Core solid-supported

A limitation of this approach was the fact that the cyclization could not be accomplished on the resin. This would preclude further functionalization of the core. Therefore an alternate approach was to link the resin to the core via an aminoalcohol spacer as in 93. Furthermore, since linkage was conducted through the P-ketoester component rather than through the nitrogen atom, dihydropyridines 94 could now be formed on the solid support. When the 4-aryl substituent of 94 was nitro, on-resin reduction to the corresponding amine was possible. This allowed for further addition of diversity elements to the core scaffold before cleavage from the resin. 

The utility of the stepwise, double-coupling procedure is demonstrated in the parallel synthesis of Tamoxifen derivatives on solid support [127] (Scheme 1-29). 1-Alkenylboronates thus obtained by a diboration-cross coupling sequence are further coupled with p-silyUodobenzene supported on polymer resin. Using this strategy, each position about the ethylene core is modified by the appropriate choice of alkyne, aryl halide, and cleavage conditions for the synthesis of a library of Tamoxifen derivatives. 

In another application, the group of Berteina-Raboin demonstrated the solid-supported synthesis of the indole core of melatonin analogues under microwave irradiation (Scheme 7.6) [26]. A benzoic acid derivative was coupled to Rink amide resin by... 

Two strategies have emerged for the synthesis of natural-product-like libraries on solid. The first involves building the entire core structure on solid support, a very challenging proposi-... 

Scheme 1 Synthesis of fifc-PPEs on a solid support (S), in the presence of core (C) molecules, and/or by the addition of a non-halogenated arylethyne terminator (T)...

Alternatively, initiator cores have been tethered to solid support (Merrifield resins [83]). Using protein synthesis procedures that avoid the workup difficulties involved in handling large excesses of reagents, one can readily control dendrimer growth. Unfortunately, only noncleavable linkers have been examined to date with these PAMAM dendrimers. The use of initiator cores possessing cleavable linkers should make dendrimer synthesis and isolation very facile. This was demonstrated for mono-dendrons derived from poly(lysines) as reported by Tam et al. [105-107] (Fig. 26). 

Frank, R. and Coring, R. (1988) Simultaneous multiple peptide synthesis under continuous flow conditions on cellulose paper discs as segmental solid supports. 

In addition to the benefits of MEF from metal nanostructures deposited onto solid supports that are very useful in surface bioassays, MEF can also be observed from individual nanostructures in bioassays carried out in solution. In this regard, fluorophores and metal nanostructures can be assembled in core-shell architecture and can be used as fluorescent nanoparticles as indicators in biological plications such as imaging of cellular activity or single-molecule sensing. 

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