136672-34-9

Upstream product

• 615-65-6 2-chloro-4-methyl-benzenamine 
• 145349-62-8 2-chlorophenyl-4-methylphenylboronic a cid 
• 860002-00-2 1-(2-chloro-4-methyl-phenyl)-semicarbazide 

Downstream Products

• 193887-70-6 4-azido-3-chlorobenzyl bromide 
• 193887-72-8 (2R,3R,4S,5R,6S)-3-(4-Azido-3-chloro-benzyloxy)-4,5-bis-benzyloxy-2-benzyloxymethyl-6-methoxy-tetrahydro-pyran 
• 193887-71-7 (2R,3R,4S,5R,6S)-2-(4-Azido-3-chloro-benzyloxymethyl)-3,4,5-tris-benzyloxy-6-methoxy-tetrahydro-pyran 

Relevant academic research and scientific papers

In vitro antiplasmodial efficacy of synthetic coumarin-triazole analogs

Twenty two diverse coumarin-triazole derivatives were synthesized by alkylation of 7-hydroxy-4-methyl-coumarin followed by click chemistry at 7-position. These compounds were evaluated for their in vitro antiplasmodial activity against chloroquine sensitive strain of Plasmodium falciparum (3D7). Compound 9 (7-[1-(2, 4-dimethoxy-phenyl)-1H- [1–3] triazol-4-ylmethoxy]-4-methyl-chromen-2-one) was found most active with IC50 value 0.763 ± 0.0124 μg/mL. Further, the structure of compound 20 was characterized by single crystal X-ray diffraction. In view of impressive results, we considered it worthwhile to validate the results of in vitro antiplasmodial activity by assessing whether these compounds are capable of hampering the catalytic activity of DNA gyrase, thus preventing its supercoiling function.

Synthesis and antitumor activity of 1-substituted 1,2,3-triazole-mollugin derivatives

A new series of mollugin-1,2,3-triazole derivatives were synthesized using a copper(I)-catalyzed Huisgen 1,3-dipolar cycloaddition reaction of corresponding O-propargylated mollugin with aryl azides. All the compounds were evaluated for their cytotoxicity on five human cancer cell lines (HL-60, A549, SMMC-7721, SW480, and MCF-7) using MTS assays. Among the synthesized series, most of them showed cytotoxicity and most of all, compounds 14 and 17 exhibited significant cytotoxicity of all five cancer cell lines.

Intramolecular Carbonylative C–H Functionalization of 1,2,3- Triazoles for the Synthesis of Triazolo[1,5-a]indolones

This study presents a synthesis of 4H-[1,2,3]triazolo[1,5-a]indol-4-ones. The key step in the synthesis of this new heterocyclic scaffold is an intramolecular cyclization via an unprecedented carbonylative C–H functionalization of 1-(2-bromoaryl)-1,2,3-tr

Design, synthesis and biological evaluation of ciprofloxacin tethered bis-1,2,3-triazole conjugates as potent antibacterial agents

A series of new bis-1,2,3-triazole linked ciprofloxacin conjugates was designed, synthesized and evaluated in?vitro antibacterial activity against a panel of clinically relevant bacteria. A significant part of the compounds displayed enhanced activity against both Gram-positive and Gram-negative species of bacteria as compared to the parent drug. Additionally, negligible toxicity profile of compounds indicates that they may act a good antibiotic in future. Despite relatively small number of synthesized conjugates, it was possible to observe important dependences between their structure and activity.

In situ "click" assembly of small molecule matrix metalloprotease inhibitors containing zinc-chelating groups

(Chemical Equation Presented) A panel of small molecule-based MMP inhibitors containing rhodanine warheads was assembled using "one-pot" click chemistry. Upon biological screening, moderate inhibitors were identified which specifically targets MMP-7 and MMP-13 over other MMPs.

4-Azido-3-chlorobenzyl Ether, New Protection for Hydroxy Functions

The 4-azido-3-chlorobenzyl (Cl-Azb) group was readily introduced to hydroxy functions by the use of a crystalline reagent, 4-azido-3-chlorobenzyl bromide, which was prepared from commercially available 2-chloro-4-methylaniline in two steps. Cl-Azb ethers have improved acid stability as compared to the corresponding parent 4-azidobenzyl (Azb) ether. Cl-Azb ethers were stable to direct 2,3-dichloro-5,6-dicyanobenzoquinone (DDQ) oxidation, but were cleaved smoothly by DDQ oxidation after conversion to the corresponding iminophosphorane derivative.