37385-04-9Relevant academic research and scientific papers
C7-Functionalization of Indoles via Organocatalytic Enantioselective Friedel-Crafts Alkylation of 4-Amino- indoles with 2-Butene-1,4-diones and 3-Aroylacrylates
Huang, Tongkun,Zhao, Yunlong,Meng, Shanshui,Chan, Albert S. C.,Zhao, Junling
, p. 3632 - 3638 (2019)
An efficient protocol for the enantioselective C7 Friedel-Crafts alkylation between 4-aminoindoles and 2-butene-1,4-diones or 3-aroylacrylates was reported. This process was catalyzed by a chiral phosphoric acid, affording the corresponding 1,4-disubstituted indoles in moderate to high yields with good to high enantioselectivities. This reaction could be performed on a gram scale without loss of efficiency, and a representative derivatization of the products was also investigated to prepare the corresponding C3 formylation compound. (Figure presented.).
