1242061-60-4Relevant articles and documents
Efficient and general synthesis of 3-aminoindolines and 3-aminoindoles via copper-catalyzed three-component coupling reaction
Chernyak, Dmitri,Chernyak, Natalia,Gevorgyan, Vladimir
supporting information; experimental part, p. 961 - 966 (2010/07/13)
An efficient three-component coupling (TCC) reaction toward a variety of 3-aminoindoline and 3-aminoindole derivatives has been developed. This cascade transformation proceeds via the copper-catalyzed coupling reaction between 2-aminobenzaldehyde, a secondary amine, and an alkyne leading to a propargylamine intermediate which, under the reaction conditions, undergoes cyclization into the indoline core. The latter, upon treatment with a base, smoothly isomerizes into the indole. Alternatively, the indole can directly be synthesized in a one-pot sequential reaction.