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Enantioselective [3 + 2] annulation of 4-isothiocyanato pyrazolones and alkynyl ketones under organocatalysis

Wenyao Wang, Shiqiang Wei, Xiaoze Bao, Shah Nawaz, Jingping Qü, Baomin Wang

2021Organic & Biomolecular Chemistry19 citationsDOI

Abstract

An asymmetric [3 + 2] annulation reaction of 4-isothiocyanato pyrazolones with alkynyl ketones in the presence of an organic catalyst derived from a cinchona alkaloid under mild conditions is realized. This protocol provides unprecedented expeditious access to a wide range of optically active spiro[pyrroline-pyrazolones] with various electronic properties in high yields with good to excellent enantioselectivities.

Topics & Concepts

PyrazolonesAnnulationEnantioselective synthesisOrganocatalysisChemistryCatalysisOrganic chemistryStereochemistryCatalytic C–H Functionalization MethodsSulfur-Based Synthesis TechniquesSynthesis and Catalytic Reactions
Enantioselective [3 + 2] annulation of 4-isothiocyanato pyrazolones and alkynyl ketones under organocatalysis | Litcius