Nitrogen-containing heterocyclic compounds form the basis of many drugs due to their useful physiological and pharmacological properties, including the ability to easily form hydrogen bonds with biological targets; currently, 75% of all FDA-approved drugs fall into this category.
A quinoline or isoquinoline moiety is a key building block for many of these drugs, due to its ability to inhibit cell growth. Functionalised quinolinium and isoquinolinium salt moieties are key to the function of many treatments for conditions such as cancer, HIV, malaria, and diabetes.
In a recent study at Diamond, we see scientists from AstraZeneca study a novel method for the reductive functionalisation of quinolinium and isoquinolinium salts using an extended range of electrophiles. The mild reaction conditions include the use of a low-loaded rhodium catalyst and an inexpensive formic acid as the terminal reductant. The team used in situ small molecule single crystal diffraction to identify the species formed.
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