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Process Development for a Tetrazole-Based Agonist Intermediate

有机合成与工艺文献分享 2025-07-01 08:59
文章摘要
本文主要介绍了一种基于四唑的激动剂中间体的第一代工艺开发过程。背景方面，研究涉及有机合成中的工艺优化问题，特别是在硝化反应中观察到的延迟放热现象。研究目的是解决工艺中的多个关键问题，包括三乙胺导致的副反应、异丁醇副产物的难以分离以及16号化合物的易消旋化问题。结论表明，通过替换反应试剂（如用氯乙胺盐酸盐替代乙醇胺）、优化反应条件（如控制温度和碱用量）以及添加碳酸氢钠等措施，成功解决了工艺中的关键问题，实现了更安全、高效的合成路径。
Process Development for a Tetrazole-Based Agonist Intermediate
查看文献： Process Research and Development for a Tetrazole-Based Growth Hormone Secretagogue (GHS) Pharmaceutical Development Candidate
查看期刊： Journal of Organic Chemistry
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