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Rapid Process Development and GMP Manufacturing of E7130

有机合成与工艺文献分享 2025-04-23 04:25

文章摘要

本文介绍了抗癌候选药物E7130的快速工艺开发与GMP生产。背景方面，初始合成路线存在产率低、反应条件苛刻等问题，特别是脱保护步骤导致大量副产物。研究目的旨在通过结构修饰和工艺优化提高合成效率，包括将TBS基团替换为TES基团、改变C52位氮原子引入策略等改进措施。结论显示，通过第三代路线采用新型Zr/Ni介导的酮偶联反应，并优化还原剂为锰，成功将杂质控制在可接受水平，最终在1.5年内实现了超过10克的GMP标准生产。

Rapid Process Development and GMP Manufacturing of E7130

查看文献： What Does It Take to Develop Structurally Complex Molecules by Total Synthesis? Rapid Process Development and GMP Manufacturing of E7130 Drug Substance for First-in-Human Clinical Study
查看期刊：Organic Process Research & Development

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