Enantioselective Synthesis of Substituted Piperidines by Addition of Aryl Grignard Reagents to Pyridine N-Oxides

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• 作者：Munawar Hussain ; Thomas Sainte-Luce Banchelin ; Hans Andersson ; Roger Olsson ; Fredrik Almqvist
• 刊名：Organic Letters
• 出版年：2013
• 出版时间：January 4, 2013
• 年：2013
• 卷：15
• 期：1
• 页码：54-57
• 全文大小：218K
• 年卷期：v.15,no.1(January 4, 2013)
• ISSN：1523-7052

文摘

The synthesis of optically active piperidines by enantioselective addition of aryl Grignard reagents to pyridine N-oxides and lithium binolate followed by reduction is reported for the first time. The reaction results in high yields (51鈥?4%) in combination with good ee (54鈥?0%). Some of these products were subsequently recrystallized, affording enhanced optical purities (>99% ee).