Generation of novel, potent urotensin-II receptor antagonists by alkylation-cyclization of isoindolinone C3-carbanions

We report a facile alkylation-cyclization reaction involving the isoindolinone C3 position, which resulted in tricyclic derivatives 2 and 10 in 48% and 32% yields, respectively. These novel compounds possess potent urotensin-II receptor antagonist activity.