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Asymmetric Three-Component Heck Arylation/Amination of Nonconjugated Cyclodienes.

Daoyong ZhuZhiwei JiaoYonggui Robin ChiThéo P GonçalvesKuo-Wei HuangJianrong Steve Zhou
Published in: Angewandte Chemie (International ed. in English) (2020)
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.
Keyphrases
  • drug discovery
  • solid state
  • molecular docking