期刊
BEILSTEIN JOURNAL OF ORGANIC CHEMISTRY
卷 16, 期 -, 页码 638-644出版社
BEILSTEIN-INSTITUT
DOI: 10.3762/bjoc.16.60
关键词
aziridines; chiral disulfonimides; difluoromethyl compounds; fluorinated diazo reagents; strong Bronsted acids
资金
- National Key Research and Development Program of China [2019YFA0905100]
- National Natural Science Foundation of China [21772142, 21901181, 21961142015]
- Tianjin Municipal Science & Technology Commission [19JCQNJC04700]
A diastereo- and enantioselective approach to access chiral CF2-functionalized aziridines from difluorodiazoethyl phenyl sulfone (PhSO2CF2CHN2) and in situ-formed aldimines is described. This multicomponent reaction is enabled by a combined strong Bronsted acid catalytic platform consisting of a chiral disulfonimide and 2-carboxyphenylboronic acid. The optical purity of the obtained CF2-substituted aziridines could be further improved by a practical dissolution-filtration procedure.
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