Dibenzocyclooctene lignin derivatives with bioactivity
A technology of biphenyl cyclooctene and lignans, which is applied to the preparation of organic active ingredients, organic compounds, medical preparations containing active ingredients, etc., can solve the problems of high price, achieve low toxicity, good solubility, The effect of stabilizing inhibition
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Embodiment 1
[0027] The preparation of embodiment 1 biphenyl cyclooctene lignan derivatives:
[0028] The construction method of biaryl skeleton:
[0029] 1) Ullmann-type coupling: at room temperature to 80°C, with a substrate concentration of 0.04-2.0mol / L, in 0.1-1 equivalent of tetraalkylammonium halide, in a polar organic solvent and in the presence of Zn, chiral monophosphine Under the catalysis of the ligand and the divalent or zero-valent nickel complex catalyst, the number of moles of the substrate and the number of moles of the catalyst is 10 to 100:1, react for 3 to 6 hours, and purify by column chromatography to obtain the product in a certain yield , the product was dissolved in a polar solvent and 3 equivalents of LiAlH were added at 0 °C 4 , slowly raised to room temperature, reacted for 1 hour to 3 hours, and purified by column chromatography to obtain an activity test sample. Dissolve the coupling product in tetrahydrofuran and add to 0.1-0.3mol / L SmI at -78°C 2 solution...
Embodiment 2
[0038] Embodiment 2 biological experiments:
[0039] Test materials and methods
[0040] 1. The sample was dissolved in DMSO to prepare 20mg / mL, and then diluted with DMEM culture medium to different concentrations.
[0041] 2. Cell model: HepG transfected by hepatitis B virus (HBV) 2 cells, HepG 2 2.2.15 Cells.
[0042] 3. Drug toxicity test: MTT method MTT (Aldrich)
[0043] 4. HBV antigen detection: ELISA kit from Shanghai Industrial Kehua Biotechnology Co., Ltd.
[0045] Add 120 μl (4×10 5 cells / mL) Hep G 2 .2.2.15 cells, 37°C, 5% CO 2 The monolayer was cultured for 72 hours, the supernatant was discarded, and the medicinal solution prepared to 5 concentrations as required was added, and a cell control group was set at the same time. Change the sample solution once every 3 days, co-cultivate for 9 days, discard the supernatant, add 90μL of DMEM and 10μL of the 5mg / ml MTT in the incubator for 3hours. Discard the supernatant, add 100...
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