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Asymmetric Three‐Component Heck Arylation/Amination of Nonconjugated Cyclodienes
Author(s) -
Zhu Daoyong,
Jiao Zhiwei,
Chi Yonggui Robin,
Gonçalves Théo P.,
Huang KuoWei,
Zhou Jianrong Steve
Publication year - 2020
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.201915864
Subject(s) - indoline , amination , chemistry , stereoselectivity , component (thermodynamics) , aryl , organic chemistry , combinatorial chemistry , catalysis , alkyl , physics , thermodynamics
Substituted cyclohexylamines are becoming increasingly important in drug discovery. Asymmetric Heck insertion/amination of nonconjugated cyclodienes proceeds to give 5‐aryl cyclohexenylamines with good enantioselectivity and exclusive trans configurations. Primary and secondary anilines, indoline, and benzylamines are suitable amines. The weakly donating diphosphite Kelliphite forms a deep unsymmetrical pocket, which is essential for stereoselective anti attack of amines.