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Efficient Synthesis of Fused Oxazepino-isoquinoline Scaffolds via an Ugi, Followed by an Intramolecular Cyclization.
ACS Combinatorial Science ( IF 3.903 ) Pub Date : 2017-03-09 , DOI: 10.1021/acscombsci.7b00002
Yong Li 1, 2 , Jiang-Ping Meng 1 , Jie Lei 1, 2 , Zhong-Zhu Chen 1 , Dian-Yong Tang 1 , Jin Zhu 1, 2 , Jin Zhang 1 , Zhi-Gang Xu 1
Affiliation  

A mild and efficient protocol was developed for the synthesis of oxazepino-isoquinolines via a one-pot Ugi four-component reaction, followed by the intramolecular addition of the resulting alcohol to an alkyne moiety under microwave irradiation conditions. Notably, this process only required one purification step, providing facile access to two series of complex and potentially interesting biologically active scaffolds.

中文翻译:

通过Ugi高效合成熔融的氧杂庚酮-异喹啉骨架,然后进行分子内环化。

开发了一种温和而有效的方案,用于通过一锅Ugi四组分反应合成氧杂庚烷-异喹啉,然后在微波辐射条件下将所得醇分子内添加到炔烃部分。值得注意的是,该过程仅需一个纯化步骤,即可轻松获得两套复杂且潜在有趣的生物活性支架。
更新日期:2017-03-16
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