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Kilogram Palladium Catalyzed C-H Activation

有机合成与工艺文献分享 2025-03-27 08:56

文章摘要

本文介绍了辉瑞全球研发团队的Michael Pamment及其同事开发的一种公斤级合成方法，用于制备oxazolidinone抗菌剂32。研究采用了钯催化的C-H活化策略来构建关键的oxindole中间体30。整个合成过程为6步线性序列，其中C-H活化化学在第四步中发挥了关键作用。研究发现，使用三氟甲苯作为溶剂可以最小化产物分解，并以75%的产率获得所需的oxindole 32，且产物易于分离。该方法最终以86%的产率生成了4.9公斤的oxindole 32。文章还提到了Buchwald团队最初开发的从氯乙酰苯胺合成oxindole的方法，并提出了三种可能的机理途径。

Kilogram Palladium Catalyzed C-H Activation

查看文献： Development of a Synthesis For a Long-Term Oxazolidinone Antibacterial
查看期刊：Organic Process Research & Development

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