Brominated PTP1B inhibitor as well as synthesis method and application thereof in preparation of medicine for curing type 2 diabetes
A kind of inhibitor, bromination technology, applied in the field of chemical total synthesis of brominated compound bis-methane, can solve the problems of poor chemical and biological stability, not much, high electronegativity, etc., and achieve good industrial production prospects and process Simple operation and reduced reaction cost
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Embodiment 1
[0029] Example 1 The chemical synthesis and structural identification of "bis-(2,3-dibromo-4,5-dimethoxy-phenyl)-methane"
[0030] (1) Chemical synthesis and structure identification of Bis-(3,4-dimethoxy-phenyl)-methanone3
[0031] Add 44.16g (240mmol) veratrol (compound 1), 33.84g (240mmol) veratrol (compound 2) and 200g polyphosphoric acid into a 1000ml three-necked reaction flask according to the molar ratio of 1:1, and stir at 80°C for reaction 1h; Cool to 60°C and add 500ml of ice water dropwise to the reactant within 30min, at this time, a large amount of water-insoluble pink solid precipitates out of the reactant; after removing water by filtration, dissolve the obtained solid in 200ml of dichloromethane , washed three times with an equal volume of 3% sodium hydroxide solution and distilled water successively; after drying the dichloromethane phase with anhydrous sodium sulfate, concentrate under reduced pressure to obtain a pink solid; wash the solid with petroleum et...
Embodiment 2
[0039] Example 2 Determination of protein tyrosine phospholipase 1B inhibitory activity
[0040] Prepare the test compound bis-(2,3-dibromo-4,5-dimethoxy-phenyl)-methane with DMSO into different concentrations of the test solution, take 2 μL of the test solution and add it to the standard The bioassay system (50mM Tris-HCl, PH 6.5, 2mM pNPP, 2% DMSO, 30nM hGST-PTP1B), negative control: DMSO, positive control: sodium orthovanadate, the reaction temperature is 30°C, and the dynamic measurement wavelength is 405nm The light absorption at the time of 3min, according to the following formula to calculate the inhibitory rate of compound PTP1B enzyme activity. Inhibition rate=(experimental group A value-negative control group A value) / (control group A value-negative control group A)×100%, the results are shown in Table 1.
[0041] Table 1 protein tyrosine phospholipase 1B inhibition rate (%)
[0042] Table 1 Inhibitory Ratio(%)of PTP1B
[0043]
[0044] The test results show th...
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