Rhodium(III)-Catalyzed Regioselective Direct C-2 Alkenylation of Indoles Assisted by the Removable N-(2-Pyrimidyl) Group

摘要: The C-2-alkenylindole unit is a key component of numerous natural products and pharmacophores. However, the intermolecular direct construction core structural motif remains challenging in organic synthesis. Here we report new, efficient, versatile methodology for synthesis C-2-alkenylindoles through rhodium(III)-catalyzed CH functionalization indoles with acrylates under air by employing metal-directing group strategy. This strategy gives rare selectivity alkenylation N-(2-pyrimidyl)indoles at C-2 position provides functionalized C-2- alkenylindoles mild conditions broad substrate tolerance. An expansion has also been demonstrated to, example, pyrrole facile deprotection pyrimidyl group. All results suggest that this could be served as highly attractive alternative biologically important C-2-alkenylindoles.