Chemical libraries, polymer-supported

The advent of combinatorial techniques and solid phase organic synthesis may lead to preparation of large numbers of structurally related molecules in short periods of time. This is important especially for the optimization of lead structures in the pharmaceutical industry [40]. It is now well established and documented that the combinatorial technology and solid phase techniques could offer sufficient latitude for preparation of corresponding chemical libraries with broad structural diversity. The diverse potentiality of (3-lactam moiety as specific pharmacophores and scaffolds has attracted ample interests from pharmaceutical industries for the synthetic methods based on polymer-supported techniques. 

After extending the use of polymer supports into the realm of organic synthesis, the access to small molecule libraries has been accelerated due to the availability of carrying out suitable chemical reactions with the aid of automated synthesis equipment.2,3... 

Salvino JM, Kumar NV, Orton E, Airey J, Kiesow T, Crawford K., Mathew R, KroUkowski P, Drew M, Engers D, Kro-likowski D, Herpin T, Gardyan M, McGeehan G, Labaudiniere R. Polymer-supported tetrafluorophenol a new activated resin for chemical library synthesis. J. Comb. Chem. 2000 2 691-697. Baxendale IR, Ley SV. Polymer-supported reagents for multi-step organic synthesis appUcation to the synthesis of sildenafil. Bioorg. Med. Chem. Lett. 2000 10 1983-1986. 

Rare earth metal triflates are recognized as a very efficient Lewis acid catalysts of several reactions including the aldol reaction, the Michael reaction, allylation, the Diels-Alder reaction, the Friedel-Crafts reaction, and glycosylation [110]. A polymer-sup-ported scandium catalyst has been developed and used for quinoline library synthesis (Sch. 8) [111], because lanthanide triflates were known to be effective in the synthesis of quinolines from A-arylimines [112,113]. This catalyst (103) was readily prepared from poly(acrylonitrile) 100 by chemical modification. A variety of combinations of aldehydes, amines, and olefins are possible in this reaction. Use of the polymer-supported catalyst has several advantages in quinoline library construction. 

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