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Cyclization of 2‑Bromoarylamine with n‑Butyronitrile

有机合成与工艺文献分享 2025-04-18 06:51
文章摘要
本文探讨了替米沙坦关键中间体双苯并咪唑5的合成方法。研究团队开发了一种新方法，通过铜催化的邻卤代芳基脒环化反应构建双苯并咪唑结构，避免了传统的硝化和PPA介导的环化步骤。研究过程中意外发现2-溴芳胺11与乙腈环化反应可获得95%收率的副产物5A，这验证了通过2-碘苯胺与芳基腈的分子间环化反应合成苯并咪唑的可行性。最终提出的2-溴芳胺11与正丁腈环化路线成功规避了传统方法中使用硝酸/硫酸硝化和PPA环化的缺点。
Cyclization of 2‑Bromoarylamine with n‑Butyronitrile
查看文献： Optimized Synthesis of the Key Intermediate of Telmisartan via the Cyclization of 2-Bromoarylamine with n-Butyronitrile
查看期刊： Organic Process Research & Development
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