A Convenient Route to 1-Alkyl-5-trifluoromethyl-1,2,3-triazole-4-carboxylic Acids Employing a Diazo Transfer Reaction

作者：Iminov Rustam T; Mashkov Alexander V; Chalyk Bohdan A; Mykhailiuk Pavel K; Tverdokhlebov Anton V^*; Tolmachev Andrey A; Volovenko Yulian M; Shishkin Oleg V; Shishkina Svetlana V

来源：European Journal of Organic Chemistry, 2013, 2013(14): 2891-2897.

DOI：10.1002/ejoc.201300030

• Synthetic methods
• Medicinal chemistry
• Nitrogen heterocycles
• Amines
• Azides
• Fluorine

The reaction of ethyl 3-(alkylamino)-4,4,4-trifluoro-but-2-enoates with mesyl azide in the presence of 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU) gave ethyl 1-alkyl-5-trifluoromethyl-1,2,3-triazole-4-carboxylates in good yields. Further hydrolysis of the ester group afforded the title compounds on a multigram scale.

• 出版日期2013-5