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个人信息Personal Information
教授
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
An Organocatalytic Asymmetric Friedel-Crafts Addition/Fluorination Sequence: Construction of Oxindole-Pyrazolone Conjugates Bearing Vicinal Tetrasubstituted Stereocenters
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论文类型：期刊论文
发表时间：2015-11-06
发表刊物：ORGANIC LETTERS
收录刊物：SCIE、PubMed、Scopus
卷号：17
期号：21
页面范围：5168-5171
ISSN号：1523-7060
摘要：A highly efficient and practical one-pot sequential process, consisting of an organocatalytic enantioselective Friedel-Crafts-type addition of 4-nonsubstituted pyrazolones to isatin-derived N-Boc ketimines and a subsequent diastereoselective fluorination of the pyrazolone moiety, is developed. This reaction sequence delivers novel oxindole pyrazolone adducts featuring vicinal tetrasubstituted stereocenters with a 0.5 mol % catalyst loading in high yield with excellent enantio- and diastereocontrol. Notably, chloro, bromo, and thioether functionalities can be readily incorporated, rendering a broad diversity of the product.
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