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Combinatorial Chemistry on Solid Supports (Paperback, Softcover reprint of hardcover 1st ed. 2007)
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Combinatorial Chemistry on Solid Supports (Paperback, Softcover reprint of hardcover 1st ed. 2007)
Series: Topics in Current Chemistry, 278
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Themodernbillion-dollardrug-discoveryprocessstronglyreliesonbothhi-
throughput synthesis and screening methods. Whereas the latter is
based on molecular biological methods, the ef?cient and reliable
generation of c- pound collections often makes use of combinatorial
chemistry. Discovered in the 1980s, this methodology was explored
extensively in the 1990s by groups in academia and in industry.
Without any doubt, combinatorial chemistry changed the whole
drug-discovery process and found many applications in cropscience
and the material sciences. However, since its implementation,
solution- and solid-phase techniques have been competing with each
other, and although many companies started
theircombinatorialchemistryprogramwithsolid-phasetechniques,
soluti- phase combinatorial methods have taken over and now account
for appro- mately 25% of all combinatorial efforts. The syntheses
of complex, non-polymeric structures, discovered in the 1960s by
the late Bruce Merri?eld, was largely ignored in the context of
solid supports, mainly due to the fact that appropriate synthesis
techniques were not available. Since solid-phase chemical
methodology strongly differs from traditional solution-phase
chemistry, two chapters deal with this topic. The Brase group
(Jung, Wiehn, Brase) gives an overview of multifunctional linkers,
which can beusedforthegenerationofdiversity-orientedcollections,
simplybycleavage fromresins. Still in its infancy, solid-phase
reactions employ "simple" amide chemistry in most cases due to
their high-yielding, reliable protocols. Ljungdahl, Br- ?eld, and
Kann address solid-phase organometallic chemistry, which is now one
ofthe great challenges in reliable solid-phase organicsynthesis."
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