作者:Anthonius H. J. Engwerda、Rick Maassen、Paul Tinnemans、Hugo Meekes、Floris P. J. T. Rutjes、Elias Vlieg
DOI:10.1002/anie.201811289
日期:2019.2.4
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
甲氟喹是预防和治疗疟疾的重要药物。它可以消旋混合物形式商购获得,其中只有一种对映异构体具有抗疟疾的活性,而另一种对映异构体却具有严重的精神作用。通过将药物转化为可消旋的外消旋团聚体结晶的化合物,实现了甲氟喹的脱消氨作用为所需的对映异构体。