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Synthesis of Substituted Pyridines via (3+3) Cycloaddition

有机合成与工艺文献分享 2025-10-09 07:22
文章摘要
本文报道了安进公司开发的吡啶合成方法，用于制备sotorasib的起始原料。研究背景是传统吡啶合成方法的局限性，研究目的是开发通过(3+3)环加成反应合成2,3,4-取代吡啶的新方法。研究发现三氯化铁添加剂能有效控制二氢吡啶浓度，防止其发生非生产性二聚，并通过过量烯醛实现氧化芳构化。该研究综合运用ReactIR原位反应动力学分析、HRMS、离线HPLC分析和对照NMR研究等多种正交技术，建立了详细的反应机理认知，为类似反应提供了重要参考。
Synthesis of Substituted Pyridines via (3+3) Cycloaddition
查看文献： Synthesis of Substituted Pyridines via Formal (3+3) Cycloaddition of Enamines with Unsaturated Aldehydes and Ketones
查看期刊：Journal of Organic Chemistry
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