Category Archives: Synthesis

Synthesis: Sulfonylated Pyridines


Sulfonyl pyridines have utility both as constituents of bioactive molecules and as synthetic intermediates.  Typical methods for their preparation have suffered from the use of odiferous thiols, capricious oxidation steps, poor atom economy, and production of significant amounts of hazardous … Continue reading

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Synthesis: Copper-mediated trifluoromethylation


The introduction of fluorine in the course of a lead optimisation programme has become a key tool in the medicinal chemist’s armoury and many drug candidates incorporate one or more fluorine atoms.  Two reviews published in 2008 in J.Med.Chem. and … Continue reading

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Aromatic chloride to nitrile transformation


Introducing a nitrile in the place of less polar substituents is a fairly common approach to reducing lipophilicity in a lead molecule but in this review from the MedChem group at Pfizer the associated benefits of specifically the aromatic chloride to … Continue reading

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