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Organocatalytic Enantioselective Synthesis of Pyrazoles Bearing a Quaternary Stereocenter
Author(s) -
Vila Carlos,
Amr Fares Ibrahim,
Blay Gonzalo,
Muñoz M. Carmen,
Pedro José R.
Publication year - 2016
Publication title -
chemistry – an asian journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.18
H-Index - 106
eISSN - 1861-471X
pISSN - 1861-4728
DOI - 10.1002/asia.201600325
Subject(s) - stereocenter , enantioselective synthesis , pyrazolones , thiourea , chemistry , isatin , stereochemistry , organic chemistry , catalysis
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 Ac 2 O/Et 3 N. The corresponding pyrazoles were afforded in high yields and excellent enantioselectivities.