133931-21-2Relevant articles and documents
Synthesis of polysubstituted indoles and indolines by means of zirconocene-stabilized benzyne complexes
Tidwell, Jeffrey H.,Buchwald, Stephen L.
, p. 11797 - 11810 (2007/10/02)
The development of a new method for the regiospecific synthesis of polysubstituted indoles and indolines is reported. The key steps involve the generation of zirconocene-stabilized benzyne complexes and subsequent intramolecular olefin insertion reactions to provide tricyclic indoline zirconacycles. The zirconacyclic intermediates were cleaved with iodine to yield diiodo indolines, which were converted to a wide variety of indole and indoline products, such as analogs of tryptamine, serotonin, tryptophan, and the pharmacophore of CC-1065.