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通过 Ugi 反应,随后进行分子内环化,高效合成稠合的噁唑并异喹啉骨架。

Efficient Synthesis of Fused Oxazepino-isoquinoline Scaffolds via an Ugi, Followed by an Intramolecular Cyclization.

机构信息

Chongqing Engineering Laboratory of Targeted and Innovative Therapeutics, Chongqing Key Laboratory of Kinase Modulators as Innovative Medicine, IATTI, Chongqing University of Arts and Sciences , 319 Honghe Avenue, Yongchuan, Chongqing 402160, China.

Key Laboratory for Asymmetric Synthesis and Chiral Technology of Sichuan Province, Chengdu Institute of Organic Chemistry, Chinese Academy of Sciences . Chengdu 610041, China.

出版信息

ACS Comb Sci. 2017 May 8;19(5):324-330. doi: 10.1021/acscombsci.7b00002. Epub 2017 Mar 16.

DOI:10.1021/acscombsci.7b00002
PMID:28271876
Abstract

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.

摘要

开发了一种温和高效的合成方法,通过一锅 Ugi 四组分反应合成了恶唑并异喹啉,然后在微波辐射条件下,使所得醇的分子内加成到炔基部分。值得注意的是,该过程仅需要一步纯化步骤,为获得两种复杂且具有潜在生物活性的骨架提供了简便的途径。

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