Diarylpyrimidine compound, composition and application
A compound and composition technology, applied in the field of medicine, can solve the problems of poor drug resistance and achieve the effect of great application value
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Embodiment 1
[0070] The preparation of embodiment 1 target molecule
[0071] The thin-layer chromatography silica gel plate uses Yantai Huanghai HSGF254 or Qingdao GF254 silica gel plate, the specification of the silicon amine plate used in thin-layer chromatography (TLC) is 0.15mm-0.2mm, and the specification of thin-layer chromatography separation and purification product is 0.4 mm-0.5mm.
[0072] The raw materials used in the present invention are mainly purchased from Sinopharm Chemical Reagent Co., Ltd., Beijing Coup Technology Co., Ltd., Aladdin Chemical Reagent Co., Ltd., Darui Chemicals and other companies.
[0073] Unless otherwise specified in the examples, the solution refers to an aqueous solution.
[0074] Unless otherwise specified in the examples, the reaction temperature is room temperature, which is 20°C-30°C.
[0075] The technical scheme that the present invention adopts is as follows:
[0076]
[0077] Synthetic route of compound (Ⅰ). Reagents and conditions: (a) ...
Embodiment 2
[0183] Example 2 Evaluation of biological activity of target molecule
[0184] 1. In vitro test method for receptor tyrosine kinase inhibitory activity
[0185] Prepare Kinase Assay Buffer
[0186] ① Melt the Kinase Detection Buffer at room temperature and observe whether there is precipitation.
[0187] ②If precipitation occurs, incubate at 37°C (Kinase Detection Buffer) for 15 minutes and shake frequently to dissolve the precipitation. Alternatively, carefully aspirate the supernatant to remove the pellet.
[0188] Prepare Kinase Assay Reagents
[0189] ①Equilibrate Kinase Detection Buffer (Kinase Detection Buffer) and (Kinase Detection Substrate) at room temperature before use.
[0190] ② Pour all the Kinase Detection Buffer into the brown bottle containing the Kinase Detection Substrate to dissolve the lyophilized powder substrate, thus making the Kinase Detection Reagent.
[0191] ③Gently oscillate, vortex or invert to mix to form a homogeneous solution, and the subs...
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