Recent progress in the synthesis and characterization of well-defined conjugated polymers and oligomers is presented. The different synthetic schemes for most of the important conjugated polymers will be discussed using a subdivision into three main sections, covering hydrocarbon polymers, heterocyclic polymers and the oligomers, respectively. Although the materials properties will be referred to, the main emphasis of the review is directed to the different strategies that are now available to produce conjugated polymers and welldefined oligomers in a reproducible way and with full control over most of the important macromolecular properties.
BackgroundPraziquantel remains the drug of choice for the worldwide treatment and control of schistosomiasis. The drug is synthesized and administered as a racemate. Use of the pure active enantiomer would be desirable since the inactive enantiomer is associated with side effects and is responsible for the extremely bitter taste of the pill.Methodology/Principal FindingsWe have identified two resolution approaches toward the production of praziquantel as a single enantiomer. One approach starts with commercially available praziquantel and involves a hydrolysis to an intermediate amine, which is resolved with a derivative of tartaric acid. This method was discovered through an open collaboration on the internet. The second method, identified by a contract research organisation, employs a different intermediate that may be resolved with tartaric acid itself.Conclusions/SignificanceBoth resolution procedures identified show promise for the large-scale, economically viable production of praziquantel as a single enantiomer for a low price. Additionally, they may be employed by laboratories for the production of smaller amounts of enantiopure drug for research purposes that should be useful in, for example, elucidation of the drug's mechanism of action.
Dutch Resolution is the term given to the use of mixtures (families) of resolving agents in classical resolutions. In this status report an overview is given of the latest results and new (possible) families of resolving agents are introduced. The concept of families is discussed as well as the factors that come into play on use of families. Practical aspects of Dutch Resolution in particular and resolutions in general are discussed.
High-throughput screening (HTS) represents a major cornerstone of drug discovery. The availability of an innovative, relevant and high-quality compound collection to be screened often dictates the final fate of a drug discovery campaign. Given that the chemical space to be sampled in research programs is practically infinite and sparsely populated, significant efforts and resources need to be invested in the generation and maintenance of a competitive compound collection. The European Lead Factory (ELF) project is addressing this challenge by leveraging the diverse experience and know-how of academic groups and small and medium enterprises (SMEs) engaged in synthetic and/or medicinal chemistry. Here, we describe the novelty, diversity, structural complexity, physicochemical characteristics and overall attractiveness of this first batch of ELF compounds for HTS purposes.
Schwarze Schafe in der Familie? Für einen kombinatorischen Prozess zur Racematspaltung über die Trennung diastereomerer Salze mithilfe von Gemischen („Familien“) strukturell verwandter Reagentien (Beispiele sind gezeigt) wurde der Begriff „Dutch Resolution“ geprägt. Einige Familienmitglieder werden nicht in die Salze eingebaut; offensichtlich verhindern sie die Keimbildung. Daraus ergibt sich eine vereinfachte Zwei‐Komponenten‐Methode mit hohen Erfolgsquoten schon zu Beginn des (iterativen) Prozesses.
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