Traceless Solid Phase Synthesis of Bicyclic Dihydropyrimidone Libraries Using Microwave-Assisted Cyclization Cleavage
Poster Jul 25, 2006
Rolando Pérez, Doris Dallinger and C. Oliver Kappe
4-Aryl-3,4-dihydro-2(1H)-pyrimidone esters ("Biginelli compounds", DHPMs) represent a heterocyclic system of remarkable pharmacological efficiency. More recently, appropriately functionalized DHPMs have emerged as potent calcium channel blockers, antihypertensive agents, a1a -adrenergic antagonists, mitotic kinesin Eg5 inhibitors and neuropeptide Y (NPY) antagonists. In recent years several different pathways for the synthesis of DHPMs have been reported, including combinatorial approaches, using e.g. solid phase reaction conditions. We now report a variation of the Biginelli condensation using methyl 4-chloroacetoacetate as the building block both in solution and in solid phase. This modification allows the rapid entry into a variety of bicyclic heterocyclic ring scaffolds.
The Pathogen Box: A Catalyst for Neglected Disease Drug DiscoveryPoster
Modelled after the Malaria Box, the Pathogen Box contains ~400 diverse drug-like molecules active against neglected diseases of interest such as Chagas disease, cryptosporidiosis, hookworm, sleeping sickness, leishmaniasis, lymphatic filariasis, malaria, onchocerciasis, schistosomiasis, trichuriasis, tuberculosis.READ MORE
Selective Debenzylation of N-Benzyloxypyrazinones in FlowPoster
Selective and reproducible debenzylation of benzyloxypyrazinones by using catalytic transfer hydrogenation in flow chemistry to yield N-hydroxypyrazinones. The flow methodology enabled us to avoid overreduction of the compounds to pyrazin-2(1H)-ones.READ MORE