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Combinatorial chemistry
The basic principles
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What is it about?
• Synthesising a large number of similar compounds in a short period of time.
• Compounds that are generated are analogues of compounds that are already biologically active
• Chemists want to find a new medicine that is more effective than an existing one, or causes fewer side effects
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A simple model
1. Take some beads made from a polymer
2. React the beads with a group called a linker
3. Mix the bead in with an alcohol that you want to use in a chemical reaction. The linker will bind to it and hold it on the bead.
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A simple model
4. Have 6 reaction vessels each containing a different acyl chloride. Put a 1/6 of your beads into a mesh bag and put into a container.
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A simple model
5. Esterification occurs forming 6 different esters.
6. The beads are removed from the vessel by lifting up the mesh bag. They are washed to remove any unreacted acyl chloride
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A simple model7. A reaction is used to break the linker
group down.
8. The polymer beads are reused
9. You have made 6 different esters which can now be tested for biological activity
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A simple model10. How many esters would you have made
if you had attached 6 different alcohols to the beads?
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A simple model
Large numbers of similar compounds have been synthesised in a very short period
of time. Imagine how much longer it would take if you did the reaction with one alcohol
and acyl chloride, and then did it again with a different acyl chloride, and then again,
and again…. 36 times!