A1 Refereed original research article in a scientific journal
Asymmetric Synthesis of Five-Membered Spiropyrazolones via N-Heterocyclic Carbene (NHC)-Catalyzed [3+2] Annulations
Authors: Li S, Wang L, Chauhan P, Peuronen A, Rissanen K, Enders D
Publisher: GEORG THIEME VERLAG KG
Publication year: 2017
Journal: Synthesis: stuttgart
Journal name in source: SYNTHESIS-STUTTGART
Journal acronym: SYNTHESIS-STUTTGART
Volume: 49
Issue: 8
First page : 1808
Last page: 1815
Number of pages: 8
ISSN: 0039-7881
DOI: https://doi.org/10.1055/s-0036-1588381
Abstract
A new synthetic strategy for the asymmetric synthesis of five-membered spiropyrazolones via N-heterocyclic carbene-catalyzed [3+2] annulations employing enals and unsaturated pyrazolones as substrates has been developed. The new protocol allows the flexible variation of all four substituents of the pharmaceutically important spiropyrazolones in moderate to very good yields and in most cases with excellent diastereoselectivities and good to excellent enantioselectivities.
A new synthetic strategy for the asymmetric synthesis of five-membered spiropyrazolones via N-heterocyclic carbene-catalyzed [3+2] annulations employing enals and unsaturated pyrazolones as substrates has been developed. The new protocol allows the flexible variation of all four substituents of the pharmaceutically important spiropyrazolones in moderate to very good yields and in most cases with excellent diastereoselectivities and good to excellent enantioselectivities.