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Chromone splicing 3-hydroxymethyloxindole derivatives and its preparation method and application

A technology of indole derivatives and oxidized indole, which is applied in the fields of organic chemistry methods, drug combinations, organic chemistry, etc., to achieve the effects of simple operation, cheap raw material synthesis, and easy-to-obtain raw material synthesis

Active Publication Date: 2021-05-07
GUIZHOU UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] Furthermore, the construction of quaternary carbon centers in the synthesis of complex molecules has been a major challenge in organic synthesis

Method used

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  • Chromone splicing 3-hydroxymethyloxindole derivatives and its preparation method and application
  • Chromone splicing 3-hydroxymethyloxindole derivatives and its preparation method and application
  • Chromone splicing 3-hydroxymethyloxindole derivatives and its preparation method and application

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Embodiment Construction

[0019](1) Synthesis Preparation of Representative Reaction Intermediate 3

[0020]

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Abstract

The invention discloses a chromone splicing 3-hydroxymethyl oxindole derivative. In the invention, the corresponding isatin 1 and dihydrochromone 2 first undergo a Knoevenagel condensation reaction to generate an intermediate 3, and then the intermediate 3 is combined with Formaldehyde undergoes 1,3-hydrogen transfer reaction and hydroxymethylation reaction in formalin to generate the final product chromone splicing 3-hydroxymethyl indole derivatives, which include chromone skeleton and 3-hydroxymethyl oxidation The indole skeleton; the synthesis of chromone-spliced ​​3-hydroxymethyl indole derivatives are potential drug molecular intermediates or drug analogues, and have extremely important research significance. The invention is simple and easy to operate, the synthesis of raw materials is cheap and easy to obtain, and can be carried out in the water phase. There is no catalyst for green reaction, and it also has good air stability, wide applicability, and good compatibility with various substituents. sex. The present invention finds that the substance has a certain activity of inhibiting tumor cell growth.

Description

Technical field[0001]The present invention relates to the field of pharmaceutical chemistry, in particular, a preparation method and preparation method thereof of a humexone splicing 3-hydroxymethyl oxide hydroxide.Background technique[0002]It is extremely important in organic chemistry and pharmacy in organic chemistry and pharmaceutical chemistry in organic chemistry and pharmaceutical chemistry in bio-active natural product skeletons. (1), 3-season carbon oxide hydrazine compound is a widely presence of multiple pharmacologically active molecules, with biological activity such as anti-inflammatory, anti-tumor, antioxidant (eg.figure 1 Indicated). (2), the ketone frame compound is derived from the active ingredient of natural product, with multiple drug activity. Given the ketone shelf compound and 3-season carbon oxide hydride with multiple bioactive (egfigure 1 Indicated). Therefore, the ketone skeleton is spliced ​​into a 3-season carbon oxide compound, synthesizing a series of...

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D405/04A61K31/404A61P35/00A61P35/02
CPCA61P35/00A61P35/02C07B2200/13C07D405/04
Inventor 刘雄利张文会徐圣文左雄周英田民义
Owner GUIZHOU UNIV