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First GMP Synthesis of SGD-9501-TFA (4)

有机合成与工艺文献分享 2025-04-12 06:25
文章摘要
本文主要介绍了SGD-9501-TFA (4)的首次GMP合成过程。研究背景涉及活性连接片段2和有效载荷3的获取，重点关注季铵化反应。研究目的是优化反应条件，解决反应停滞和产物抑制问题，并提高产物的纯度和稳定性。通过实验发现，减少NaI用量会导致反应停滞，而残余盐分和水分会影响产物的物理性质。最终，通过优化反应条件和采用三阶段冻干程序，成功合成了目标产物，尽管产物纯度仍有提升空间。结论部分指出，冻干程序的优化对提高产物纯度和稳定性至关重要。
First GMP Synthesis of SGD-9501-TFA (4)
查看文献： Process Development for the First GMP Synthesis of SGD-9501-TFA, Part 2: Synthesis of the Payload, Linker, and Drug Linker
查看期刊： Organic Process Research & Development
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