Journal
DRUG DISCOVERY TODAY
Volume 13, Issue 15-16, Pages 677-684Publisher
ELSEVIER SCI LTD
DOI: 10.1016/j.drudis.2008.03.007
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In the scenario of a continuous request for better drugs in shorter times, medicinal chemists must face the challenging task of preparing new patentable molecules, combining high activity and selectivity, drug-likeness and good pharmacokinetic properties. Multiparametric optimization requires a substantial improvement of the efficacy and throughput of the early discovery process, leading to a significant revolution in organic synthesis and chemistry technologies. Chemists are searching for ways to simplify synthetic protocols, for example, by the use of polymer-assisted solution-phase synthesis, microwave-assisted organic synthesis and flow chemistry. Organic synthesis is benefiting of fast and robust reactions, with breakthrough approaches often entailing the privileged use of multicomponent reactions, click chemistry and ring-closing metathesis.
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