Summary
Summary Drug synthesis and retro synthesis
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Drug design and mechanisms of drug action - 1st semester Includes bullet points, key diagrams and images
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Drug Synthesis and Retro-synthesisSynthesis Order
Lead discovery:
Synthesis of diverse structures in high-throughput-screening
Large number of compounds (10,000)
Emphasis on speed not yield
Lead optimisation:
Find hits from lead discovery
Synthesis of related analogues
Smaller number of compounds (1000)
Process chemistry:
Synthesis of promising compounds
Small number of compound but large scale (10)
Product manufacture:
Synthesis of approved drug for trials
Singular compound but large scale
Production under GMP
Scaffolds and Skeletons of Drug Molecules
Key central scaffold which functional groups are attached to
Useful when synthesising
Linear- alkane, alkene and alkyne
Cyclic- carbocyclic, heterocyclic, aromatic and herteroaromatic
Ionisable- amine, guanidine and carboxylic acid
Polar- alcohol, phenol, sulphonamide, ether, thioether and halogen
Carbonyl- ketone, ester, urea, amide and carbamate
Drug Synthesis
Starting material (SM) should be cheap and easily available
Sequence of steps changes SM into target molecule (TM)
Synthesis- a series of reactions that leads forward from an SM to the TM
Retro-synthesis- mental process for planning a synthesis by moving backwards
from the TM and simplify back to a SM
Retro-Synthesis Terminology
Starting material (SM)
Target material (TM)
Types of reactions:
Functional group inter-conversion (FGI)
Functional group addition (FGA)
Functional group removal (FGR)
Disconnection- break a bond to form a precursor
Synthon- ideal fragment produced by disconnection
Synthetic equivalent- reagent or compound that corresponds to a synthon
Disconnection
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