144873-97-2

Usage

Uses

Used in Pharmaceutical Synthesis:
[2-[1-(TRIPHENYLMETHYL)-1H-TETRAZOL-5-YL]PHENYL]BORONIC ACID is used as a key component in the synthesis of potential pharmaceuticals. Its ability to form complexes with other molecules makes it a promising candidate for the development of new drugs with novel mechanisms of action.
Used in Chemical Research:
In the field of chemical research, [2-[1-(TRIPHENYLMETHYL)-1H-TETRAZOL-5-YL]PHENYL]BORONIC ACID is employed as a boronic acid derivative to study its interactions with various molecules. This helps researchers understand its potential applications and limitations in different chemical processes.
Used in Bioimaging as a Fluorescent Probe:
[2-[1-(TRIPHENYLMETHYL)-1H-TETRAZOL-5-YL]PHENYL]BORONIC ACID has been studied for its potential as a fluorescent probe in bioimaging. Its ability to form complexes with proteins or nucleic acids allows it to be used for tracking and visualizing specific biological processes, which can be crucial in understanding disease mechanisms and developing targeted therapies.
Used as a Catalyst in Organic Synthesis Reactions:
In organic synthesis, [2-[1-(TRIPHENYLMETHYL)-1H-TETRAZOL-5-YL]PHENYL]BORONIC ACID is utilized as a catalyst to facilitate various chemical reactions. Its unique structure enables it to improve the efficiency and selectivity of these reactions, leading to the production of desired compounds with fewer side products and less environmental impact.

Upstream product

• 154750-11-5 N-(triphenylmethyl)phenyltetrazole 
• 121-43-7 Trimethyl borate 
• 5419-55-6 Triisopropyl borate 
• 18039-42-4 5-Phenyl-1H-tetrazole 
• 76-83-5 trityl chloride 
• 100-47-0 benzonitrile 

Downstream Products

• 188714-71-8 5-[2-(3-Methyl-benzofuran-6-yl)-phenyl]-1-trityl-1H-tetrazole 
• 188714-62-7 5-[2-(1-Trityl-1H-tetrazol-5-yl)-phenyl]-benzofuran-2-carboxylic acid ethyl ester 
• 188714-68-3 5-[2-(3-Methyl-benzofuran-5-yl)-phenyl]-1-trityl-1H-tetrazole 
• 188714-82-1 5-[2-(2-Methyl-benzofuran-7-yl)-phenyl]-1-trityl-1H-tetrazole 
• 138402-11-6 2-butyl-3-{4-[2-(1H-tetrazol-5-yl)phenyl]benzyl}-1,3-diazaspiro[4.4]non-1-en-4-one 
• 138402-10-5 trityl irbesartan 
• 170791-09-0 cilexetil trityl candesartan 
• 1038921-12-8 (E)-2-((2-ethyl-7-methyl-3-((1S)-5-(2-(1-trityl-1H-tetrazol-5-yl)phenyl)-2,3-dihydro-1H-inden-1-yl)-3H-imidazo[4,5-b]pyridin-5-yl)methylene)cyclopentanone 
• 1038920-14-7 1-(2-ethyl-7-methyl-3-{(S)-5-[2-(1-trityl-1H-tetrazol-5-yl)-phenyl]-indan-1-yl}-3H-imidazo[4,5-b]pyridin-5-yl)-2-methyl-propan-1-one 
• 1038920-35-2 5-chloro-2-ethyl-7-methyl-3-((1S)-5-(2-(1-trityl-1H-tetrazol-5-yl)phenyl)-2,3-dihydro-1H-inden-1-yl)-3H-imidazo[4,5-b]pyridine 
• 1038921-00-4 1-(2-ethyl-7-methyl-3-((1S)-5-(2-(1-trityl-1H-tetrazol-5-yl)phenyl)-2,3-dihydro-1H-inden-1-yl)-3H-imidazo[4,5-b]pyridin-5-yl)-3-methylbutan-1-one 
• 1038921-07-1 2-ethyl-5-((5-ethyl-1,3,4-oxadiazol-2-yl)methyl)-7-methyl-3-((1S)-5-(2-(1-trityl-1H-tetrazol-5-yl)phenyl)-2,3-dihydro-1H-inden-1-yl)-3H-imidazo[4,5-b]pyridine 
• 1038921-09-3 (E)-2-((2-ethyl-7-methyl-3-((1S)-5-(2-(1-trityl-1H-tetrazol-5-yl)phenyl)-2,3-dihydro-1H-inden-1-yl)-3H-imidazo[4,5-b]pyridin-5-yl)methylene)cyclohexanone 
• 1038919-75-3 5-benzyl-2-ethyl-7-methyl-3-((1S)-5-(2-(1-trityl-1H-tetrazol-5-yl)phenyl)-2,3-dihydro-1H-inden-1-yl)-3H-imidazo[4,5-b]pyridine 

Relevant academic research and scientific papers

The synthesis of radiolabeled Irbesartan using N,N-dimethyl[ 14C]formamide as a source of carbon-14 isotope

Irbesartan (Avapro) is in clinical use as an antihypertensive drug. It is a nonpeptide angiotensin II receptor antagonist. A radiolabeled version of this drug, intended for use in environmental fate studies, was prepared from N,N-dimethyl[14C]f

DUAL-ACTING THIOPHENE, PYRROLE, THIAZOLE AND FURAN ANTIHYPERTENSIVE AGENTS

In one aspect, the invention relates to compounds having the formula:wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.

