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A metal-free route to 2-aminooxazoles by taking advantage of the unique ring opening of benzoxazoles and oxadiazoles with secondary amines

机译:通过利用苯并恶唑和恶二唑与仲胺的独特开环来实现无金属合成2-氨基恶唑的途径

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摘要

Toss an amine into the ring: A new metal-free protocol for the amination of oxazoles has been developed by using iodobenzene diacetate to couple various oxazoles with amines (see scheme). The reaction proceeds through a ring-opening and subsequent ring-closing pathway. The optimal conditions are very mild and the substrate scope is broad, producing a range of 2-aminooxazoles, an important pharmacophore with high bioactivity.
机译:将胺扔进环中:通过使用碘代二苯碘乙酸酯将各种恶唑与胺偶合,开发了一种新的无金属的恶唑胺化方案(请参阅方案)。反应通过开环和随后的闭环途径进行。最佳条件非常温和,底物范围广,可产生一系列2-氨基恶唑,这是一种具有高生物活性的重要药效团。

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