Asymmetric Construction of Bispiro-Cyclopropane-Pyrazolones via a [2+1] Cyclization Reaction by Dipeptide-Based Phosphonium Salt Catalysis

Article abstract of DOI:10.1002/adsc.202000073

We reported herein an efficient alternative for asymmetric synthesis of structurally complicated chiral bispiro-cyclopropane-pyrazolones via dipeptide-based phosphonium salt catalyzed [2+1] cyclization of 2,3-dioxopyrrolidines and halogenated pyrazolones. With this catalytic asymmetric protocol, a broad range of bispiro heterocyclic compounds bearing a pyrazolone unit were prepared in high yields with excellent diastereo- and enatioselectivities. Of note, this transformation proceeds in a really short time under mild reaction conditions. (Figure presented.).