Wang Y, Bluhm L H, Li T
Department of Chemistry, Vanderbilt University, Nashville, Tennessee 37235, USA.
Anal Chem. 2000 Nov 1;72(21):5459-65. doi: 10.1021/ac000529e.
Selection of chiral selectors for the resolution of racemic N-(1-naphthyl)leucine ester 1 was studied with a 200-member parallel library prepared on polymeric synthesis resin. Through this study, the library screening procedure developed previously is improved and other pertinent issues concerning the screening process are also addressed. The equilibration time required for screening is reduced from 24 h to approximately 3 h. Excellent correlation of the outcome between the resin batch equilibration experiment and chromatographic separation is further demonstrated. It is also demonstrated that selectors with separation factors as low as 1.4 could be identified by this batch screening process. In addition, a great deal of information regarding enantioselective interactions was obtained in this parallel library study. Such information should prove useful in improving future library designs.
利用在聚合物合成树脂上制备的包含200个成员的平行文库,研究了用于拆分外消旋N-(1-萘基)亮氨酸酯1的手性选择剂。通过这项研究,改进了之前开发的文库筛选程序,并解决了与筛选过程相关的其他问题。筛选所需的平衡时间从24小时减少到约3小时。进一步证明了树脂批次平衡实验与色谱分离结果之间具有良好的相关性。还证明了通过该批次筛选过程可以识别分离因子低至1.4的选择剂。此外,在这项平行文库研究中获得了大量关于对映选择性相互作用的信息。这些信息应有助于改进未来的文库设计。