141072-06-2

Upstream product

• 67-56-1 methanol 
• 66086-33-7 Di-tert-butyl acetylenedicarboxylate 
• 70978-37-9 1-(azidomethyl)-4-methoxybenzene 
• 922-67-8 propynoic acid methyl ester 
• 1729-67-5 Methyl 2,3-dibromopropionate 
• 105-13-5 4-Methoxybenzyl alcohol 
• 824-94-2 p-methoxybenzyl chloride 
• 2746-25-0 p-Methoxybenzyl bromide 

Downstream Products

• 716361-79-4 1-(4-methoxybenzyl)-1H-1,2,3-triazole-4-carboxylic acid 

Relevant academic research and scientific papers

Catalytic cyclization of 2,3-dibromopropionates with benzyl azides to afford 1-benzyl-1,2,3-triazole-4-carboxylate: The use of A nontoxic bismuth catalyst

We synthesized 1,2,3-triazoles via the cyclization of 2,3-dibromopropionates with benzyl azides. Bismuth chloride is an efficient catalyst, and the reaction is accelerated by weak bases such as sodium acetate. A variety of functional groups are compatible

Efficient Synthesis of 5-Trifluoromethylthio-1,2,3-Triazoles: One-Pot Multicomponent Reaction from Elemental Sulfur and TMSCF 3

A sequential multistep reaction toward 5-trifluoromethyl thio-1,2,3-triazoles has been established, starting from alkynes, organo azides, S 8, and (trifluoromethyl)trimethylsilane (TMSCF 3). This reaction features mild conditions, easy operation, and readily available substrates.

Synthesis and biological evaluation of 1-benzyl-N-(2-(phenylamino)pyridin-3-yl)-1H-1,2,3-triazole-4-carboxamides as antimitotic agents

A library of 1-benzyl-N-(2-(phenylamino)pyridin-3-yl)-1H-1,2,3-triazole-4-carboxamides (7a–al) have been designed, synthesized and screened for their anti-proliferative activity against some selected human cancer cell lines namely DU-145, A-549, MCF-7 and HeLa. Most of them have shown promising cytotoxicity against lung cancer cell line (A549), amongst them 7f was found to be the most potent anti-proliferative congener. Furthermore, 7f exhibited comparable tubulin polymerization inhibition (IC50 value 2.04 μM) to the standard E7010 (IC50 value 2.15 μM). Moreover, flow cytometric analysis revealed that this compound induced apoptosis via cell cycle arrest at G2/M phase in A549 cells. Induction of apoptosis was further observed by examining the mitochondrial membrane potential and was also confirmed by Hoechst staining as well as Annexin V-FITC assays. Furthermore, molecular docking studies indicated that compound 7f binds to the colchicine binding site of the β-tubulin. Thus, 7f exhibits anti-proliferative properties by inhibiting the tubulin polymerization through the binding at the colchicine active site and by induction of apoptosis.

Design and development of Isatin-triazole hydrazones as potential inhibitors of microtubule affinity-regulating kinase 4 for the therapeutic management of cell proliferation and metastasis

Microtubule affinity-regulating kinase 4 (MARK4) is a potential drug target as the same is found to be over expressed in several types of cancers. In search of effective MARK4 inhibitors, we have synthesized and characterized Isatin-triazole hydrazones (9a-i) and evaluated their inhibitory potential. Of all the compounds, 9g showed better binding affinity and enzyme inhibition potential in sub micromolar range. Human serum albumin (HSA) binding assay suggested an easy transportation of 9g in blood stream due to its binding affinity. In vitro anticancer studies performed on MCF-7, MDA-MB-435s and HepG2 cells using 9g showed inhibition of cell proliferation and cell migration. Further, 9g induces apoptosis in these cancerous cells, with IC50 values of 6.22, 9.94 and 8.14 μM, respectively. Putatively, 9g seems to cause oxidative stress resulting in apoptosis. Functional assay of 9g with a panel of 26 kinases showed MARK4 specific profile. In conclusion, 9g seems to possess an effective inhibitory potential towards MARK4 adding an additional repertoire to anticancer therapeutics.

EFFECT OF SOLVENT AND REACTION TIME ON THE PRODUCTS OF THE 1,3-DIPOLAR CYCLOADDITION OF SUBSTITUTED BENZYL AZIDES WITH DI-tert-BUTYL ACETYLENEDICARBOXYLATE

The 1,3-dipolar cycloaddition of substituted benzyl azides with di-tert-butyl acetylenedicarboxylate was found to be sensitive to the solvent (and time) of the reaction.Di-tert-butyl 1,2,3-triazole-4,5-dicarboxylate derivatives were obtained when the reac