Ruthenium-catalyzed enantioselective hydrogenation of quinoxalinones and quinazolinones

An efficient Ru-catalyzed enantioselective hydrogenation of quinoxalinone and quinazolinone derivatives has been successfully developed, providing a straightforward and facile access to chiral dihydroquinoxalinones and dihydroquinazolinones with excellent results (89-98% yields, up to 98% ee). Importantly, the key enantiopure dihydroquinoxalinone intermediate towards the synthesis of a bioactive BRD4 inhibitor was conveniently synthesized by this catalytic hydrogenation methodology.

Automated summary

An efficient Ru-catalyzed enantioselective hydrogenation method has been successfully developed for the synthesis of chiral dihydroquinoxalinones and dihydroquinazolinones with excellent results (89-98% yields, up to 98% ee). Additionally, a key enantiopure dihydroquinoxalinone intermediate towards the synthesis of a bioactive BRD4 inhibitor was conveniently synthesized using this catalytic hydrogenation methodology.