Natural product-led drug discovery has made a strong come back in recent years.One of the key steps in natural product research is the isolation of bioactive compounds.Compared to synthetic compounds, natural products are often sterically more complex, with more bridgehead tetrahedral carbon atoms, rings, and chiral centers.Since optical isomers could possess considerable different bioactivities, it is therefore important to resolve these enantiomers and diastereomers to better understand their respective pharmacological activities.