增强消旋化的抗疟药物甲氟喹的损耗。
Attrition-Enhanced Deracemization of the Antimalaria Drug Mefloquine.
机构信息
Institute for Molecules and Materials, Radboud University, Heyendaalseweg 135, 6525, AJ, Nijmegen, The Netherlands.
出版信息
Angew Chem Int Ed Engl. 2019 Feb 4;58(6):1670-1673. doi: 10.1002/anie.201811289. Epub 2018 Dec 21.
PMID:30508314
Abstract
Mefloquine is an important drug for prevention and treatment of malaria. It is commercially available as a racemic mixture, wherein only one enantiomer is active against malaria, while the other one causes severe psychotropic effects. By converting the drug into a compound that crystallizes as a racemizable racemic conglomerate, the deracemization of mefloquine into the desired enantiomer was achieved.
摘要
盐酸甲氟喹是一种重要的疟疾预防和治疗药物。它有消旋混合物形式的商品出售，其中只有一个对映异构体对疟疾有活性，而另一个则会产生严重的精神作用。通过将药物转化为结晶为外消旋外消旋混合物的化合物，实现了盐酸甲氟喹向所需对映异构体的去消旋化。
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