Compound for inhibiting COX (cyclooxygenase)-2 as well as preparation method and application thereof
A cyclooxygenase and compound technology, which is applied in the directions of organic chemistry, pharmaceutical combination, pharmaceutical formulation, etc., can solve problems such as low bioavailability, and achieve the effects of simple preparation method, mild conditions and high yield.
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Embodiment 1
[0054] Preparation method of compound inhibiting cyclooxygenase-2
[0055] 1.1 Synthesis of genipin methylated intermediate a
[0056] Dissolve 3g of genipin in 180g of anhydrous methanol, cool to 0°C in an ice bath, and quickly add 1.68g of boron trifluoride ether, then stir at room temperature (220r min -1 ) reaction, TLC detects the reaction process, after the reaction is complete, add saturated NaHCO 3 Quenching is carried out, then the reaction solution is extracted with an organic solvent and the organic phase is separated and collected, and finally the organic phase is treated with anhydrous Na 2 SO 4 Carrying out drying treatment, and then distilling off the organic solvent to obtain a colorless oily liquid, which is the genipin methylated intermediate a;
[0057] 1.2 Synthesis of compounds that inhibit cyclooxygenase-2
[0058] Take 1g of genipin methylation intermediate a, add triethylamine to adjust the pH value to 9, cool to 0°C in an ice bath, slowly add 3g of...
Embodiment 2
[0064] Preparation method of compound inhibiting cyclooxygenase-2
[0065] 2.1 Synthesis of genipin methylation intermediate a
[0066] Dissolve 3g of genipin in 120g of anhydrous methanol, cool to 0°C in an ice bath, and quickly add 1.68g of boron trifluoride ether, then stir at room temperature (220r min -1 ) reaction, TLC detects the reaction process, after the reaction is complete, add saturated NaHCO 3 Quenching is carried out, then the reaction solution is extracted with an organic solvent and the organic phase is separated and collected, and finally the organic phase is treated with anhydrous Na 2 SO 4Carrying out drying treatment, and then distilling off the organic solvent to obtain a colorless oily liquid, which is the genipin methylated intermediate a;
[0067] 2.2 Synthesis of compounds that inhibit cyclooxygenase-2
[0068] Take 1g of genipin methylation intermediate a, add triethylamine to adjust the pH value to 8, cool to 0°C in an ice bath, slowly add 3g of...
Embodiment 3
[0074] Preparation method of compound inhibiting cyclooxygenase-2
[0075] 3.1 Synthesis of genipin methylated intermediate a
[0076] Dissolve 3g of genipin in 150g of anhydrous methanol, cool to 0°C in an ice bath, and quickly add 1.68g of boron trifluoride ether, then stir at room temperature (220r min -1 ) reaction, TLC detects the reaction process, after the reaction is complete, add saturated NaHCO 3 Quenching is carried out, then the reaction solution is extracted with an organic solvent and the organic phase is separated and collected, and finally the organic phase is treated with anhydrous Na 2 SO 4 Carrying out drying treatment, and then distilling off the organic solvent to obtain a colorless oily liquid, which is the genipin methylated intermediate a;
[0077] 3.2 Synthesis of compounds that inhibit cyclooxygenase-2
[0078] Take 1g of genipin methylation intermediate a, add triethylamine to adjust the pH value to 9, cool to 0°C in an ice bath, slowly add 3g of...
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