Asymmetric Three-Component Heck Arylation/Amination Of Nonconjugated Cyclodienes
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION(2020)
摘要
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.
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关键词
allylic amination,phosphites,Heck reaction,palladium,metal migration
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