98236-56-7

Upstream product

• 680-15-9 2,2-difluoro-2-(fluorosulfonyl)acetate 
• 151451-83-1 4-iodo-1-phenyl-1H-1,2,3-triazole 
• 62-53-3 aniline 
• 622-37-7 Phenyl azide 
• 138801-84-0 1-phenyl-4-(trimethylsilyl)-1H-1,2,3-triazole 
• 661-54-1 3,3,3-trifluoroprop-1-yne 
• 98236-58-9 1-phenyl-4-(1-hydroxypropyl)-5-trifluoromethyl-1,2,3-triazole 
• 98236-57-8 1-phenyl-4-trifluoromethyl-5-bromo-1,2,3-triazole 

Relevant academic research and scientific papers

Methyl-2,2-difluoro-2-(fluorosulfonyl) acetate (MDFA)/copper (I) iodide mediated and tetrabutylammonium iodide promoted trifluoromethylation of 1-aryl-4-iodo-1,2,3-triazoles

While several methods are available for the synthesis of a host of trifluoromethylated heterocycles, very few of them have been applied to access 4-trifluoromethylated 1,2,3-triazoles. We report herein a general methodology for the trifluoromethylation of 1-aryl-4-iodo-1, 2, 3-triazoles. Tetrabutylammonium iodide (TBAI) has been shown to provide enhanced conversion in these CuI-mediated reaction using methyl 2,2-difluoro-2-(fluorosulfonyl)acetate (MDFA). The method exhibited broad functional group tolerance and was applied to the synthesis of a library of 1-aryl-4-trifluoromethyl-1,2,3-triazoles on the multi-gram scale.

1,3-DIPOLAR ADDITION OF AROMATIC AZIDES TO FLUORINE-CONTAINING ACETYLENES AND DIACETYLENES

Triazoles with fluorine containing substituents at positions 4 and 5 of the heterocycle were obtained as a result of the reaction of aromatic azides with perfluoroalkyl(aryl)acetylenes and trifluoromethyldiacetylenes.