Automation in medicinal chemistry is often seen simply as a part of the com
binatorial chemistry technologies used to meet the need for large, diverse
screening collections for lead generation. However, the application of auto
mation to the lead optimization phase of drug discovery offers the prospect
of reduced cycle times via increased efficiency in target compound prepara
tion. The realization of this goal requires the integration of efficient pr
ocesses with equipment capable of delivering quality compounds and, of cour
se, the skilled medicinal chemists.