Solid-Phase Synthesis A Practical Guide

This volume provides the information needed to synthesize peptides by solid-phase synthesis (SPS) - employing polymeric support (resins), anchoring linkages (handles), coupling reagents (activators), and protection schemes. It presents strategies for creating a wide variety of compounds for drug discovery and analyzes peptides, DNA, carbohydrates, conjugates of biomolecules, and small molecules.

The solid support strategy in solid-phase synthesis; amino acids -alpha-amino protecting groups; side-chain protecting groups; solid supports for the synthesis of peptides and small molecules; coupling methods - solid-phase formation of amide and ester bonds; homodetic cyclic peptides; disulfide formation in synthetic peptides and proteins -the state of the art; solid-phase convergent approaches to the synthesis of native peptides and proteins; preparation of glyco-, phospho-, and sulfopeptides; oligonucleotide synthesis; synthesis of oligonucleotide-peptide conjugates and nucleopeptides; the chemistry of peptide nucleic acids; solid-phase synthesis of pseudopeptides and oligomeric peptide backbone mimetics; instrumentation; the purification of synthetic peptides; analysis of synthetic peptides; the chromatographic analysis of combinational arrays - parallel HPLC and HPLC-MS.

Steven A. Kates, Fernando Albericio