Protocol for stereodivergent asymmetric hydrogenation of quinoxalines

Chiral 1,2,3,4-tetrahydroquinoxalines are ubiquitous in natural products and bioactive molecules. Herein, we disclose a protocol for stereodivergent asymmetric hydrogenation of disubstituted quinoxalines for the preparation of both cis- and trans-enantioenriched disubstituted tetrahydroquinoxalines (up to >20:1 d.r. and 99% ee). We describe steps for synthesis of ligands and substrate, setup of hydrogenation of disubstituted quinoxalines, and purification of products. Additionally, we provide detailed diagrams of the hydrogenation installation. For complete details on the use and execution of this protocol, please refer to Liu et al.(1)