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One-Pot Synthesis of Fully Substituted Oxazol-2-amines via Staudinger/Aza-Wittig/Isomerization Reaction
Heterocycles ( IF 0.8 ) Pub Date : 2022-01-04 , DOI: 10.3987/com-21-14600
Hai Xie , Qing-Qing Hu , Xiu-Ting Qin , Jia-Min Liang , Lu- Li , Ya-Li Zhang , Zhen Lu

Readily available vinyl azide alcohols reacted with triphenylphosphine and aromatic isocyanates via sequential Staudinger reaction and intramolecular aza-Wittig reaction to afford the corresponding isoxazole intermediates, which can isomerize into aromatic oxazol-2-amines in situ without addition of catalyst under 115 ℃. This methodology provided a new and efficient one-pot approach for fully substituted oxazol-2-amines.

中文翻译:

通过施陶丁格/氮杂维蒂希/异构化反应一锅法合成完全取代的 Oxazol-2-胺

易得的叠氮乙烯醇与三苯基膦和芳香族异氰酸酯通过顺序施陶丁格反应和分子内氮杂-维蒂希反应得到相应的异恶唑中间体,在115 ℃下无需添加催化剂即可原位异构化为芳香族恶唑-2-胺。该方法为完全取代的 oxazol-2-amines 提供了一种新的有效的一锅法。
更新日期:2022-01-04
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