Preparation method of hydroxycamptothecine
A technology of hydroxycamptothecin and camptothecin, which is applied in the field of preparation of hydroxycamptothecin, can solve the problems of low safety factor, long time-consuming, inconvenient reaction operation, etc., achieve high total yield, simple experimental operation, increase light The effect of chemical reaction conversion rate
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[0024] The specific technical solutions of the present invention are described in conjunction with the embodiments.
[0025] The preparation method of hydroxycamptothecin includes the following steps:
[0026] (1) N-oxidation reaction
[0027] Accurately weigh an appropriate amount of camptothecin and place it in a round bottom flask. Heat in a water bath, add acid solvent at 30-45°C and stir for 10 min to dissolve camptothecin. Increase the temperature to 60-70°C at a uniform speed, add sodium perborate as an oxidizer, continue to stir and reflux. Warm up and continue to respond. When the reaction is over, stop heating and cool to room temperature naturally. The reaction solution was concentrated under reduced pressure, a large amount of ice water was added to the concentrated solution, and it was allowed to stand for crystallization. After the crystals are completely precipitated, they are filtered, washed with a small amount of distilled water, and dried to obtain 1-oxycampto...
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