C7-Friedel–Crafts alkylation of 4-aminoindoles with para-quinone methide derivatives under catalyst-free conditions

Abstract

The first example of Friedel–Crafts alkylation of indoles with para-quinone methide derivatives at the C7 position was developed by using 4-alkylaminoindoles as nucleophiles under catalyst-free conditions. It is a mild and efficient protocol to access 7-indolyl-containing triarylmethane derivatives. This methodology features advantages including broad scope, operational simplicity, and the potential utility for the synthesis of biologically active compounds.

Graphical Abstract

Keyword:

• Catalyst-free
• Friedel–Crafts alkylation
• indole
• para-quinone methides
• triarylmethane

Additional information

Funding

We thank the National Natural Science Foundation of China [Grant 21772199 and 21971264] for financial support of this program.