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使用三组分反应进行吡啶鎓吡唑-3-醇内盐库的溶液相平行合成。

Solution-phase parallel synthesis of a pyridinium pyrazol-3-olate inner salt library using a three-component reaction.

作者信息

Varga Laszló, Nagy Tamas, Dorman György, Kalman Ferenc, Urge Laszló, Darvas Ferenc

机构信息

ComGenex Inc., Budapest, Hungary.

出版信息

J Comb Chem. 2006 May-Jun;8(3):338-43. doi: 10.1021/cc0501514.

Abstract

We present here the discovery of a novel, versatile, multicomponent reaction leading to various 4-[4-(pyridinium-1-yl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]-2H-pyrazol-3-olate inner salts. The structure of the unusual zwitterionic inner salts was elucidated, and the scope of the novel reaction was investigated. After rapid optimization, the reaction was adapted to parallel synthesis, and an 800-membered compound library was produced.

摘要

我们在此展示了一种新型、通用的多组分反应的发现,该反应可生成各种4-[4-(吡啶-1-基)-2,5-二氧代-2,5-二氢-1H-吡咯-3-基]-2H-吡唑-3-醇内盐。阐明了这种不寻常的两性离子内盐的结构,并研究了该新型反应的适用范围。经过快速优化后,该反应适用于平行合成,并生成了一个包含800个化合物的文库。

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