Synthesis of biologically potent new 3-(heteroaryl)aminocoumarin derivatives via Buchwald-Hartwig C-N coupling

New 3-(heteroaryl)aminocoumarin derivatives were synthesized from 3-aminocoumarin, applying optimized Buchwald-Hartwig amination conditions using Palladium acetate, Cesium carbonate, and BINAP in 1,4-dioxane employing elevated temperature conditions and under an argon atmosphere. The target heteroarylaminocoumarin derivatives were obtained in moderate to good yields ranging from 56% to 98%. The procedure described Could be widely employed for the preparation of new heterocyclic compounds when one of the core moieties is coumarin and has the potential to be active drug candidates. (C) 2009 Elsevier Ltd. All rights reserved.