Ligand-Controlled Palladium-Catalyzed Pyridylation of 1-tert-Butoxycarbonyl-3-iodoazetidine: Regioselective Synthesis of 2- and 3-Heteroarylazetidines

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• 作者：Yudan Zhang ; Zhiyue Geng ; Jingya Li ; Dapeng Zou ; Yangjie Wu and Yusheng Wu
• 刊名：Advanced Synthesis & Catalysis
• 出版年：2017
• 出版时间：February 2, 2017
• 年：2017
• 卷：359
• 期：3
• 页码：390-394
• 全文大小：1041K
• ISSN：1615-4169

文摘

The first efficient regioselective pyridylation of 1-tert-butoxycarbonyl-3-iodoazetidine to produce 2- and 3-heteroarylazetidines under palladium-catalyzed conditions has been developed. The established direct pyridylation of azetidines affords 2- vs. 3-heteroarylazetidines in moderate to good yields (up to 92%) and with good regioselectivity (up to 98:2) by using different ligands.