Application of compound in preparation of drug inhibiting kallikrein klk7 and its synthesis process
A kallikrein and compound technology, applied in the field of biomedicine, can solve the problems of inability to penetrate the stratum corneum of the skin, slow absorption and diffusion, and fast degradation, and achieves a simple and easy synthesis method, stable inhibition effect, and inhibition efficiency. high effect
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Embodiment 1
[0034] The application of the compound in the preparation of the medicine for inhibiting kallikrein KLK7, the structural formula of the compound is:
[0035]
Embodiment 2
[0037] The method for the compound described in Synthetic Example 1, the synthetic route is as follows:
[0038]
[0039] in:
[0040] Synthesis of Substance 23: Add Substance 21, Substance 22, and glacial acetic acid into a reaction flask, heat to reflux for 4 to 8 hours, cool, filter, wash with water, and dichloromethane to obtain Substance 23 ;
[0041] Synthesis of Substance 24: Add the mixture of Substance 23 and pyridine to the reaction bottle, then add phosphorus oxychloride dropwise, after the addition is complete, heat up to react, after the reaction is completed, cool the reaction solution to 50°C, add chloroform, and stir React, cool to 5°C, add cold water, separate the organic phase, wash the chloroform layer with cold water to be neutral, concentrate to remove chloroform, and dry to obtain the substance 24;
[0042] Synthesis of Compound IV: Add Substance 24, Substance 25, Toluene, Potassium Carbonate to the reaction flask, reflux for 4 hours, cool to 25°C, f...
Embodiment 3
[0046] The method for the compound described in synthetic embodiment 1, described synthetic route is described in embodiment 2:
[0047] Synthesis of Substance 23: Add Substance 21, Substance 22, and glacial acetic acid into a reaction flask, heat to reflux for 8 hours, cool, filter, wash with water, and dichloromethane to obtain Substance 23;
[0048] Synthesis of Substance 24: Add the mixture of Substance 23 and pyridine to the reaction bottle, then add phosphorus oxychloride dropwise, after the addition is complete, heat up to react, after the reaction is completed, cool the reaction solution to 50°C, add chloroform, and stir React, cool to 5°C, add cold water, separate the organic phase, wash the chloroform layer with cold water to be neutral, concentrate to remove chloroform, and dry to obtain the substance 24;
[0049] Synthesis of Compound IV: Add Substance 24, Substance 25, Toluene, Potassium Carbonate to the reaction flask, reflux for 4 hours, cool to 25°C, filter, wash...
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