Approaches for multi-gram scale isolation of enantiomers for drug discovery.

作者: Daniela Rossi , Marilù Tarantino , Giacomo Rossino , Marta Rui , Markus Juza

DOI: 10.1080/17460441.2017.1383981

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摘要: ABSTRACTIntroduction: Over the last 30 years, scientific community has directed its efforts towards identification of enantioselective approaches to obtain desired active enantiomer. Accordingly, efficient production single enantiomers from small large scale, throughout Drug Discovery (DD) programs, become great interest and a fundamental challenge.Areas covered: This review focuses on two strategies for preparing in high yields with an excellent enantiomeric excess (ee). Separation racemates, synthesis procedures, integrated have been extensively reviewed, offer guide that enables selection suitable methodology producing pure scales large.Expert opinion: past decades, drug regulatory agencies set strict rules use racemates enantiomers, leading transformation market. Indeed, number drugs approved as ...

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