)biphenyl-4-yl-) methyl]
• Synonyms: Ethyl -2-ethoxy-1-[[(2-(1Htetrazol-5-yl)biphenyl-4-yl-) methyl];Candesartan Ethyl Ester;1H-BenziMidazole-7-carboxylicacid,2-ethoxy-1-[[2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]Methyl]-,ethylesteror2-Ethoxy-1-[[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]Methyl]-,1H-benziMidazole-7-carboxylicethylester;2-Ethoxy-1-[[2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-1H-benzimidazole-7-carboxylic acid ethyl ester;Candesartan Cilexetil EP IMpurity A;1H-BenziMidazole-7-carboxylic acid, 2-ethoxy-1-[[2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]Methyl]-, ethyl ester;Candesartan ester;Ethyl 1-((2'-(2H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-c
• CAS NO: 139481-58-6
• Molecular Formula: C₂₆H₂₄N₆O₃
• Molecular Weight: 468.52
• Product Categories: Candesartan Cilexetil;Aromatics;Bases & Related Reagents;Heterocycles;Intermediates & Fine Chemicals;Nucleotides;Pharmaceuticals
• Mol File: 139481-58-6.mol

Chemical Properties

• Melting Point: 157-159°C
• Boiling Point: 709.56 °C at 760 mmHg
• Flash Point: 382.928 °C
• Appearance: Off-White Solid
• Density: 1.33
• Storage Temp.: Refrigerator
• Solubility: Chloroform (Slightly), Ethyl Acetate (Slightly, Sonicated), Methanol (Slightly)
• PKA: 4.15±0.10(Predicted)
• CAS DataBase Reference: Ethyl -2-ethoxy-1-[[(2-(1Htetrazol-5-yl)biphenyl-4-yl-) methyl](CAS DataBase Reference)
• NIST Chemistry Reference: Ethyl -2-ethoxy-1-[[(2-(1Htetrazol-5-yl)biphenyl-4-yl-) methyl](139481-58-6)
• EPA Substance Registry System: Ethyl -2-ethoxy-1-[[(2-(1Htetrazol-5-yl)biphenyl-4-yl-) methyl](139481-58-6)

Safety Data

• Hazardous Substances Data: 139481-58-6(Hazardous Substances Data)

Usage

Uses

Used in Pharmaceutical Industry:
Ethyl -2-ethoxy-1-[[(2-(1Htetrazol-5-yl)biphenyl-4-yl-) methyl] is used as a Candesartan analog for its role as an angiotensin II antagonist. The application reason is that it can potentially help in the treatment of hypertension and heart failure by blocking the effects of angiotensin II, a hormone that narrows blood vessels and increases blood pressure.
Used in Chemical Research:
In the field of chemical research, Ethyl -2-ethoxy-1-[[(2-(1Htetrazol-5-yl)biphenyl-4-yl-) methyl] can be used as a starting material or intermediate for the synthesis of other complex organic compounds. The application reason is its unique molecular structure, which can be further modified or functionalized to create new compounds with specific properties and applications.
Used in Drug Development:
Ethyl -2-ethoxy-1-[[(2-(1Htetrazol-5-yl)biphenyl-4-yl-) methyl] may also be used in drug development as a potential candidate for the treatment of various diseases. The application reason is its ability to act as an angiotensin II antagonist, which could lead to the development of new drugs for hypertension, heart failure, and other related conditions.

Upstream product

• 3970-35-2 2-chloro-3-nitrobezoic acid 
• 3979-45-1 ethyl 2-chloro-3-nitrobenzoate 
• 854538-89-9 ethyl 2-(4-bromobenzylamine)-3-nitrobenzoate 
• 916891-90-2 ethyl 3-amino-2-(4-bromobenzylamine)-benzoate 
• 139481-41-7 ethyl 1-[(2'-cyano-[1,1']-biphenyl-4-yl)methyl]-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate 
• 916891-91-3 ethyl 2-ethoxy-1-[[2'-[(1-methyl-1-phenyl-ethyl)-2H-tetrazol-5-yl]-[1,1']biphenyl-4-yl]methyl]-1H-benzoimidazole-7-carboxylate 
• 854538-88-8 ethyl 1-(4-bromobenzyl)-2-ethoxy-benzimidazole-7-carboxylate 
• 155884-01-8 (2-(2H-tetrazol-5-yl)phenyl)boronic acid 
• 1118-03-2 trimethyltin azide 

Downstream Products

• 139481-59-7 candesartan 
• 139481-72-4 2-Ethoxy-1-[[2'-(N-triphenylmethyltetrazol-5-yl)-biphenyl-4-yl]methyl]benzimidazole-7-carboxylic acid 
• 170791-09-0 cilexetil trityl candesartan 
• 145040-37-5 candesartan cilexetil 

Relevant articles and documents

METHOD FOR PREPARING TRITYL CANDESARTAN

The present invention uses a candesartan cyclic compound as a starting material and performs thereon a three-step reaction of forming tetrazole, hydrolysis and adding a protecting group to directly obtain trityl candesartan without separating an intermediate product via crystallization. The operating process is simple and thus is more applicable to industrial production.

ONE POT PROCESS FOR THE PREPARATION OF CANDESARTAN

Present invention is to provide one pot synthesis of candesartan without isolating the ester intermediate.

METHOD FOR OBTAINING BENZIMIDAZOLE DERIVATIVES AND INTERMEDIATES THEREOF

The present invention relates to a method for obtaining benzimizadole derivatives and intermediates thereof, preferably, for obtaining Candesartan and Candesartan cilexetil. Said method allows the benzimizadole derivatives to be obtained with a higher yield.

Process for the production of tetrazolyl compounds

Disclosed is a method for removing a protective group of an N-protected tetrazolyl compound which comprises reacting said N-protected tetrazolyl compound with a mineral acid under substantially anhydrous conditions in the presence of an alcohol, insuring a high reaction yield of the object tetrazolyl compound.

1-(CYCLOHEXYLOXYCARBONYLOXY)ETHYL 2-ETHOXY-1-[[2'-(1H-TETRAZOL-5-YL)BIPHENYL-4-YL]METHYL]BENZIMIDAZOLE-7-CARBOXYLATE AND COMPOSITIONS AND METHODS OF PHARMACEUTICAL USE THEREOF

1-(Cyclohexyloxycarbonyloxy)ethyl 2-ethoxy-1-[[2'-(1 H-tetrazol-5-y l)biphenyl-4-yl]methyl]benzimidazole-7-carboxylate or a pharmaceutically acceptable salt thereof has potent angiotensin II antihypertensive activity, thus being useful as therapeutic agents for treating circulatory system diseases such as hypertensive diseases, heart diseases (e.g. hypercardia, heart failure, cardiac infarction, etc.), strokes, cerebral apoplexy, nephritis, etc.