Transcript Combinatorial chemistry

Combinatorial chemistry
The basic principles
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
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.
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.
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
A simple model
7. 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
A simple model
10. How many esters would you have made
if you had attached 6 different alcohols
to the beads?
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!