Polymer Library Preparation

Fig. 7.14 3D-representation of imprinting factors (IF) obtained from the rebinding of BV in phosphate buffer pH 7.4 to the polymer library prepared from the design shown in Fig. 7.13. Arrows indicate compositions selected for upscaling as well as the conventional composition used to produce the previously reported MIP...

In related work a library of 1,458 peptide ligands and various metal salts was tested in hydrolysis reactions of (p-nitrophenyl)phosphates.35 An active substructure composed of polymer-bound histidine in combination with Eu3+ was identified by further dissecting the original hit structure. It needs to be pointed out that catalytically active polymer beads can also be tested for catalytic activity using IR-thermography. In a seminal paper this was demonstrated using 7,000 encoded polymer beads prepared by split-and-pool methods, specifically in the metal-free acylation of alcohols.36... 

Within the following sections we will give a brief overview of the available high-throughput methods for the preparation and screening of polymer libraries and then focus our discussion on well recognized literature examples of polymer libraries. 

Polymer libraries are generally not prepared for their own sake, but rather in order to explore some key property of the investigated materials. The technique used to prepare a given polymer library is often dictated by the method(s) to be used to screen or characterize the library compositions for the key properties of interest. 

More specific libraries, such as polymer thin film (gradient) libraries or libraries prepared via controlled polymerization techniques, are not part of this overview, but will be discussed in detail in other chapters of this book [94, 95],... 

In Chap. I, we provide an introduction to the strategies that have been reported for the preparation and characterization of polymer libraries and then highlight... 

The deconvolution of compound libraries prepared by the mix-and-split method can be greatly simplified by using polymeric supports that have been labelled with various dyes prior to library synthesis. In this case, the first monomer can be identified from the color or the UV spectrum of each bead. This type of labelling can, for instance, be achieved by partial derivatization of the support with different dyes [47], or by the use of polymers prepared from monomers showing characteristic IR or Raman spectra [48],... 

Two complementary procedures have been developed for alkylation of secondary amines [11] - both of which involve the use an excess of amine to drive the reaction to completion. The remaining amine was removed from the required tertiary amine using a polymer supported isocyanate 5 as a nucleophilic scavenger (under thermodynamic control) (Table 1 entry 2). The use of this amine scavenger has subsequently been applied in the purification of urea-based libraries prepared by solid-phase organic synthesis [12],... 

Monger et al. (100) reported the synthesis and screening of a 1344-member discrete polymer library L15 as a source of catalysts for the dehydration of the p-hydroxy ketone 11.33 to the enone 11.34 (equation 1, Fig. 11.21). The main feamres of L15, obtained from poly(acrylic anhydride) 11.32 (101) as a scaffold and the amine monomer set Mi (11 representatives) are reported in Fig. 11.21. The protocols for library preparation followed the same principles seen for L14 in the previous section. The presence of both acidic (the COOH backbone, to protonate the OH in 11.33 and promote its departure) and basic groups (side chains in some Mi representatives, to promote proton abstraction) should fulfill the core functional requirements to exert the overall catalytic activity. 

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