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Purification of Artemisinin from the Product Solution of a Semisynthetic Reaction within a Single Crystallization Step
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2019-07-12 00:00:00 , DOI: 10.1021/acs.oprd.9b00175 Elena Horosanskaia 1, 2 , Susann Triemer 1 , Andreas Seidel-Morgenstern 1, 2 , Heike Lorenz 1
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2019-07-12 00:00:00 , DOI: 10.1021/acs.oprd.9b00175 Elena Horosanskaia 1, 2 , Susann Triemer 1 , Andreas Seidel-Morgenstern 1, 2 , Heike Lorenz 1
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Artemisinin, a natural compound isolated from the Artemisia annua L. plant, represents an indispensable ingredient in artemsisinin-based combination therapies (ACT) against malaria. Starting from dihydroartemisinic acid, a biosynthetic precursor of the target, a semisynthetic pathway described previously provides in the reactor effluent approximately 69% artemisinin together with structurally similar byproducts. Successful purification of artemisinin was achieved by a combination of continuous chromatography and crystallization. This work is directed to isolate crystalline artemisinin of high purity from the effluent of the catalytic reaction by crystallization only. On the basis of knowledge of artemisinin solubility and nucleation behavior in the reaction medium, a seeded cooling crystallization was designed and implemented subsequent to organic synthesis. It provided crystalline artemisinin with a final purity of 99.9% in a single straightforward crystallization step, simplifying the overall purification process significantly. The new purification method was further demonstrated to successfully isolate pure crystalline artemisinin from a synthesis solution produced directly using crude A. annua extract as initial feed.
中文翻译：
在单个结晶步骤中从半合成反应的产物溶液中纯化青蒿素
青蒿素，一种从青蒿中分离的天然化合物植物乳杆菌代表基于青蒿素的抗疟疾联合疗法（ACT）中必不可少的成分。从靶的生物合成前体二氢青蒿酸开始，先前描述的半合成途径在反应器流出物中提供约69％的青蒿素以及结构相似的副产物。通过连续色谱和结晶相结合，成功纯化了青蒿素。该工作旨在仅通过结晶从催化反应的流出物中分离出高纯度的结晶青蒿素。基于青蒿素在反应介质中的溶解度和成核行为的知识，设计并在有机合成后实施了晶种冷却结晶。它在一个简单的结晶步骤中为结晶青蒿素提供了99.9％的最终纯度，从而大大简化了整个纯化过程。进一步证明了这种新的纯化方法可以成功地从直接使用粗品生产的合成溶液中分离出纯结晶的青蒿素秋葵提取物作为初始饲料。
更新日期：2019-07-12
中文翻译：
在单个结晶步骤中从半合成反应的产物溶液中纯化青蒿素
青蒿素，一种从青蒿中分离的天然化合物植物乳杆菌代表基于青蒿素的抗疟疾联合疗法（ACT）中必不可少的成分。从靶的生物合成前体二氢青蒿酸开始，先前描述的半合成途径在反应器流出物中提供约69％的青蒿素以及结构相似的副产物。通过连续色谱和结晶相结合，成功纯化了青蒿素。该工作旨在仅通过结晶从催化反应的流出物中分离出高纯度的结晶青蒿素。基于青蒿素在反应介质中的溶解度和成核行为的知识，设计并在有机合成后实施了晶种冷却结晶。它在一个简单的结晶步骤中为结晶青蒿素提供了99.9％的最终纯度，从而大大简化了整个纯化过程。进一步证明了这种新的纯化方法可以成功地从直接使用粗品生产的合成溶液中分离出纯结晶的青蒿素秋葵提取物作为初始饲料。
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