MOLECULAR LIBRARIES IN LIQUID-PHASE VIA UGI-MCR

Citation
I. Ugi et al., MOLECULAR LIBRARIES IN LIQUID-PHASE VIA UGI-MCR, Research of chemical intermediates, 22(7), 1996, pp. 625-644
Citations number
28
Categorie Soggetti
Chemistry
ISSN journal
09226168
Volume
22
Issue
7
Year of publication
1996
Pages
625 - 644
Database
ISI
SICI code
0922-6168(1996)22:7<625:MLILVU>2.0.ZU;2-I
Abstract
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.