1422965-67-0

Upstream product

• 623-73-4 diazoacetic acid ethyl ester 
• 126855-72-9 N-(4-methylphenyl)-2,2,2-trifluoroacetimidoyl chloride 
• 106-49-0 p-toluidine 
• 2101-86-2 p-methylazidobenzene 
• 372-31-6 ethyl 4,4,4-trifluoroacetoacetate 
• 5720-05-8 4-methylphenylboronic acid 

Relevant academic research and scientific papers

Preparation method of 5-trifluoromethyl substituted 1, 2, 3-triazole compound

The invention discloses a preparation method of a 5-trifluoromethyl substituted 1, 2, 3-triazole compound, which comprises the steps of adding cesium carbonate, a molecular sieve, trifluoroethyl imine chloride and a diazo compound into an organic solvent,

Discovery and biological evaluation of novel 6,7-disubstituted-4-(2-fluorophenoxy)quinoline derivatives possessing 1,2,3-triazole-4-carboxamide moiety as c-Met kinase inhibitors

A series of 6,7-disubstituted-4-(2-fluorophenoxy)quinoline derivatives possessing 1,2,3-triazole-4-carboxamide moiety were designed, synthesized and evaluated for their in vitro biological activities against c-Met kinase and five typical cancer cell lines (A549, H460, HT-29, MKN-45 and U87MG). Most compounds showed moderate to excellent antiproliferative activity. In this study, a promising compound 34, with a c-Met IC50 value of 1.04 nM, was identified as a multitargeted receptor tyrosine kinase inhibitor. The SAR analyses indicated that compounds with halogen group, especially fluoro group, at 4-position on the phenyl ring (moiety B) have potent antitumor activity, and methylation on the 5-atom linker played an important role in the c-Met enzymatic activity.

Novel synthesis of 1,4,5-trisubstituted 1,2,3-triazoles via a one-pot three-component reaction of boronic acids, azide, and active methylene ketones

A series of 1-aryl-5-trifluoromethyl (or difluoromethyl)-1,4,5- trisubstituted 1,2,3-triazoles were synthesized in high yield by a novel one-pot three-component reaction of arylboronic acids, sodium azide, and active methylene ketones, such as ethyl 4,4-difluoroacetoacetate or ethyl 4,4,4-trifluoroacetoacetate in the presence of Cu(OAc)2 and piperidine using a DMSO/H2O (10/1) mixture as solvent.