Synthesis of a Small Library of Imidazolidin-2-ones using Gold Catalysis on Solid Phase

AGUSTINA LA VENIA; NOELIA MEDRAN; VIKTOR KRCHNAK; SEBASTIAN A. TESTERO

ACS Combinatorial Science

AMER CHEM SOCIETY

Año: 2016 vol. 18 p. 482 - 489

An efficient andhigh-yielding solid phase synthesis of a small library of imidazolidin-2-onesand imidazol-2-ones was carried outemploying a high chemo- and regio-selectivegold-catalyzed cycloisomerization as a key step. Polymer-supported amino acidsderivatized with several alkynesfunctionalities combined with tosyl- andphenyl-ureas have been subjected to gold-catalysis exhibiting exclusively C-Nbond formation. The present work proves thepotential of solidphase synthesis and homogeneous gold catalysis as anefficient and powerfulsynthetic tool for the generation of drug-like heterocycles.