Alpha-mangostin derivatives as well as preparation method and application thereof
A technology of nimbin and its derivatives, which is applied in the field of medicine, can solve problems such as difficult to achieve therapeutic effect, lack of therapeutic effect on cerebral infarction or vascular dementia, and achieve high safety, good therapeutic effect, and reduced toxicity
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Embodiment 1
[0038] Embodiment 1: the synthesis (synthetic route figure such as figure 1 shown)
[0039]
[0040] Take α-Neebisin (40mg, 0.1mmol) in toluene solution, stir until dissolved, the solution turns yellow at this time, add 2,3-dichloro-5,6 dicyanoquinone (DDQ, 45mg, 0.2mmol) , reacted at 40°C, detected by TLC during the reaction, the reaction was completed after 5 hours, the toluene was distilled off under reduced pressure, separated and purified by silica gel column chromatography, and the yellow solid compound HZA was obtained with a yield of 85%.
[0041] Weigh BTC (60mg, 0.202mmol) into a 25mL two-necked bottle, add 5mL of anhydrous dichloromethane, stir magnetically, add equivalent N-methylaniline, triethylamine (0.25mmol) and Add 5mL of dichloromethane slowly in an ice bath, remove the ice-salt bath after the addition, and stir at room temperature for 4 hours.
[0042] Add HZA (40mg, 0.1mmol) to a 10ml single-necked bottle, add a trace of DMAP, 5mL of dichloromethane, ...
Embodiment 2
[0044] Embodiment 2: the synthesis (synthetic route figure such as figure 1 shown)
[0045]
[0046] The synthetic method of compound HZA is the same as above.
[0047] Weigh BTC (58mg, 0.2mmol) into a 25mL two-necked bottle, add 5mL of anhydrous dichloromethane, stir magnetically, add an equivalent amount of N-ethylaniline, triethylamine (0.25mmol) and Add 5mL of dichloromethane slowly in an ice bath, remove the ice-salt bath after the addition, and stir at room temperature for 4 hours.
[0048] Add HZA (40mg, 0.1mmol) to a 10ml single-necked bottle, add a trace of DMAP, 5mL of dichloromethane, and stir magnetically at room temperature until completely dissolved. Slowly add the solution dropwise to the reaction solution in the previous step under the ice-salt bath, remove the ice-salt bath after the dropwise addition, and stir at room temperature. After the reaction is completed, add 3 to 6 times the volume of distilled water to the above reaction solution, then extract...
Embodiment 3
[0050] Embodiment 3: the synthesis (synthetic route figure such as figure 1 shown)
[0051]
[0052] The synthetic method of compound HZA is the same as above.
[0053] Weigh BTC (58mg, 0.2mmol) into a 25mL two-necked bottle, add 5mL of anhydrous dichloromethane, stir magnetically, add an equivalent amount of N-methyl-o-methylaniline, triethylamine (0.25 mmol) and 5mL of dichloromethane were slowly added dropwise in an ice bath, and the ice-salt bath was removed after the dropwise addition, and stirred at room temperature for 4h.
[0054] Add HZA (40mg, 0.1mmol) to a 10ml single-necked bottle, add a trace of DMAP, 5mL of dichloromethane, and stir magnetically at room temperature until completely dissolved. Slowly add the solution dropwise to the reaction solution in the previous step under the ice-salt bath, remove the ice-salt bath after the dropwise addition, and stir at room temperature. After the reaction is completed, add 3 to 6 times the volume of distilled water t...
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