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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：日本东京大学
学位：博士
所在单位：化工学院
电子邮箱：qujp@dlut.edu.cn
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.
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