INDOLE-PYRIDO[2,3-d]PYRIMIDINE HYBRIDS: THREE-COMPONENT SYNTHESIS AND BINDING STUDIES AGAINST DOPAMINERGIC RECEPTORS

MANUEL NOGUERAS; JUSTO COBO; DIDIER VARGAS; JORGE TRILLERAS; MARÍA DE LOS ANGELES ÁLVAREZ; ANDUJAR SEBASTIAN; RICARDO D. ENRIZ; DIEGO CORTÉS

Congreso; 19th European Symposium on Organic Chemistr; 2015

Pteridine is the heterocyclic core presents in important biological metabolites such folic acid or pterin;deazapteridine analogs, such pyrido[2,3-d]pyrimidine compounds exhibit relevant enzymatic activityalong with for example antiproliferative propierties, such as dihydrofolate reductase (DHFR) inhibition, [1]being used e.g. in the treatment of cancer.[2,3] We are here reporting the MCR?s between corresponding4-aminopyrimidine 1a or 1b, 3-(1H-indol-3-yl)-3-oxopropanenitrile 2 and aromatic aldehydes 3, both atclassical reflux in acetic acid and under free-solvent MWI-assisted with InCl3 as a catalyst, to afford thehybrids 4 and 5, with better results for these last environmentally friendlier conditions.