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First GMP Synthesis of SGD-9501-TFA (2)

有机合成与工艺文献分享 2025-04-10 07:50
文章摘要
本文介绍了SGD-9501-TFA (2)的首次GMP合成过程。研究背景涉及有机合成工艺的优化，特别是在未保护的二甲基丝氨酸直接偶联反应中遇到的挑战。研究目的是通过优化反应条件，减少副反应如胍基化和寡聚化，并提高产物的纯度和收率。结论表明，通过预活化阶段的优化、使用特定的缓冲溶液洗涤以及反应结晶技术，成功实现了高效、可控的合成过程，并在氟醇脱保护策略下有效抑制了副反应。
First GMP Synthesis of SGD-9501-TFA (2)
查看文献： Process Development for the First GMP Synthesis of SGD-9501-TFA, Part 1: Synthesis of Two Oligopeptide Fragments
查看期刊：Organic Process Research & Development
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