Expedient Synthesis of α-Heteroaryl Piperidines Using a Pd-Catalyzed Suzuki Cross-Coupling–Reduction Sequence

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• 作者：Kevin D. Hesp ; Dilinie P. Fernando ; Wenhua Jiao ; Allyn T. Londregan
• 刊名：Organic Letters
• 出版年：2014
• 出版时间：January 17, 2014
• 年：2014
• 卷：16
• 期：2
• 页码：413-415
• 全文大小：245K
• ISSN：1523-7052

文摘

A method for the modular synthesis of 伪-heteroaryl piperidines is reported. The two-step procedure consists of an initial Pd-catalyzed Suzuki cross-coupling of the heteroaryl bromide with a boronate ester derived from N-Boc piperidone, followed by subsequent tetrahydropyridine reduction. Using this method, 伪-heteroaryl piperidine products featuring a broad range of pharmaceutically relevant azine and diazine substitutions have been prepared.