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Large-Scale Tandem Cyclization

有机合成与工艺文献分享 2025-03-20 06:47
文章摘要
本文探讨了一种大规模串联环化反应在有机合成中的应用，特别是针对化合物13的合成。化合物13是一种生长抑素受体亚型4（SSTR4）激动剂，具有治疗疼痛的潜力。研究采用硫叶立德和含有电子缺陷烯烃的脂肪族仲胺在碱驱动下生成融合环系统。初步概念验证证实了该方法的可行性。开发了一种无金属、更收敛的七步合成路线，包括六次分离，总产率超过25%，并大幅缩短了循环时间。新开发的化学方法也适用于制备另一种具有3-氮杂双环[3.1.0]己烷核心的化合物（28）。
Large-Scale Tandem Cyclization
查看文献： Large-Scale Tandem Cyclization Applied to Potentially High-Volume SSTR4 Agonists
查看期刊： Organic Process Research & Development
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