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Enabling Enantiopurity: Combining Racemization and Dual-Drug Co-crystal Resolution
Crystal Growth & Design ( IF 3.8 ) Pub Date : 2018-04-23 00:00:00 , DOI: 10.1021/acs.cgd.8b00438
Bram Harmsen 1 , Tom Leyssens 1
Affiliation  

A new process methodology to obtain enantiopure (S)-Ibuprofen has been designed. Starting from racemic Ibuprofen, co-crystallization with Levetiracetam is used as a resolution tool to obtain only the target enantiomer, (S)-Ibuprofen, in the solid state. The resulting mother liquor, enriched in (R)-Ibuprofen, is recovered and submitted to a racemization cycle, after which another co-crystallization step is introduced. Levetiracetam can be recovered from the co-crystal phase and reused, resulting in an economical use of the resolution agent. Overall, a novel approach to transform a racemic compound into enantiopure material has been developed.

中文翻译:

启用对映体纯度:将消旋和双药物共晶体拆分相结合

设计了一种新的工艺方法来获得对映纯(S)-布洛芬。从外消旋布洛芬开始,与左乙拉西坦共结晶被用作拆分工具,仅获得固态的目标对映异构体(S)-布洛芬。回收富含(R)-布洛芬的所得母液并进行消旋化循环,此后引入另一共结晶步骤。左乙拉西坦可从共结晶相中回收并再利用,从而可经济地使用拆分剂。总的来说,已经开发了一种将外消旋化合物转变为对映体纯净材料的新颖方法。
更新日期:2018-04-23
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