1266741-05-2

Usage

Uses

Used in Pharmaceutical Industry:
Deferasirox Methyl Ester is used as an iron chelator for the treatment of iron overload in patients who have received multiple blood transfusions. It is designed to improve the oral bioavailability of deferasirox, making it a potential alternative treatment for patients who have difficulty tolerating the oral or intravenous administration of deferasirox. Its improved solubility and bioavailability may offer a promising option for the management of iron overload in certain patient populations.

Upstream product

• 65-45-2 salicylamide 
• 69-72-7 salicylic acid 
• 67-56-1 methanol 
• 201530-41-8 deferasirox 
• 1218-69-5 2-(2-hydroxyphenyl)-4H-benzo[e][1,3]oxazin-4-one 
• 4510-12-7 methyl 4-hydrazinobenzoate 
• 1642597-20-3 methyl 4-(3,5-dibromo-1H-1,2,4-triazol-1-yl)-benzoate 
• 269409-97-4 2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenol 
• 75-75-2 methanesulfonic acid 

Downstream Products

• 201530-41-8 deferasirox 
• 1414867-91-6 4-(5-(2-((4-boronobenzyl)oxy)phenyl)-3-(2-hydroxyphenyl)-1H-1,2,4-triazol-1-yl)benzoic acid 
• 1414867-92-7 4-(3-(2-hydroxyphenyl)-5-(2-((4-(3a,5,5-trimethylhexahydro-4,6-methanobenzo[d][1,3,2]dioxaborol-2-yl)benzyl)oxy)phenyl)-1H-1,2,4-triazol-1-yl)benzoic acid 
• 1414867-90-5 methyl 4-(3-(2-hydroxyphenyl)-5-(2-((4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzyl)oxy)phenyl)-1H-1,2,4-triazol-1-yl)benzoate 

Relevant academic research and scientific papers

In vitrostudies of deferasirox derivatives as potential organelle-targeting traceable anti-cancer therapeutics

We report here strategic functionalization of the FDA approved chelator deferasirox (1) in an effort to produce organelle-targeting iron chelators with enhanced activity against A549 lung cancer cells. Derivative 8 was found to have improved antiproliferative activity relative to 1. Fluorescent cell imaging revealed that compound 8 preferentially localises within the lysosome.

CELL ACTIVATABLE IRON CHELATORS

Provided herein are compounds of the formula (I): wherein the variables are as defined herein. Pharmaceutical compositions of the compounds are also provided. In some aspects, these compounds may be used for the treatment of diseases or disorders, such as

Excitation Wavelength Dependent Fluorescence of an ESIPT Triazole Derivative for Amine Sensing and Anti-Counterfeiting Applications

Excitation wavelength dependent (Ex-De) emission materials have potential applications in anti-counterfeiting labels and bioimaging. Nevertheless, few purely organic chromophores are used in these areas. In this study, multiple excited states were incorporated into a molecule that was excited state intramolecular proton transfer (ESIPT) active, with the goal of manipulating the relaxation pathways of the excited states. The triazole derivative exhibits Ex-De photoluminescence (PL), and the maximum PL wavelength is located at 526 nm and 593 nm under a series of excitation wavelengths. Spectral identification indicates that the excimer and ESIPT processes are responsible for the green (526 nm) and orange (593 nm) fluorescence, respectively. Importantly, the quick response code and test strip prepared with this triazole derivative can be used for anti-counterfeiting and food spoilage detection applications, respectively. This research opens the door for developing novel Ex-De materials for anti-counterfeiting purposes.

1,2,4-triazole compound, salt thereof and applications of compound and salt

The invention discloses a 1,2,4-triazole compound, salt thereof and applications of the compound and salt. The compound has a structural formula shown in the description, wherein R represents hydrogen, phenyl or substituted phenyl, and a substituted group of substituted phenyl is selected from carboxyl, an ester group, C1-4 alkyl, C1-4 alkoxy groups, C1-4 halogenated alkyl, C1-4 halogenated alkoxygroups, C2-4 alkynyl, halogen, cyano groups, acyl, nitryl or hydroxyl. The compound has high insecticidal activity for aphids, part of compound has the insecticidal activity for aphids equivalent tothat of a commercial insecticide dinotefuran, and the compound can be used for controlling lepidoptera pests, coleoptera pests, heteropteran pests, diptera pests, orthoptera pests and homoptera pests.

IRON COMPLEXING AGENT AND USES THEREOF IN THE TREATMENT AND PREVENTION OF COLORECTAL CANCER

A complex comprising a non-absorbable portion attached to an iron chelator moiety, a composition comprising the complex and the use of the complex in the treatment of colorectal cancer. In one embodiment the non-absorbable portion is a polymer such as a polysaccharide, including chitosan, chitin, cellulose or pectin. In one embodiment the iron chelator moiety comprises at least one functional group selected from catechol, hydroxamate or carboxylate, or any combination thereof.

Microemulsion technique for the novel synthesis of deferasirox using metal mediated coupling

A novel and efficient synthesis of Deferasirox has been accomplished using transition metal catalyzed sequential cross coupling reactions. First stage of the synthesis employs the use of Chan-Lam coupling between 3,5-dibromo-1H[1,2,4] triazole and (4-(methoxycarbonyl)-phenyl)boronic acid to give methyl 4-(3,5-dibromo-1H-1,2,4-triazol-1-yl)benzoate which is further elaboarated to Deferasirox by Suzuki-Miyaura coupling with 2-hydroxyphenyl-boronic acid pinacol ester in microemlusion.

Synthesis and characterization of related substances of deferasirox, an iron (Fe3+) chelating agent

Deferasirox is an orally active iron chelating agent, and during process development for deferasirox, we observed six related substances (impurities), namely deferasirox methyl ester, deferasirox salicylyl derivative, deferasirox ethyl ester, deferasirox methoxy carbonyl derivative, bis(salicyl)imide, and deferasirox-2-isomer. The present work describes the detection, origin, synthesis, and characterization of these related substances.

A boronate prochelator built on a triazole framework for peroxide-triggered tridentate metal binding

Iron chelating agents have the potential to minimize damage associated with oxidative stress in a range of diseases; however, this potential is countered by risks of indiscriminant metal binding or iron depletion in conditions not associated with systemic

PROCESS FOR THE PREPARATION OF 4-[3,5-BIS(2-HYDROXYPHENYL)-1H-1,2,4-TRIAZOL-1-YL]-BENZOIC ACID AND ITS AMINE SALTS

The present invention relates to an improved process for the preparation of 4-[3,5-bis(2-hydroxyphenyl)-1H-1,2,4-triazol-1-yl]benzoic acid compound of formula (1) and process for its purification.