A methodology for the synthesis of highly functionalized 2- and 4-aminoquinoline derivatives

Abstract: A methodology for the synthesis of 2- and 4-aminoquinoline derivatives, which takes advantage of selective activation of 2- or 4-substituent of 2-methylsulfanyl-3-acyl-1H-quinolin-4-one 1, has been developed. Since a procedure for formation of 3-aminoquinolinones from the 4-quinolinone 1 was described previously, the new methodology comprises a general methodology for the selective syntheses of three isomeric 2-, 3- and 4-aminoquinoline derivatives starting with the common 4-quinolinone 1. [Copyright &y& Elsevier]