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通过微波辅助多组分反应,对具有潜在生物活性的吡唑并[4,3-f]喹啉衍生物进行了导向多样性合成。

A diversity-oriented synthesis of pyrazolo[4,3-f]quinoline derivatives with potential bioactivities via microwave-assisted multi-component reactions.

机构信息

School of Chemistry and Chemical Engineering, Xuzhou Normal University, Xuzhou, Jiangsu, 221116, People's Republic of China.

出版信息

Mol Divers. 2011 May;15(2):497-505. doi: 10.1007/s11030-010-9272-3. Epub 2010 Sep 3.

DOI:10.1007/s11030-010-9272-3
PMID:20814822
Abstract

Six new series of pyrazolo[4,3-f]quinoline derivatives with potential bioactivities were synthesized by the three-component reactions of aromatic aldehydes, 5-aminoindazole, and various cyclic 1,3-dicarbonyl compounds under microwave irradiation. This protocol has the valuable features of structural diversity of products, broader substrate scope, operational simplicity, high yields, and short reaction time. Moreover, the structure of compound 88a was confirmed by an X-ray crystallographic analysis and attested to the chemoselectivity of reaction where 1-methyl barbituric acid participated.

摘要

六种新的吡唑并[4,3-f]喹啉衍生物具有潜在的生物活性,通过微波辐射下芳香醛、5-氨基吲唑和各种环状 1,3-二羰基化合物的三组分反应合成。该方案具有产物结构多样性、底物范围更广、操作简单、产率高和反应时间短等优点。此外,化合物 88a 的结构通过 X 射线晶体学分析得到证实,并证明了 1-甲基巴比妥酸参与的反应具有化学选择性。

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