School of Pharmacy, China Pharmaceutical University, Jiangsu, Nanjing 210009 (China).
Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Shanghai 201203 (China).
Angew Chem Int Ed Engl. 2015 Oct 26;54(44):12918-22. doi: 10.1002/anie.201507273. Epub 2015 Sep 14.
Structurally simple and inexpensive chiral tridentate ligands were employed for substantially advancing the purely chemical dynamic kinetic resolution (DKR) of unprotected racemic tailor-made α-amino acids (TM-α-AAs), enabling the first DKR of TM-α-AAs bearing tertiary alkyl chains as well as multiple unprotected functional groups. Owing to the operationally convenient conditions, virtually complete stereoselectivity, and full recyclability of the source of chirality, this method should find wide applications for the preparation of TM-α-AAs, especially on large scale.
我们使用结构简单、价格低廉的手性三齿配体，大大推进了未保护的外消旋手性定制α-氨基酸（TM-α-AAs）的纯化学动态动力学拆分（DKR），实现了首例带有叔烷基链和多个未保护官能团的 TM-α-AAs 的 DKR。由于操作条件方便、立体选择性几乎完全以及手性源的可完全回收性，该方法应该会广泛应用于 TM-α-AAs 的制备，尤其是大规模制备。
