An Efficient Three-Component One-Pot Approach to the Synthesis of 2,3,4,5-Tetrahydro-1H-2-benzazepines by Means of Rhodium-Catalyzed Hydroaminomethylation
摘要:
We have developed a novel and efficient three-component one-pot, catalytic approach for the synthesis of 2,3,4,5-tetrahydro-1H-2-benzazepines, using a rhodium catalyst that does not require phosphine. The isolated yields are excellent and the protocol tolerates anilines of diverse basicity.
AbstractAn acid‐catalyzed aza‐Prins‐type endo cyclization of 2‐alkenylbenzaldehydes with BocNH2 or aniline derivatives through in situ generation of iminium intermediates has been developed, and various 1‐aminoindene derivatives were readily obtained. The first catalytic asymmetric variant of the present reaction has also been demonstrated.