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Stereochemical Editing via Coupled Epimerization and Resolution

有机合成与工艺文献分享 2025-11-14 08:01
文章摘要
本文研究背景涉及哌嗪结构单元在药物adagrasib大规模生产中的需求，原有合成路线存在操作不便和副反应问题。研究目的旨在开发一种基于供应中心合成原则的新路线，避免使用氰化钠并优化工艺效率。通过识别(S)-扁桃酸作为光学拆分剂、乙二醇作为溶剂加速差向异构化，并结合多批次循环回收策略，最终实现了更高效的哌嗪合成路径，同时优化脱苄基步骤降低了试剂消耗，形成比传统对映体纯起始物料更优越的合成方案。
Stereochemical Editing via Coupled Epimerization and Resolution
查看文献： Stereochemical Editing via Coupled Epimerization and Optical Resolution to Sustainably Manufacture a Key Adagrasib Building Block
查看期刊：Organic Process Research & Development
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