Asymmetric Construction of a Multi-Pharmacophore-Containing Dispirotriheterocyclic Scaffold and Identification of a Human Carboxylesterase 1 Inhibitor.
Release Time:2019-03-12 Hits:
Indexed by: Journal Article
Date of Publication: 2018-01-01
Journal: Organic letters
Included Journals: SCIE、PubMed
Volume: 20
Issue: 11
Page Number: 3394-3398
ISSN: 1523-7052
Abstract: A catalytic asymmetric [3 + 2] cyclization of novel 4-isothiocyanato pyrazolones and isatin-derived ketimines was developed, delivering a wide range of intriguing dispirotriheterocyclic products in high yield with excellent diastereoselectivity and enantioselectivity. A chiral sulfoxide derivative of this dispirocyclic product was identified to be a promising hit of the human carboxylesterase 1 inhibitor, and the significant difference of the activity between two enantiomers emphasized the importance of this asymmetric process.
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