Interfacing Microwave Synthesis with Enabling Technologies in Drug Discovery
Poster Mar 30, 2006
Doris Dallinger and C. Oliver Kappe
IntroductionModern drug discovery steadily relies on high-speed organic synthesis and combinatorial chemistry techniques for the rapid generation of compound libraries. Microwave-assisted organic synthesis in combination with polymer-assisted solution phase (PASP) methods are powerful techniques that are frequently applied in both academia and industry.
Here we report on the rapid synthesis/decoration of privileged heterocyclic scaffolds, namely the dihydropyrimidine (DHPM) scaffold, by applying microwave heating in conjunction with PASP approaches. The use of resin-bound catalysts, reagents and scavengers as well as fluorous reagents in conjunction with microwave heating will be described for amidations, esterifications via a Mitsunobu protocol and N-acylations.
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
Predicting Regioselectivityand Lability of Cytochrome P450 Metabolism using Quantum Mechanical SimulationsPoster
Predicting Regioselectivity and Lability of Cytochrome P450 Metabolism using Quantum Mechanical SimulationsREAD MORE
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