| Title : Asymmetric Construction of a Multi-Pharmacophore-Containing Dispirotriheterocyclic Scaffold and Identification of a Human Carboxylesterase 1 Inhibitor - Bao_2018_Org.Lett_20_3394 |
| Author(s) : Bao X , Wei S , Qian X , Qu J , Wang B , Zou L , Ge G |
| Ref : Org Lett , 20 :3394 , 2018 |
|
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. |
| PubMedSearch : Bao_2018_Org.Lett_20_3394 |
| PubMedID: 29786435 |
Bao X, Wei S, Qian X, Qu J, Wang B, Zou L, Ge G (2018)
Asymmetric Construction of a Multi-Pharmacophore-Containing Dispirotriheterocyclic Scaffold and Identification of a Human Carboxylesterase 1 Inhibitor
Org Lett
20 :3394
Bao X, Wei S, Qian X, Qu J, Wang B, Zou L, Ge G (2018)
Org Lett
20 :3394