Efficient Synthesis of Polysubstituted Pyrroles Based on [3+2] Cycloaddition Strategy Utilizing [1,2]‐Phospha‐Brook Rearrangement under Brønsted Base Catalysis

摘要: An efficient method for the synthesis of polysubstituted pyrroles was established based on [3+2] cycloaddition strategy utilizing [1,2]-phospha-Brook rearrangement under Bronsted base catalysis. The less-explored approach cycloaddition, that is, reaction a C3 subunit with imines, successfully achieved by making use newly designed subunits containing requisite umpolung. two-step formal involves catalytic generation an α-oxygenated propargyl anion through followed γ-addition to imine catalysis and subsequent intramolecular cyclization mediated Au catalyst or halogenation reagent afford having variety substituents in positional selective manner. thus synthesized were amenable further transformations, such as palladium-catalyzed cross-coupling reactions. operationally very simple readily available substrates provides new access diverse array well-organized pyrroles.