PAsp

An important breakthrough in that respect was the use of soHd-phase organic synthesis (SPOS) where the attachment of the substrate to an insoluble support allowed for easy workup (filtration) and for rapid generation of products via split-mix procedures [1,2]. An important subsequent development consisted of the immobihzation of reagents, scavengers and catalysts. This technique, coined polymer-assisted solution phase chemistry (PASP), allowed solution phase synthesis of compoimds, yet still enjoying the bene-... 

Finally, the introduction of focused microwave instruments further enabled to speed up the synthesis of libraries, by reducing the actual time needed for reaction [28-34]. The combination of using dedicated microwave instruments and sohd or solution phase tagging subsequently became a very powerful tool for PASP and SPOS apphcations [25,26,33-51]. 

An alternative approach towards the PASP synthesis of isocyanides was developed by Bradley [100,101]. It involved the use of a polymer-supported sul-fonyl chloride in the presence of base to afford the dehydration of formamides (Scheme 21). The formamides required could be easily prepared by reaction of the corresponding amines with a formylated benzotriazole resin. Opti-... 

Both PASP and MAOS are by now recognized as powerful tools by synthetic chemists. The use of both techniques together is somewhat newer and has not yet reached widespread use, as the relatively small number of publications testifies. However, we feel that the examples presented clearly demonstrate how powerful this combination can be, in particular if we keep in mind how complementary these tools are, one simplifying work-up and purification procedures while the other one decreases the reaction time. Considering the ever-increasing interest in the pharmaceutical industry for focused, mediumsized, high purity combinatorial libraries, this combination should attract more and more interest from both academic and industrial laboratories. At the same time, the need to increase productivity should bring synthetic and... 

Polymer micelles are nanometer sized (usually several tens of nanometers) self-assembled particles having a hydrophobic core and hydrophilic outer shell composed of amphiphilic AB- or ABA-type block copolymers, and are utilized as drug delivery vehicles. The first polymer micelle-type drug delivery vehicle was made of PEG-b-poly(aspartic acid) (PEG-b-PAsp), immobilizing the hydro-phobic anticancer drugDXR [188-191]. After this achievement by Kataoka et al., a great amount of research on polymer micelles has been carried out, and there are several reviews available on the subject [192-194]. 

Treves, A., Turolla, R., Zane, S., Colpi, M. (2000), Isolated neutron stars accretors and coolers , PASP 112, 297. 

EDC FDPP Fmoc HOBt LiHMDS MAMP MCPBA MeOPEG NCA NMP PAL PASP PBP PEG SASRIN TEA TFA TMAD N-Ethyl-N - [ 3 - (dimethy lamino)propy 1] -c arbodiimide hydrochloride Pentafluoro phenyldiphenyl phosphate 9 -Fluoreny lme thoxy c arbony 1 Hydroxybenzotriazol Lithium hexamethyldisilazane Merrifield, alpha methoxy phenyl resin w-Chloroperbenzoic acid Methoxy polyethylene glycol /V-Carboxv a-aminoacid anhydride /V - M e t h v 1 pyrrol i do n e Peptide amide linker Polymer assisted solution phase Penicillin-binding proteins Polyethylene glycol Super acid sensitive resin Triethylamine Trifluoroacetic acid Tetramethylamine azodicarboxylate. 

Scheme 5 Application of polymer-assisted solution phase (PASP) technique in Staudinger...

One of the major innovations in combinatorial and medicinal chemistry in recent years aiming at efficient diversity-oriented synthesis has been the implementation of polymer reagents in polymer-assisted solution phase (PASP) synthesis. This contribution will present—following an introduction to the field—a concept of advanced polymer reagents based on reactive intermediates and active reactants that should extend the scope PASP synthesis significantly. Experimental procedures describing preparation and use of the novel polymer reagents are included. 

Polymer-Assisted Solution Phase (PASP) Synthesis... 

Fig. 1. Polymer-assisted solution phase (PASP) synthesis combines the merits of solution-phase chemistry with the advantages of facilitated phase separation by using polymer reagents (a) or scavenger resins (b).

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