一类2,3,4-三取代吡咯类化合物及其合成方法和应用

2,3,4-tri-substituted pyrrole compound and synthesis method and application thereof

Abstract

The invention relates to a 2,3,4-tri-substituted pyrrole compound and a synthesis method and application thereof. Particularly, under mild conditions, copper-catalyzed isonitrile and allene are subjected to a cyclization reaction, and a simple polysubstituted pyrrole synthesis method is opened up. The compound is shown as the following general molecular formula, wherein R1 and R2 are alkyl groups or aryl groups for providing electrons, and R3 is an alkyl group or halogen. The method is used for synthesizing a series of three-bit aryl sulfone functional group containing 2,3,4-tri-substituted pyrrole compounds for the first time, and the method has wide prospects on the aspect of synthesis and application of a built compound library. Two of the synthesized three-bit aryl sulfone functional group containing 2,3,4-tri-substituted pyrrole compounds are selected for testing in-vitro tumor cell inhibitory activity, and the compound has inhibitory activity on human leukemia cells (HL-60). The formula is shown in the description.
本发明涉及一类2,3,4‑三取代吡咯类化合物及其合成方法和应用,具体是在较温和条件下,铜催化异腈和联烯发生环化反应,开拓了较为简单的合成多取代吡咯的方法。该类化合物结构通式如下式所示,其中R1,R2为给电子的烷基或者芳基;R3为烷基或卤素。本申请首次运用该方法合成出了一系列3位含有芳基砜官能团的2,3,4‑三取代吡咯类化合物,在建立该类化合物库的合成应用方面具有广阔的前景。本申请在合成的一系列3位含有芳基砜官能团的2,3,4‑三取代吡咯类化合物中选取两个进行了体外肿瘤细胞抑制活性的测试,对人白血病细胞(HL‑60)有抑制活性。

Claims

Description

Topics

Download Full PDF Version (Non-Commercial Use)

Patent Citations (0)

    Publication numberPublication dateAssigneeTitle

NO-Patent Citations (0)

    Title

Cited By (0)

    Publication numberPublication dateAssigneeTitle