王保民

个人信息Personal Information

教授

博士生导师

硕士生导师

性别:男

毕业院校:兰州大学

学位:博士

所在单位:化工学院

学科:有机化学. 药物化学. 精细化工

办公地点:西部校区化工实验楼G-413

联系方式:0411-84986190 15942819406

电子邮箱:bmwang@dlut.edu.cn

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Asymmetric Construction of a Multi-Pharmacophore-Containing Dispirotriheterocyclic Scaffold and Identification of a Human Carboxylesterase 1 Inhibitor.

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论文类型:期刊论文

发表时间:2018-01-01

发表刊物:Organic letters

收录刊物:PubMed、SCIE

卷号:20

期号:11

页面范围:3394-3398

ISSN号:1523-7052

摘要: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.