Water-soluble triptolide derivative and preparation method and application thereof
A technology of triptolide and its derivatives, applied in the field of medicine, can solve the problems of triptolide's poor water solubility, limited research and development, narrow therapeutic window, etc., and achieve the goals of improving water solubility, facilitating salt formation, and reducing toxic and side effects Effect
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Embodiment 1
[0038] The preparation method of the water-soluble triptolide derivative of the present embodiment specifically comprises the following steps:
[0039]
[0040] (1) After mixing 1.0g (6.58mmol) of hydroquinone and 0.54g (7.50mmol) of acrylic acid, add it to 10mL of methanesulfonic acid at one time, heat and stir at 70°C for 18h, TLC detects that the reaction is complete, stop stirring, and add 125mL of water, It was extracted with ethyl acetate successively, washed with pure water, saturated aqueous sodium bicarbonate solution and saturated brine, dried over anhydrous sodium sulfate, and evaporated to dryness under reduced pressure. Recrystallized from chloroform-n-hexane to obtain a yellow solid compound XC-01 with a yield of about 67%. [M+H] + :221.0; 1 H NMR, 600MHz (CDCl 3 )δ6.45(q,1H), 3.04(s,2H), 1.96(m,3H), 1.92(m,3H), 1.41(s,6H).
[0041]
[0042] (2) 1.1g (5mmol) of the compound of step (1) was dissolved in 40mL of acetic acid solution; 0.57mL (11mmol) of br...
Embodiment 2
[0062] The preparation method of the water-soluble triptolide derivative of the present embodiment specifically comprises the following steps:
[0063] (1) For every 1.0g (6.58mmol) of hydroquinone, mix with 0.85g (7.50mmol) of 3-methyl-2-butenoic acid and add to 10mL methanesulfonic acid at one time, heat and stir at 70°C for 4h, TLC Check that the reaction is complete, stop stirring, add 125mL of water, extract with ethyl acetate successively, wash with water, saturated aqueous sodium bicarbonate solution and saturated brine, dry over anhydrous sodium sulfate, evaporate to dryness under reduced pressure, and recrystallize with chloroform-n-hexane to obtain yellow solid. [M+H] + :221.0; 1 H NMR, 600MHz (CDCl 3 )δ6.45(q,1H), 3.04(s,2H), 1.96(m,3H), 1.92(m,3H), 1.41(s,6H).
[0064] (2) 6.6g (30mmol) of the compound in step (1) was dissolved in 200mL of acetic acid solution; 3.4mL (66mmol) of bromine water was added dropwise to the above solution and stirred at room temperat...
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