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Enantioselective Synthesis of 1,2‐Diarylaziridines by the Organocatalytic Reductive Amination of α‐Chloroketones
Author(s) -
Malkov Andrei V.,
Stončius Sigitas,
Kočovský Pavel
Publication year - 2007
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.200700165
Subject(s) - enantioselective synthesis , reductive amination , amination , formamide , computer science , reduction (mathematics) , simple (philosophy) , combinatorial chemistry , chemistry , mathematics , catalysis , organic chemistry , philosophy , geometry , epistemology
One‐sided triangles : A simple protocol has been developed for the synthesis of highly useful single enantiomers of 1,2‐diarylaziridines. The method involves conversion of the readily available α‐chloroacetophenones into the corresponding imines, followed by an enantioselective reduction with Cl 3 SiH catalyzed by the L ‐valine‐derived formamide L* and ring closure to give the desired aziridines (see scheme).