期刊
CHEMISTRY-AN ASIAN JOURNAL
卷 11, 期 10, 页码 1532-1536出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/asia.201600325
关键词
asymmetric catalysis; isatin-derived ketimines; organocatalysis; pyrazoles; quaternary stereocenters
资金
- MINECO (Gobierno de Espana) [CTQ2013-47494-P]
- Generalitat Valenciana [ISIC2012/001]
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 Ac2O/Et3N. The corresponding pyrazoles were afforded in high yields and excellent enantioselectivities.
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