通过芳基炔环加成反应一锅法合成 1-烷基-1H-吲唑类化合物。
One-pot synthesis of 1-alkyl-1H-indazoles from 1,1-dialkylhydrazones via aryne annulation.
机构信息
Department of Chemistry, Iowa State University, Ames, IA 50011, USA.
出版信息
Org Biomol Chem. 2012 Mar 28;10(12):2409-12. doi: 10.1039/c2ob07117g. Epub 2012 Feb 16.
Abstract
The reaction of readily accessible 1,1-dialkylhydrazones with commercially available o-(trimethylsilyl)aryl triflates provides a direct one-step route to pharmaceutically important 1-alkylindazoles. The products are obtained in high yields by one-pot NCS-chlorination/aryne annulation or Ac(2)O-acylation/deprotection/aromatization protocols.
摘要
易得的 1,1-二烷基腙与市售的邻-(三甲基甲硅烷基)芳基三氟甲磺酸酯反应，为合成具有重要药用价值的 1-烷基吲哚提供了一条直接的一步法途径。通过一锅法 NCS 氯化/芳基炔环加成或 Ac(2)O 酰化/脱保护/芳构化反应方案，可以高产率得到产物。
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