Room-Temperature,Metal-Free,and One-Pot Preparation of 2H-Indazoles through a Mills Reaction and Cyclization Sequence |
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Authors: | Dr Masaru Kondo Dr Shinobu Takizawa Yuzhao Jiang Prof Dr Hiroaki Sasai |
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Institution: | The Institute of Scientific and Industrial Research (ISIR), Osaka University, Mihogaoka, Ibaraki-shi, Osaka, 567-0047 Japan |
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Abstract: | 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. |
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Keywords: | cyclization indazole metal-free synthesis nitrogen heterocycles one-pot reaction |
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