DUAL-ACTING OXAZOLE ANTIHYPERTENSIVE AGENTS

In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 re

DUAL-ACTING ANTIHYPERTENSIVE AGENTS

In one aspect, the invention relates to compounds having the formula: wherein: Ar, r, Z, X, R3, and R5-7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.

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.

METHOD FOR THE PRODUCTION OF LOSARTAN

The invention relates to a novel method for the production of losartan, an imidazol derivative with the chemical name 2-n-butyl-4-chloro-5-hydroxymethyl-1-{[2'-(1H-tetrazol-5-yl)biphenyl-4-]methyl}imidazol and the pharmacologically active salts thereof. The invention also relates to novel intermediate products which are suitable for the production of losartan, and to novel methods for the production of intermediate compounds which are suitable for the production of losartan. One aspect of the invention is a method for the production of a compound of general formula (I), which can arise as an intermediate step in the inventive representation of losartan.

METHOD FOR PRODUCTION OF CANDESARTAN

The invention relates to novel methods for the production of Candesartan, or a protected form of Candesartan, a Candesartan salt or ester, compounds of application in said method, methods for production thereof, use thereof in said method, a novel polymorph of Candesartan cilexetil, a method for production and use thereof for production of a medicament.

NOVEL SYNTHESIS OF IRBESARTAN

Provided are a method of making irbesartan via a Suzuki coupling reaction and a novel intermediate, 2-butyl-3-(4'-bromobenzyl)-1,3-diazaspiro[4.4]non-1-ene-4-one, for such process. The novel process includes the step of reacting such intermediate with a protected imidazolephenylboronic acid.

5-aryleheteroarylalkyl-1,3,5-trisubstituted-1,2,4-triazole compounds for treatment of circulatory disorders

A class of 5-arylheteroarylalkyl-1,3,5-trisubstituted-1,2,4-triazole compounds is described for use in treatment of circulatory disorders such as hypertension. Compounds of particular interest are angiotensin II antagonists of the formula wherein A is selected from wherein m is one; wherein R1 is selected from ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, 4-methylbutyl, n-pentyl, neopentyl, benzyl, cyclohexyl, cyclohexylmethyl, 2-butenyl, 3-butenyl, 2-butynyl, 3-butynyl and 2-hydroxybutyl; wherein R2 is selected from ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, 4-methylbutyl, tert-butyl, n-pentyl, neo-pentyl, 1-oxoethyl, 1-oxopropyl, 1-oxobutyl, 1-oxopentyl, 1,1-dimethoxypropyl, 1,1-dimethoxypentyl, halo, difluoromethyl, 1-oxo-2-phenylethyl, 1-oxo-2-cyclohexylethyl, 1,1-difluoro-2-phenylethyl, 1,1-difluoro-2-cyclohexylethyl, 2-cyclohexylethyl, 1,1-difluoro-3-cyclohexylpropyl, 1,1-dimethoxybutyl, 1,1-difluoroethyl, 1,1-difluoropropyl, 1,1-difluorobutyl, 1,1-difluoropentyl, benzyl, 2-phenylethyl, 1,1-difluoro-3-phenylpropyl, cyclohexylmethyl, cyclohexanoyl, 1-butenyl, 2-butenyl, 3-butenyl, 1-butynyl, 2-butynyl, 3-butynyl, propylthio and butylthio; wherein each of R3, R4, R6 through R11 is hydrido and R5 is selected from COOH, SH, PO3H2, SO3H, CONHNH2, CONHNHSO2CF3, OH, wherein each of R42 and R43 is independently selected from chloro, cyano, nitro, trifluoromethyl, methoxycarbonyl and trifluoromethylsulfonyl.

N-ARYLHETEROARYLALKYL IMIDAZOL-2-ONE COMPOUNDS FOR TREATMENT OF CIRCULATORY DISORDERS

A class of N-arylheteroarylalkyl imidazol-2-one compounds is described for use in treatment of circulatory disorders such as hypertension and congestive heart failure. Compounds of particular interest are angiotensin II antagonists of the formula STR1 wherein A is selected from STR2 wherein m is one; wherein R 1 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, 4-methylbutyl, 2-ethylbutyl, n-pentyl, neopentyl, phenyl, methylphenyl, difluorophenyl, benzyl, phenethyl, cyclohexyl, cyclohexylmethyl, cyclohexylethyl, cyclohexanoyl, 1-oxo-2-cyclohexylethyl, benzoyl, 1-oxo-2-phenethyl, 1-oxopropyl, 1-oxobutyl, 1-oxopentyl and 2-hydroxybutyl; wherein R 0 is hydrido; wherein R 2 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, isopentyl, neopentyl, phenyl, benzyl, phenethyl, cyclohexyl, cyclohexylmethyl, propylthio, butylthio, and hydroxyalkyl; wherein each of R 3, R 4, R 6, R 7, R. sup.8, R 9, R 10 and R. sup.11 is hydrido and R 5 must be selected from COOH, SH, P0 3 H. sub.2, SO 3 H, CONHNH 2, CONHNHSO 2 CF 3, OH, STR3 wherein each of R 42 and R 43 is independently selected from chloro, cyano, nitro, trifluoromethyl, methoxycarbonyl and trifluoromethylsulfonyl; or a tautomer thereof or a pharmaceutically-aceptable salt thereof.