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Artesunate purification process

A technology of artesunate and process, which is applied in the field of artesunate purification process, can solve the problems of complex crystallization steps, unsuitability for industrial production, and long time, and achieve shortened crystallization time, short reaction time, energy consumption and environmental protection Effect

Active Publication Date: 2013-10-30
重庆恒星生物技术有限责任公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The crystallization step is complicated to operate and takes a long time, which is not suitable for industrial production

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Weigh 1kg dihydroartemisinin, 18L chloroform, 1kg succinic anhydride, 0.12L triethylamine, add chloroform, dihydroartemisinin, succinic anhydride, triethylamine successively in the reaction tank, Stir the reaction at room temperature, react for 1 hour, the thin layer chromatography detects that the reaction is complete, add dilute hydrochloric acid until acidic to terminate the reaction.

[0026] Transfer the reaction solution into an extraction tank, add the same volume of pure water for extraction, repeat the extraction step 3 times, filter the reaction solution, and concentrate the filtrate to 1 / 20 of the original volume at 60°C.

[0027] Add an equal volume of petroleum ether, stir evenly, let stand for 4 minutes to crystallize, centrifugally filter, and dry at 60°C to obtain 1.32 kg of crude artesunate.

[0028] Add 1.32L of methanol, stir at room temperature to dissolve, after completely dissolved, add purified water, and stir while adding water, until the artesun...

Embodiment 2

[0031] Weigh 10kg dihydroartemisinin, 180L chloroform, 8kg succinic anhydride, 1L triethylamine, add chloroform, dihydroartemisinin, succinic anhydride, triethylamine in turn in the reaction tank, The reaction was stirred and reacted for 1.5 hours. Thin-layer chromatography detected that the reaction was complete, and dilute hydrochloric acid was added until acidic to terminate the reaction.

[0032] Transfer the reaction solution into an extraction tank, add the same volume of pure water for extraction, repeat the extraction step 5 times, filter the reaction solution, and concentrate the filtrate at 60°C to 1 / 25 of the original volume.

[0033] Add an equal volume of petroleum ether, stir evenly, let stand for 5 minutes to crystallize, centrifugally filter, and dry at 60°C to obtain 13.0 kg of crude artesunate.

[0034] Add 13.0L of methanol, stir at room temperature to dissolve, after completely dissolved, add pure water, stir while adding water, until all artesunate crystal...

Embodiment 3

[0037] Take by weighing 20kg dihydroartemisinin, 360L chloroform, 16kg succinic anhydride, 2.4L triethylamine, add chloroform, dihydroartemisinin, succinic anhydride, triethylamine successively in reaction tank, in Stir the reaction at room temperature, react for 1 hour, the thin layer chromatography detects that the reaction is complete, add dilute hydrochloric acid until acidic to terminate the reaction.

[0038] Transfer the reaction solution into an extraction tank, add the same volume of pure water for extraction, repeat the extraction step 4 times, filter the reaction solution, and concentrate the filtrate at 60°C to 1 / 20 of the original volume.

[0039] Add an equal volume of petroleum ether, stir evenly, let stand for 6 minutes to crystallize, centrifugally filter, and dry at 50°C to obtain 26.2 kg of crude artesunate.

[0040] Add 26.2L of methanol, stir at room temperature to dissolve, after completely dissolved, add purified water, and stir while adding water, until...

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PUM

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Abstract

The invention relates to an artesunate purification process, and aims to provide an artesunate purification process with simple process, high yield and short crystallization time, and a preparation method. The artesunate purification process comprises six steps including esterification, extraction, concentration, crystallization, purification and drying. The process provided by the invention simplifies the purification and separation of artesunate, has advantages of short reaction time, especially greatly shortened crystallization time of only 4-6 min, product yield above 93%, product purity higher than 99%, recyclable solvents, low energy consumption and environmental protection, so as to greatly reduce costs of artesunate anti-malaria drugs and contribute to the public welfare of the global against malaria resistance.

Description

technical field [0001] The invention relates to a medicine purification process, in particular to an artesunate purification process. Background technique [0002] Artesunate is a derivative of artemisinin synthesized from dihydroartemisinin, and its chemical formula is C 19 h 28 o 8 , white crystal, melting point 1290~1400℃, odorless, bitter taste, easily soluble in chloroform, soluble in acetone, slightly soluble in methanol or ethanol, almost insoluble in water. Artesunate is a specific antimalarial drug, which has a strong killing effect on Plasmodium asexuals and can quickly control the onset of malaria. It can be used alone as oral preparations and injections, and can also be combined with amodiaquine hydrochloride and other drugs Compatible with compound oral preparations and injections, it is one of the best antimalarial drugs. In addition, artesunate and weak base can form artesunate salt, which is easily soluble in water. It is convenient to make injections in ...

Claims

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Application Information

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IPC IPC(8): C07D493/20
CPCY02A50/30
Inventor 罗庆林侯磊崔小荣
Owner 重庆恒星生物技术有限责任公司
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