A new route to the paullone scaffold was designed. The key step consisted in a free radical indole formation from an o-alkenyl arylisonitrile followed by Stille coupling with N-Boc-o-iodoaniline. After deprotection and closure of the seven-membered ring by lactamisation, parent or cyano-substituted paullones were obtained in moderate to good yields.
paullone - CDK inhibitor - tin - radical reaction - seven-membered lactam
