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Room-Temperature, Metal-Free, and One-Pot Preparation of 2H-Indazoles through a Mills Reaction and Cyclization Sequence.

Masaru KondoShinobu TakizawaYuzhao JiangHiroaki Sasai
Published in: Chemistry (Weinheim an der Bergstrasse, Germany) (2019)
The Mills reaction and cyclization of readily available 2-aminobenzyl alcohols and nitrosobenzenes using thionyl bromide provided 2H-indazoles in up to 88 % yields. In the metal-free process, acetic acid played a crucial role for the both Mills reaction and cyclization. A brominated 2H-indazole could also be obtained through the one-pot sequence.
Keyphrases
  • room temperature
  • ionic liquid
  • amino acid