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Cu‐Mediated Selective N‐Arylation of Aminotriazole Acyclonucleosides
Authors:Wei Li  Yuting Fan  Yi Xia  Palma Rocchi  Ruizhi Zhu  Fanqi Qu  Johan Neyts  Juan L Iovanna  Ling Peng
Institution:1. State Key Laboratory of Virology, College of Chemistry and Molecular Sciences, Wuhan University, Wuhan 430072, P.?R. China;2. Département de Chimie, CNRS UPR 3118, 163, avenue de Luminy, F‐13288 Marseille cedex 09, (phone: +33?491?82?91?54;3. fax: +33?491?82?93?01);4. INSERM U624, 163, avenue de Luminy, F‐13288 Marseille;5. Rega Institute for Medical Research, Minderbroedersstraat 10, B‐3000 Leuven
Abstract:Novel N‐aryltriazole nucleosides were synthesized via a Cu‐mediated C? N cross‐coupling reaction, using 3‐aminotriazole acyclonucleosides and various boronic acid reagents. Interestingly, N‐arylation proceeded much more rapidly on the amide group than on the amine group, leading to selective N‐arylation of the amide functionality on nucleosides containing both groups on the triazole nucleobase.
Keywords:Nucleosides  C–  N Coupling  Arylation  Triazole nucleosides
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