Microwave‐promoted piperidination of halopyridines: a comparison between Ullmann,Buchwald–Hartwig and uncatalysed SNAr reactions |
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| Authors: | Ricardo S. Yaunner José C. Barros Joaquim F. M. da Silva |
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| Affiliation: | Laboratório de Química Medicinal do Polo de Xistoquímica (PXQMed), Instituto de Química, Universidade Federal do Rio de Janeiro, Cidade Universitária, , Rio de Janeiro, RJ, 21941‐614 Brazil |
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| Abstract: | A comparative study between the most used methodologies for the preparation of piperidinyl pyridines (Buchwald–Hartwig reaction, Ullmann reaction and nucleophilic aromatic substitution (SNAr)) by microwave‐assisted piperidination of halopyridines is reported. Our results suggest that the Ullmann reaction is most effective for less reactive halopyridines, while uncatalysed SNAr is sufficient for more reactive ones. Copyright © 2012 John Wiley & Sons, Ltd. |
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| Keywords: | C― N coupling Buchwald– Hartwig Ullmann nucleophilic aromatic susbtitution microwave irradiation |
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