拉米夫定
化学
三氟甲磺酸
水合物
产量(工程)
吡啶
连续流动
组合化学
溶剂
催化作用
有机化学
乙型肝炎病毒
病毒学
病毒
冶金
材料科学
物理
生物
机械
作者
Devender Mandala,Sravanthi Chada,Paul Watts
摘要
We report the first continuous flow synthesis of lamivudine, an antiretroviral drug used in the treatment of HIV/AIDS and hepatitis B. The key intermediate (5-acetoxy oxathiolane) was prepared by an integrated two step continuous flow process from l-menthyl glyoxalate hydrate in a single solvent, in 95% overall conversion. For the crucial glycosidation reaction, using pyridinium triflate as the novel catalyst, an improved conversion of 95% was obtained. The overall isolated yield of the desired isomer of lamivudine (40%) was improved in the flow synthesis compared to the batch process.
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