4915-97-3

Upstream product

• 14762-48-2 ethyl 2-diazo-3-oxo-propanoate 
• 62-53-3 aniline 
• 5941-50-4 ethyl β-nitroacrylate 
• 622-37-7 Phenyl azide 
• 5941-50-4 (E)-ethyl 3-nitroacrylate 
• 98-80-6 phenylboronic acid 
• 623-47-2 propynoic acid ethyl ester 
• 140-88-5 ethyl acrylate 
• 591-50-4 iodobenzene 

Downstream Products

• 4600-04-8 1-phenyl-1H-[1,2,3]triazole-4-carboxylic acid 
• 103755-58-4 (1-phenyl-1H-1,2,3-triazole-4-yl)methanol 
• 214541-36-3 1-Phenyl-1H-[1,2,3]triazole-4-carboxylic acid dimethylamide 
• 134541-91-6 1-phenyl-1H-1,2,3-triazole-4-carboxylic acid chloride 

Relevant academic research and scientific papers

Design, synthesis and in-vitro evaluation of fluorinated triazoles as multi-target directed ligands for Alzheimer disease

Alzheimer disease is multi-factorial and inflammation plays a major role in the disease progression and severity. Metals and reactive oxygen species (ROS) are the key mediators for inflammatory conditions associated with Alzheimer's. Along multi-factorial nature, major challenge for developing new drug is the ability of the molecule to cross blood brain barrier (BBB). We have designed and synthesized multi-target directed hexafluorocarbinol containing triazoles to inhibit Amyloid β aggregation and simultaneously chelate the excess metals present in the extracellular space and scavenge the ROS thus reduce the inflammatory condition. From the screened compound library, compound 1c found to be potent and safe. It has demonstrated inhibition of Amyloid β aggregation (IC50 of 4.6 μM) through selective binding with Amyloid β at the nucleation site (evidenced from the molecular docking). It also chelate metals (Cu+2, Zn+2 and Fe+3) and scavenges ROS significantly. Due to the presence of hexafluorocarbinol moiety in the molecule it may assist to permeate BBB and improve the pharmacokinetic properties. The in-vitro results of compound 1c indicate the promiscuity for the development of hexafluorocarbinol containing triazoles amide scaffold as multi-target directed therapy against Alzheimer disease.

Water as a solvent for Ru-catalyzed click reaction: Highly efficient recyclable catalytic system for triazolocoumarins synthesis

A new family of Ru (III) complexes has been synthesized, characterized and their catalytic performance has been tested for alkyne–azide cycloaddition (AAC) in water under ultrasonic irradiation conditions. These complexes are found to be effective heterog

Alkyl Propiolates Participated [3+2] Annulation for the Switchable Synthesis of 1,5- and 1,4-Disubstituted 1,2,3-Triazoles Containing Ester Side Chain

By means of a featured enamine activation, the alkyl propiolates have been successfully employed in the [3+2] annulation for the synthesis of 1,2,3-triazoles. The synthesis of both 1,4- as well as the hardly available 1,5-disubstituted 1,2,3-triazoles can be selectively accessed by using tosyl azide and tosyl hydrazine as nitrogen source, respectively.

4β-amidotriazole linked podophyllotoxin congeners: DNA topoisomerase-IIα inhibition and potential anticancer agents for prostate cancer

Topoisomerases (topo-I and topo-II) have occupied a significant role in DNA replication, transcription, and are a promising set of antitumor targets. In the present approach, a series of new 4β-amidotriazole linked podophyllotoxin derivatives (10a-i and 1

NOVEL OXABOROLE ANALOGS AND USES THEREOF

This application describes compounds, compositions, and methods which are useful in treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease caused by a parasite.

4BETA-AMIDOTRIAZOLE LINKED PODOPHYLLOTOXIN DERIVATIVES AS POTENTIAL ANTICANCER AGENTS

The present invention relates to a compound of general formula (A). The invention provides asynthesis of new 4β-amidotriazole linked podophyllotoxin derivatives of general formulae 8a-z to 9a-z useful as potential anticancer agents against human cancer ce

An efficient and recyclable thiourea-supported copper(i) chloride catalyst for azide-alkyne cycloaddition reactions

A reaction between two equivalents of bulky thiourea, i.e., 1,3-bis(2,6-dimethylphenyl)thiourea (L) [L = (ArNH)2C = S; Ar = 2,6-Me2C6H3], and CuCl2 or CuCl in THF solvent afforded a bulky thiourea-sta

Synthesis of 13N-labelled polysubstituted triazoles: Via Huisgen cycloaddition

The use of the positron emitter nitrogen-13 (13N) has been historically restricted due to its short half-life (T1/2 = 9.97 min). However, its stable isotopes (nitrogen-14 and nitrogen-15) are present in many biologically active molec

Copper Acetate Catalyzed Regio-selective Synthesis of Substituted 1,2,3-Triazoles: A Versatile Azide–Alk-ene Cycloaddition/Oxidation Approach

A copper acetate catalyzed oxidative cycloaddition reaction of benzyl and aryl azides with terminal and internal olefins that contain electron-withdrawing groups (COOR, CONH2, CN, CHO, COR) has been developed. The reaction employs air as the oxidant and does not require any base or additives to afford 1,4-disubstituted and 1,4,5-trisubstituted 1,2,3-triazoles in good to excellent yields with high regioselectivity.

Direct access to 1,4-disubstituted 1,2,3-triazoles through organocatalytic 1,3-dipolar cycloaddition reaction of α,β-unsaturated esters with azides

DBU-catalyzed organocatalytic 1,3-dipolar cycloaddition reactions of α,β-unsaturated esters with azides have been developed. This strategy generates 1,4-disubstituted 1,2,3-triazoles in high yields with high regioselectivities. It is demonstrated that some of these products can be transformed into important pharmaceutical agents.