Isoquinoline-1,3-(2h,4h)-dione substituted with methyl isobutyrate group and its preparation method and use

Abstract

The invention discloses isoquinoline-1,3(2H, 4H)-diketone containing isobutyric acid dimethyl ester groups and a preparation method and application thereof. The compound has the structure shown in the formula (I). The preparation method includes the steps that N-methacrylyl-N-alkylbenzene formamide serves as a substrate, dimethyl 2,2'-azobis(2-methylpropionate) serves as a free radical source, copper iodide serves as a catalyst, K3PO4 serves as alkali, DMF serves as a solvent, reaction is conducted in the air environment, reaction temperature is 90 DEG C, and the compound is obtained through column chromatography or thin-layer chromatography separation and purification after five hours of reaction. The compound shows a good inhibition effect on prostate cancer cells 22RV, some compounds obtained from the compound have good prospects in the aspect of prostatic cancer treatment, and a good opportunity is provided for fixing lead compounds for treating prostatic cancer. The synthesis reaction is easy to operate, a reaction system is mild, conditions are simple, cost is low, the yield is high, and the compound has great application and popularization value. Please see the formula (I) in the description.

Description

technical field [0001] The present invention relates to a class of isoquinoline-1,3-(2 H ,4 H )-diketone compounds and their preparation and use. Background technique [0002] Among many heterocyclic compounds, isoquinolinones and their derivatives have attracted widespread attention due to their remarkable pharmacological and biological activities. Several typical isoquinolines as shown in chemical formula 1-1,3-(2 H ,4 H )-diketone compounds, which exhibit important physiological activities, such as analgesia, anti-tumor, HIV-I RT inhibitor, 5-HT3 receptor antagonist, etc. Therefore, the development of nitrile-substituted isoquinoline-1,3(2 H, 4 H )-diketone compound synthesis method has important practical and theoretical value. [0003] [0004] chemical formula 1 [0005] So far, isoquinoline-1,3(2 H ,4 H )-diketone synthesis method has not been reported yet, we found N -Dimethylpropylene- N -Methyl N-methacryloyl-N-alkylbenzamide, such as the dimethyl az...

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Problems solved by technology

[0005] So far, isoquinoline-1,3(2 H ,4 H )-diketone synthesis method has not been reported yet, we found N -Dimethylpropene- N -Methyl N-methacryloyl-N-alkylbenzamide, such as the dimethyl azobisisobutyrate under the catalysis of cuprous iodide, effectively converts dimethyl isobutyrate under mild conditions for the first time Group attacking isoquinoline-1,3(2 H ,4 H )-diketone

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