Tag Archives: fluorine

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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Discovery of PF-232798 (CCR5 Antagonist)


CCR5 antagonists prevent entry of HIV into host cells by binding to the CCR5 co-receptor and stopping the gp120-CD4 complex from making the crucial interaction with CCR5 that leads to fusion of the viral and host cell membranes (see Wikipedia article … Continue reading

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Improved PK profile through fluorine and deuterium incorporation


Compound (1) was identified by scientists at Merck as a potent Aurora kinase inhibitor with the potential to be useful in the treatment of various cancers.  In this paper the authors reveal that the basic amine which is key to good … Continue reading

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