State Key Laboratory of Bioreactor Engineering, Shanghai Key Laboratory of New Drug Design, School of Pharmacy, East China University of Science and Technology, Shanghai 200237, China.
Org Biomol Chem. 2018 Jan 17;16(3):380-383. doi: 10.1039/c7ob02599h.
Reported herein is a chiral Brønsted acid-catalyzed asymmetric intramolecular allylic amination reaction, allowing facile access to a range of biologically interesting chiral 2-substituted hydroquinolines in up to 90% yield and with up to 93% ee. Furthermore, a significant effect of an N-protecting group was observed in this asymmetric process.
本文报道了一种手性 Brønsted 酸催化的不对称分子内烯丙基胺化反应,能够以高达 90%的收率和高达 93%的对映选择性,轻松获得一系列具有生物活性的手性 2-取代氢醌啉。此外,在这个不对称过程中,N-保护基具有显著的影响。