Carboxylic acid derivatization beta-carboline and preparation method thereof

A derivatization and carboline technology, which is applied in the fields of chemistry and medicine, can solve problems such as insufficient structural diversity, and achieve the effects of wide application range of substrates, strong functional group tolerance, and mild reaction conditions

Inactive Publication Date: 2018-06-22
NINGBO UNIV
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  • Abstract
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Problems solved by technology

[0004] Aiming at the existing β-carboline compounds, especially the lack of structural diversity on the benzene ring, the first technical problem to be solved by the present invention is to provide a new type of β-carbolines that carry out carboxylation on the benzene ring. Carboxylated β-carbolines, starting from carboxylated β-carbolines, will provide a molecular basis for the synthesis of numerous structurally diverse β-carbolines for biological activity research

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  • Carboxylic acid derivatization beta-carboline and preparation method thereof
  • Carboxylic acid derivatization beta-carboline and preparation method thereof
  • Carboxylic acid derivatization beta-carboline and preparation method thereof

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Embodiment Construction

[0020] In order to further understand the present invention, the preferred embodiments of the present invention are described below in conjunction with the examples, but it should be understood that these descriptions are only to further illustrate the features and advantages of the present invention, rather than limiting the claims of the present invention.

[0021] The preparation method of the examples in the present invention is as follows: in an organic solvent, add methyl-β-carboline, catalyst and condensation agent, react at a certain temperature for a certain period of time, and obtain a crude product after filtering the reaction mixture, and the crude product is re- The product is obtained after crystallization or column purification. Embodiment 1-15, methyl-beta-carboline reaction material used, catalyst, initiator, organic solvent, reaction temperature, reaction time and productive rate are shown in Table 1. The compound structures of the products are shown in Table...

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Abstract

The invention relates to carboxylic acid derivatization beta-carboline and a preparation method of the carboxylic acid derivatization beta-carboline. The method comprises the steps that organic solvent is added into the mixture of 6-methyl-beta carbazoline, metal-salt catalyst and initiator, oxygen is introduced, and after stirring reaction is conducted, the reaction is terminated; filtering is conducted, and solid crude products are collected; further purification of the crude products is conducted through recrystallization and silica gel column chromatography to obtain products. According tothe method, reaction conditions are mild, the application range of substrates is wide, and a large number of beta-carboline derivatives with diversified structures can be obtained.

Description

technical field [0001] The present invention relates to the technical fields of chemistry and medicine, in particular to a carboxylic acid derivatized β-carboline, and the invention also relates to a preparation method of the β-carboline. Background technique [0002] β-carboline compounds are a class of alkaloids widely present in terrestrial plants and marine organisms in nature. β-carboline compounds contain indole and tryptamine, and have a wide range of biological activities, such as anti-tumor, anti- Virus, antibacterial, antiprotozoal, antithrombotic, anti-Alzheimer syndrome, etc. β-carboline compounds are one of the lead compounds with the most potential application value. In recent years, a large number of β-carboline compounds have been obtained through artificial synthesis, but the research on the structure-activity relationship of these compounds is not very deep. To synthesize β-carboline compounds with structural diversity, it is necessary to further explore ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D471/04
CPCC07D471/04
Inventor 裘弘达梁洪泽林妙满马家乐何铭李咏梅闫迎华赵玲玲
Owner NINGBO UNIV
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