Enantioselective Construction of Pyrimidine-Fused Diazepinone Derivatives Bearing a Tertiary Stereogenic Center Enabled by Iridium-Catalysed Intramolecular Allylic Substitution

The iridium-catalysed enantioselective intramolecular allylic substitution of pyrimidine-tethered allylic carbonates was developed. A wide range of chiral pyrimidine-fused diazepinone derivatives were successfully constructed in 88-96% yields with 85-99% ees. This work further highlights the power of chiral-bridged biphenyl phosphoramidites in asymmetric synthesis.

Automated summary

In this study, the iridium-catalysed enantioselective intramolecular allylic substitution of pyrimidine-tethered allylic carbonates was developed, leading to the successful construction of a wide range of chiral pyrimidine-fused diazepinone derivatives with high yields and enantiomeric excesses. This work further highlights the power of chiral-bridged biphenyl phosphoramidites in asymmetric synthesis.