通过米尔斯反应和环化序列在室温下无金属一锅法制备2H-吲唑
Room-Temperature, Metal-Free, and One-Pot Preparation of 2H-Indazoles through a Mills Reaction and Cyclization Sequence.
作者信息
Kondo Masaru, Takizawa Shinobu, Jiang Yuzhao, Sasai Hiroaki
机构信息
The Institute of Scientific and Industrial Research (ISIR), Osaka University, Mihogaoka, Ibaraki-shi, Osaka, 567-0047, Japan.
Artificial Intelligence Research Center, ISIR, Osaka University, Osaka, 567-0047, Japan.
出版信息
Chemistry. 2019 Jul 25;25(42):9866-9869. doi: 10.1002/chem.201902242. Epub 2019 Jul 1.
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.
利用亚硫酰溴对易得的2-氨基苄醇和亚硝基苯进行米尔斯反应和环化反应，可得到产率高达88%的2H-吲唑。在无金属过程中，乙酸对米尔斯反应和环化反应都起着关键作用。通过一锅法序列也可得到溴代2H-吲唑。
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