一种含吲哚嗪的二芳基甲烷衍生物及其制备方法和应用

By synthesizing diarylmethane derivatives containing indoleazine and benzofuran or indole, the problem of single biological activity of existing compounds has been solved, achieving simultaneous antibacterial and anticancer activities, which has important biological activity and drug development potential.

CN116903612BActive Publication Date: 2026-07-17JIANGXI NORMAL UNIV

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
JIANGXI NORMAL UNIV
Filing Date
2022-11-02
Publication Date
2026-07-17

AI Technical Summary

Technical Problem

Existing diarylmethane compounds containing indoleazine have limited biological activity, mainly exhibiting insufficient inhibitory activity against secretory phospholipase sPLA2, and lacking antibacterial and anticancer activities.

Method used

Diarylmethane derivatives containing indoleazine and benzofuran or indole are synthesized by tandem cyclization reactions of 2-iodophenylpropadiene compounds and propargylpyridine compounds in the presence of palladium catalyst and base. The preparation method includes steps such as extraction, drying, filtration, vacuum distillation and column chromatography.

Benefits of technology

The synthesized compounds possess both antibacterial and anticancer activities. As fluorescent probes, organic synthesis intermediates, or drug intermediates, they have significant biological activity and drug development value. The reaction steps are simple, the products are easy to purify, and the substrates have strong universality.

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Abstract

本发明公开了一种含吲哚嗪的二芳基甲烷衍生物及其制备方法和应用,所述二芳基甲烷衍生物结构式如下:其中,R1选自酰基;R2选自苯基、取代苯基或C1~C5的烷基;R3选自C1~C5的烷基、卤素或氢;R4选自对甲苯璜酰基、对硝基苯磺酰基、苯磺酰基或叔丁氧羰基。本发明所述含吲哚嗪的二芳基甲烷类化合物同时含有吲哚嗪和苯并呋喃或吲哚,具有抗菌和抗癌活性,也可作为合成其它功能有机分子的中间体,对于有机合成和药物研发具有重要价值。
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