Relay Cu(I)/Brønsted Base Catalysis for Phospha‐Michael Addition/5‐exo‐dig Cyclization/Isomerization of in situ Formed aza‐Alkynyl o‐quinone methides with P(O)−H compounds to C3‐Phosphorylated Indoles

Abstract A relay Cu(I)/Brønsted base catalyzed one‐pot phospha ‐Michael addition/5‐ exo ‐ dig cyclization/isomerization of in situ generated aza ‐alkynyl o ‐quinone methides ( N ‐ o ‐AQMs) from 1‐( o ‐aminophenyl)prop‐2‐ynols with P(O)‐compounds has been established to afford C3‐phosphorylated indoles. It demonstrates that the 1,4‐conjugate addition adduct from N ‐ o ‐AQMs could undergo further cyclization with the tethered alkyne moiety to afford N ‐heterocyclic compounds. magnified image