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Underappreciated Hydrolytic Instability of DBU

有机合成与工艺文献分享 2025-09-26 06:52

文章摘要

本文研究了有机合成中常用的碱DBU的水解不稳定性问题。背景是，在合成丙型肝炎抑制剂MK-3682的工艺中，使用DBU作为碱时，发现了一个新的杂质（氨基甲酸酯9）。研究目的是分析该杂质形成的根本原因，并更广泛地评估DBU及其他脒类和胍类碱试剂的稳定性。结论表明，DBU中的杂质N-(3-氨丙基)-ε-己内酰胺是导致副产物的主要原因，并且这些碱在无缓冲和强碱性溶液中水解不稳定，但在pH低于11.6的缓冲溶液中稳定性显著提高，这一发现在设计相关工艺时应予以考虑。

Underappreciated Hydrolytic Instability of DBU

查看文献： Investigating the Underappreciated Hydrolytic Instability of 1,8-Diazabicyclo[5.4.0]undec-7-ene and Related Unsaturated Nitrogenous Bases
查看期刊： Organic Process Research & Development

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