In both lead identification and lead optimization processes there is an acu
te need for new organic small molecules. Traditional methods of organic syn
thesis are orders of magnitude too slow to satisfy the demand for these com
pounds. The fields of combinatorial and automated medicinal chemistry have
been developed to meet the increasing requirement of new compounds for drug
discovery; within these fields, speed is of the essence. The efficiency of
microwave flash-heating chemistry in dramatically reducing reaction times
(reduced from days and hours to minutes and seconds) has recently been prov
en in several different fields of organic chemistry. We believe that the ti
me saved by using focused microwaves is potentially important in traditiona
l organic synthesis but could be of even greater importance in high-speed c
ombinatorial and medicinal chemistry.