Diastereoselective Synthesis of Cyclobutanes via Rh-Catalyzed Unprecedented C–C Bond Cleavage of Alkylidenecyclopropanes

The stereoselective synthesis of highly substituted cyclobutanes
is essential for the development of lead candidates in drug discovery.
Herein, we present a novel Rh(III)-catalyzed reaction pathway for
synthesizing substituted cyclobutanes, which involves a concerted
N–C bond formation and C–C bond cleavage between 2-aryl
quinazolinones and alkylidenecyclopropanes. Notably, the combination
of Rh(III) catalyst and HFIP solvent plays a critical role in facilitating
the formation of cyclobutane rings.