Synthetic organic reactions are a fundamental enabler of allmolecule
drug discovery, and the vast majority of medicinal chemists
are initially trained—either at universities or within industry—as
synthetic organic chemists. The sheer breadth of synthetic methodology
available to the medicinal chemist represents an almost endless
source of innovation. But what reactions do medicinal chemists use in
drug discovery? And what criteria do they use in selecting synthetic
methodology?Why are arrays (all focused libraries) so powerful in
the lead-optimization process? In this Minireview, we suggest some
answers to these questions and also describe how we have tried to
expand the number of robust reactions available to the medicinal
chemist.
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