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Rapid synthesis of 3-amino isocoumarin derivatives from ynamides
Organic & Biomolecular Chemistry ( IF 3.2 ) Pub Date : 2018-09-25 , DOI: 10.1039/c8ob02305k
Loïc Habert 1, 2, 3, 4, 5 , Pascal Retailleau 6, 7, 8, 9 , Isabelle Gillaizeau 1, 2, 3, 4, 5
Affiliation  

A novel and efficient fast synthesis of 3-amino isocoumarins in good to excellent yields is reported. These interesting scaffolds can be obtained either in a single step from readily available ynamides or in a two-step sequence from the corresponding alkynyl bromide after C–N cross-coupling. This protocol, which only requires a Brønsted or Lewis acid as a promoter, offers an alternative approach toward synthesizing 3-substituted isocoumarins under smooth and fast conditions.

中文翻译:

从乙酰胺快速合成3-氨基异香豆素衍生物

报道了新颖且有效的快速合成3-氨基异香豆素的高产率至优异产率。这些有趣的支架既可以一步一步从现成的酰胺中获得,也可以通过两步序列从C–N交叉偶联后从相应的炔基溴中获得。该方案仅需要布朗斯台德酸或路易斯酸作为促进剂,为在平滑快速的条件下合成3-取代的香豆素提供了另一种方法。
更新日期:2018-10-18
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