Preparation method of stable artemisinin
A kind of artemisinin, stable technology, applied in the field of stable artemisinin preparation, can solve the problems of experiment and production danger, difficult to control the reaction, large reaction heat release, etc., to improve the reaction conversion rate, easy to operate, and speed up the reaction process Effect
Pending Publication Date: 2022-05-03
河南海汇药物研究有限公司
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Problems solved by technology
Slowly add solid sodium borohydride into the reaction system in batches, but due to the large amount of heat released by the reaction, it is often accompanied by a large amount of gas generation, which is inconvenient to operate and the reaction is not easy to control. There is a greater danger
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[0032] The following will clearly and completely describe the technical solutions in the embodiments of the present invention with reference to the accompanying drawings in the embodiments of the present invention. Obviously, the described embodiments are only some of the embodiments of the present invention, not all of them. The components of the embodiments of the invention generally described and illustrated in the figures herein may be arranged and designed in a variety of different configurations. Accordingly, the following detailed description of the embodiments of the invention provided in the accompanying drawings is not intended to limit the scope of the claimed invention, but merely represents selected embodiments of the invention. Based on the embodiments of the present invention, all other embodiments obtained by those skilled in the art without making creative efforts belong to the protection scope of the present invention.
[0033] In describing the embodiments o...
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The invention discloses a stable artemisinin preparation method which comprises the following steps: dissolving sodium borohydride in a first part of methanol solution to form a uniform sodium borohydride methanol solution; adding artemisinin into the second part of methanol solution, and stirring and mixing to obtain an artemisinin solution; adding the sodium borohydride methanol solution prepared in the step 1 into the artemisinin solution prepared in the step 2, and continuously stirring for reaction; and after the reaction is finished, adding a hydrochloric acid solution to decompose redundant sodium borohydride, then slowly dropwise adding purified water until white floccules are separated out, and carrying out suction filtration and drying to obtain dihydroartemisinin. According to the method, the feeding mode of sodium borohydride is changed, sodium borohydride is completely dissolved in a methanol solution to form a uniform liquid, the uniform liquid is added into a reaction system in a liquid phase form, the adverse effect of solid-liquid suspension on the reaction is avoided, the measure is beneficial to contact with reactants to accelerate the reaction speed, the temperature fluctuation is small, and the reaction time is shortened. The reaction is milder and controllable; the operation is simple and convenient.
Description
technical field [0001] The invention relates to the technical field of organic medicine synthesis, in particular to a stable preparation method of artemisinin. Background technique [0002] As a derivative of artemisinin, dihydroartemisinin has 48 times the antimalarial effect of artemisinin. Dihydroartemisinin is easily soluble in chloroform and can be dissolved in propanol, methanol or ethanol. It is almost insoluble in water. Since dihydroartemisinin has a good anti-malarial effect, there are many studies on the synthesis of dihydroartemisinin from artemisinin at home and abroad. Regarding the preparation process of dihydroartemisinin, the prior art mainly uses artemisinin as a raw material and sodium borohydride as a reducing agent. Most of the synthetic methods use sodium borohydride solid as reducing agent. However, from the reaction mechanism of artemisinin to synthesize dihydroartemisinin, it can be seen that the reduction of ketone by sodium borohydride is essent...
Claims
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Login to View More IPC IPC(8): C07D493/20B01J19/28B01J19/00B01F29/83
CPCC07D493/20B01J19/28B01J19/0066
Inventor 郭建钊郭宇鹏王娅娟
Owner 河南海汇药物研究有限公司