One-pot synthesis of 1-alkyl-1H-indazoles from 1,1-dialkylhydrazones via aryne annulation.

Organic & Biomolecular Chemistry
Nataliya A MarkinaRichard C Larock

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.

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Citations

Sep 28, 2012·The Journal of Organic Chemistry·Chun LuRichard C Larock
Jul 10, 2018·Journal of Biochemical and Molecular Toxicology·Zuhal Alim
Apr 10, 2014·Chemical Communications : Chem Comm·Zhenxing LiuJianbo Wang
Nov 8, 2012·Organic & Biomolecular Chemistry·Anton V DubrovskiyRichard C Larock
Feb 19, 2021·Chemical Reviews·Jiarong ShiYang Li
Mar 15, 2012·The Journal of Organic Chemistry·Pan LiFeng Shi
Nov 10, 2012·The Journal of Organic Chemistry·Nicolas RichyJoëlle Vidal

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