Matrine pyrimidine derivative, and preparation method and application thereof

A technology for matrine and pyrimidine, which is applied in the field of matrine and pyrimidine derivatives and the preparation thereof, can solve the problems of lack of matrine and pyrimidine compounds, and achieves the effects of inhibiting proliferation and differentiation and having a simple and convenient preparation method.

Active Publication Date: 2021-10-29
GUANGXI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
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Problems solved by technology

There is no research on related drugs of matr

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  • Matrine pyrimidine derivative, and preparation method and application thereof
  • Matrine pyrimidine derivative, and preparation method and application thereof
  • Matrine pyrimidine derivative, and preparation method and application thereof

Examples

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Embodiment 1

[0031] (1) Synthesis of intermediate 14-formyl-15-chloromatrine

[0032] Weigh 20g (80mml, 1eq) of matrine and place it in a 150ml dry beaker, add 120ml of dichloromethane and stir to fully dissolve the matrine, and place it in a dry environment for later use after dissolving. Prepare a 500ml dry three-necked flask, seal it, evacuate it and protect it with nitrogen, and pre-cool the three-necked flask under an ice bath. Weigh 17.52g of DMF, and inject DMF into a three-neck flask. Then weigh 36.8g of phosphorus oxychloride and slowly add it dropwise to DMF. After the dropwise addition, react at 0°C for 1h, and finally add the dissolved matrine to the reaction solution. At this time, the reaction solution changes from a colorless liquid Turned into reddish brown, remove the ice bath, let the reaction solution slowly rise to room temperature and react for 24h to terminate the reaction. After the reaction, first remove DCM and part of phosphorus oxychloride by rotary evaporator,...

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Abstract

The invention discloses a matrine pyrimidine derivative, and a preparation method and application thereof, and belongs to the technical field of medicinal chemistry. The matrine pyrimidine derivative is a compound represented by a general formula (I) shown in the specification, or a compound represented by a general formula (II) shown in the specification. The matrine pyrimidine derivative disclosed by the invention has certain inhibitory activity on human tumor cells (human prostate cancer cells DU-145, human non-small cell lung cancer cells A549, human colorectal adenocarcinoma cells HCT15 and human cervical carcinoma cells HeLa), so that proliferation and differentiation of the tumor cells can be inhibited, and a new thought is provided for research and development of anti-tumor drugs; and the preparation method disclosed by the invention is simple, convenient and controllable, and the obtained product is high in yield and extremely high in purity.

Description

technical field [0001] The invention belongs to the technical field of medicinal chemistry, and in particular relates to a matrine pyrimidine derivative and a preparation method and application thereof. Background technique [0002] Matrine is one of the main active ingredients extracted and isolated from Sophora flavescens in the early stage, and it is an alkaloid. Matrine and its derivatives have various activities, such as: anticancer, antiviral, anti-inflammatory, insecticidal, etc. Experiments have proved that matrine has a certain activity in treating cancer, but its effect is only moderate. It is speculated that this may be due to its large number of binding sites and relatively low selectivity. Therefore, improving the sensitivity and selectivity of matrine's anti-tumor target will effectively enhance the anti-cancer effect of matrine. Pyrimidine and its derivatives are very important chemical components with biological activity. Some pyrimidine derivatives have a...

Claims

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Application Information

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IPC IPC(8): C07D471/22A61P35/00A61K31/519
CPCC07D471/22A61P35/00Y02P20/55
Inventor 王立升姜文泰王兴东刘旭江俊吴黎川张淇淞
Owner GUANGXI UNIV
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