Francotte Eric, Leutert Thomas, La Vecchia Luiggi, Ossola Flavio, Richert Paul, Schmidt Alfred
Central Technologies, Novartis Pharma AG, Basel, Switzerland.
Chirality. 2002 May 5;14(4):313-7. doi: 10.1002/chir.10042.
The enantiomers of two different derivatives of tert-leucine were separated by continuous chromatography on chiral stationary phases applying the simulated moving bed technique. About 1 kg of racemic N-carbobenzoxy-tert-leucine was resolved on the cellulose-based phase Chiralcel OD using a mixture of heptane/ethanol and 0.1% of trifluoroacetic acid modifier as the mobile phase, while 520 g of the N-Boc-tert-leucine-benzylester was resolved on the amylose-based phase Chiralpak AD with a mixture of heptane/2-propanol as the mobile phase. In both instances the corresponding enantiomers were obtained in high yield and high optical purity.
采用模拟移动床技术，在手性固定相上通过连续色谱法分离了叔亮氨酸两种不同衍生物的对映体。使用庚烷/乙醇混合物和0.1%三氟乙酸改性剂作为流动相，在纤维素基手性固定相Chiralcel OD上拆分了约1 kg外消旋N-苄氧羰基-叔亮氨酸；而使用庚烷/2-丙醇混合物作为流动相，在直链淀粉基手性固定相Chiralpak AD上拆分了520 g N-Boc-叔亮氨酸-苄酯。在这两种情况下，均以高收率和高光学纯度得到了相应的对映体。
