Solid-phase synthesis overview

The requirement for diverse compound libraries by means of solid-phase synthesis led to the development of hnkers for most functional groups found in organic synthesis. The number of hnkers developed for a specific group also reflects the distribution of pharmacophoric groups present in natural products and other bioactive compounds. Tab. 3.16 gives an overview of examples of hnkers for different functional groups. 

In this chapter some general techniques for the performance of solid-phase reactions are presented. An overview of analytical tools suitable for the characterization of support-bound intermediates is also given, and strategies for the selection of reagents and reactions for parallel solid-phase synthesis are discussed. 

This article gives an overview of the main technical aspects of solid-phase synthesis and reviews the application of this technique for the synthesis of oligopeptides and proteins, oligonucleotides, oligosaccharides, and small molecules. 

How to synthesize biologically active polypeptides chemically has long been an important challenge for many fields in chemistry and biology. In the past, the development of solution-phase and solid-phase synthesis techniques has made it possible to synthesize large molecules like peptides with molecular weights up to 10,000. The purpose of this review is to provide an overview of how to prepare natural bioactive peptides synthetically. Because of space limitations, this review concentrates on peptide hormones and neurotransmitters. 

This chapter aims to present an overview on the main peptide bond modifications which have been proposed in the recent years. The solution- and solid-phase synthesis of the new synthetic oligomers, the methods for their characterization, and their biological and folding properties will be discussed. Particular emphasis will be given to those modifications which are suitable for combinatorial chemistry applications and developments. 

Often one of the steps in this domino reaction is a cycloaddition. A recent review by Dax et al. [Id] gives an overview of the state of the art of multicomponent reactions in solid phase synthesis. High pressure can play an important role in extending the scope of these reactions. 

As of today, apart from straightforward one-step derivatizations, the vast majority of analoging procedures by combinatorial synthesis are carried out on solid support. This overview focuses on organic chemistry adapted to the operation mode of solid-phase synthesis. The translation of protocols from solution chemistry to validated solid-phase procedures is a nontrivial task, often... 

Basu and Mandal have presented a comprehensive review on various sustainable synthetic strategies leading to benzimidazoles, quinoxalines, and their congeners highlighting the scope, limitations, and plausible mechanisms. These heterocyclic scaffolds have already drawn considerable interests to the researchers at large for their well-established biological and pharmaceutical properties. The authors have given emphasis on the sustainable processes that involve solid-phase synthesis, biomimetic synthesis, combinatorial synthesis, various catalytic methods, and reactions promoted by different solid sinfaces, solvent-free or on-water conditions or xmder microwave irradiation. This overview would serve as a useful somce of information to the readers in this particular area of interest. 

In this volume, state-of-the-art solid-phase synthesis is presented from different angles. Ranging from methodology development to application in the synthesis of complex native and designed structures, a complete overview is presented. 

Figure 3.1 General overview of solid-phase synthesis of sequence-defined glycopolymer segments a) suitable building blocks are synthesised, presenting a spacer unit or a functional moiety in the side chain b) these building blocks are then coupled in the solid phase until the desired chain length and sequence are obtained and c) on-resin modification of the side-chain functionalities introduces sugar ligands. The sequence-defined, monodisperse products are obtained after cleavage from the solid support. Reproduced with permission from D. Ponader,...

This chapter describes the basic protocols for solid-phase peptide synthesis using the Fmoc group as the 2 -protecting group (Fmoc-SPPS). The chapter introduces resins and their handling, choice of linkers, and the most common methods for peptide chain assembly. The proper choice of resins and linkers for solid-phase synthesis is a key parameter for successful peptide synthesis. This chapter provides an overview of the most common and usefiil resins and linkers for the synthesis of peptides with C-terminal amides, carboxylic acids, and more. The chapter finishes with robust protocols for general solid-phase peptide synthesis, i.e., the standard operations. 

Here, we present an overview of the aspects of the design, synthesis, analysis, and screening of combinatorial solid-phase glycopeptide libraries as compared to parallel glycopeptide arrays. 

This chapter will cover an overview of recent advances in solid-phase-assisted solution-phase combinatorial synthesis, specifically the use of scavenger resins in assisting in the isolation of pure product without the need for chromatography. In addition, an experimental section has been included. 

Herein, an overview is given of some characteristic examples and highlights of reactions carried out on solid support. This overview does not include solid-phase peptide or other oligomer synthesis. 

Safety-Catch and Traceless Linkers in Solid Phase Organic Synthesis Table 16.1 Overview of safety-catch linker types. 

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