6533b856fe1ef96bd12b2f1a

RESEARCH PRODUCT

ChemInform Abstract: Organocatalytic Enantioselective Synthesis of Pyrazoles Bearing a Quaternary Stereocenter.

Fares Ibrahim AmrM. Carmen MuñozGonzalo BlayCarlos VilaJosé R. Pedro

subject

chemistry.chemical_compoundBearing (mechanical)ThioureaChemistrylawEnantioselective synthesisPyrazolonesGeneral MedicineCombinatorial chemistryCatalysislaw.inventionStereocenter

description

An efficient one-pot asymmetric synthesis of pyrazoles bearing a chiral quaternary stereocenter has been developed. Quinine-derived thiourea catalyzed the enantioselective addition of pyrazolones to isatin-derived ketimines, providing the corresponding acetylated pyrazoles after in situ treatment with Ac2 O/Et3 N. The corresponding pyrazoles were afforded in high yields and excellent enantioselectivities.

https://doi.org/10.1002/chin.201640135