A Facile and Practical Synthesis of 9-Methyl-3-(1H-tetrazol-5-yl)-4H-pyrido(1,2-a)pyrimidin-4-one.

Substituted pyridopyrimidinones, 1: Convenient PTC alkylation and halogenation of 2‐hydroxy‐4H‐pyrido[1,2‐a]pyrimidin‐4‐one

“…The distinguished and unique chemical properties [2][3][4][5] and biological applications of 4H-pyrido [1,2-a]pyrimidin-4-one derivatives [6][7][8][9][10] Correspondence to: Mohamed Abass; e-mail: quinolinone@ yahoo.com. c 2007 Wiley Periodicals, Inc. evoked an interest for the continuation of the synthetic and chemical researches in this field.…”

CuI-catalyzed synthesis of multisubstituted pyrido[1,2-a]pyrimidin-4-ones through tandem Ullmann-type C–N cross-coupling and intramolecular amidation reaction

“…The nitrogen-containing bicyclic heterocycles have attracted considerable attention due to their wide applications in pharmaceuticals, agrochemicals and material sciences. 1–3 In particular, pyrido[1,2- a ]pyrimidine scaffolds have emerged as one of the most important N-fused bicyclic heterocycles for drug discovery and development, 4 and numerous pyrido[1,2- a ]pyrimidin-4-ones have exhibited a wide range of biological activities such as in antipsychotic agents, 5 tranquilizers, 6 antioxidants, 7 anticancer agents, 8 antiulcer agents, 9 antihypertensives, 10 antidepressants, 11 antiallergics, 12 antiplasmodial falcipain-2 inhibitors, 13 and spinal muscular atrophy (SMA) drugs. 14 Several pyrido[1,2- a ]pyrimidin-4-one derivatives, such as pirenperone, seganserin, lusaperidone, and risdiplam have been applied in clinical trials for decades ( Fig.…”

Palladium-Catalyzed Cyclocarbonylation of Pyridinylated Vinylogous Amides and Ureas to Generate Ring-Fused Pyridopyrimidinones

“…The pyridopyrimidinone core is a privileged scaffold with diverse pharmacological activity depending on its functionalization (Figure , red highlighting). For instance, the structural motif is exemplified by allergy drug Pemirolast , 1 , antidepressant Lusaperidone 2 , antihypertensive Seganserin 3 , antiviral compound 4 , antiulcer agent 5 , and antiproliferative probe 6 , just to name a few (Figure ). Consequently, we envisioned using this privileged template to design new frameworks for medicinal chemistry optimization, as pyrido­pyrimidi­none-embedded structures 7 and 8 have yet to be reported.…”