Direct, Regioselective N-Alkylation of 1,3-Azoles

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• 作者：Shuai Chen ; Russell F. Graceffa ; Alessandro A. Boezio
• 刊名：Organic Letters
• 出版年：2016
• 出版时间：January 4, 2016
• 年：2016
• 卷：18
• 期：1
• 页码：16-19
• 全文大小：254K
• ISSN：1523-7052

文摘

Regioselective N-alkylation of 1,3-azoles is a valuable transformation. Organomagnesium reagents were discovered to be competent bases to affect regioselective alkylation of various 1,3-azoles. Counterintuitively, substitution selectively occurred at the more sterically hindered nitrogen atom. Numerous examples are provided, on varying 1,3-azole scaffolds, with yields ranging from 25 to 95%.