We report here a
Ru-catalyzed enantioselective synthesis of biaryl-bridged
NH lactams through asymmetric reductive amination and a spontaneous
ring-closing cascade from keto esters and NH4OAc with H2 as reductant. The reaction features broad substrate generality
and high enantioselectivities (up to >99% ee). To showcase the
practical
utility, a highly enantioselective synthesis of 5-ethylindolobenzazepinone C, a promising antimitotic agent, has been rapidly completed.
Furthermore, the amide group in the products enables versatile elaborations
through directed C–H functionalization.