Standard chemistry prescribes the conversion of one or two compounds i
nto their products. In contrast, Eintopf (one-pot) multicomponent reac
tions (MCRs) involve at least three different compounds. One-pot MCRs
are a useful tool in combinatorial chemistry: From a mixture of educts
a large number of products can be simultaneously formed in liquid pha
se, called a soluble molecular library. The member compounds of such l
ibraries are investigated simultaneously for desired properties, e.g.
antibiotic activity. The main constraint is, that the underlying chemi
stry must not produce unknown side reactions and must lead to a broad
spectrum of stable products with high yields. Isocyanide multicomponen
t chemistry allows the generation of soluble libraries of very differe
nt sizes, which are easy to screen for biological or pharmaceutical ef
ficacy using the algorithms presented. Products can easily be enumerat
ed and the kinetics of the isocyanide chemistry is simple to investiga
te. Combinatorial chemistry is capable of generating and optimizing le
ads faster and with fewer resources than by conventional means. Combin
atorial chemistry based on isocyanide chemistry is by far the most imp
ortant and most impressive technique in use today to reducing time and
costs associated with lead generation and optimization during the dru
g discovery process. The simplicity of the reaction conditions involve
d means that the generation and screening of libraries can be automate
d.