The rapid expansion of combinatorial chemistry has renewed interest in solid-phase organic synthesis, a method that lends itself well to creating and screening large numbers of lead compounds. Solid-Phase Organic Syntheses, Volume 1 is the first volume in a series that will be updated annually, filling a gap in the existing chemical literature. Providing information previously unavailable from a single resource, this series is dedicated to providing researchers in the field with validated and tested methods for the solid-phase synthesis of interesting and biologically relevant molecules. Solid-phase methods will virtually always be invented for application in combinatorial organic synthesis. To meet these specific needs, Solid-Phase Organic Syntheses, Volume 1 focuses on a single type of synthetic transformation accomplished on solid support, and indicates how procedures are optimized to work with a structurally-wide variety of reagents. Written by recognized leaders in the field who review and test all chemical protocols before publication, organic transformations are organized by type of compound synthesized and reaction type.
For the first time, experimental details for proven solid-phase synthetic molecules are collected in a single, invaluable resource. Solid-Phase Organic Syntheses, Volume 1 provides combinatorial chemists and researchers in organic chemistry and medicinal chemistry with the tools and descriptive protocols to achieve syntheses of desired compounds using a variety of solid supports and reagents.
Table of Contents
Preface. 2--Aminothiazoles. Solid--Phase Mannich Reactions of a Resin--Immobilized Secondary Amine. Solid--Phase Synthesis of Ureas on Microtubes. Synthesis of p--Benzyloxybenzyl Chloride Resin. Solid--Phase Mannich Reactions of a Resin--Immobilized Alkyne. Solid--Phase Synthesis of Di--beta--Peptoids from Acrylate Resin: N--Acetyl--N--Benzyl--beta--Alaninly--N--Benzyl--beta--Alanine. Solid--Phase Synthesis of Benzoxazoles via Mitsunobu Reaction. N--Fmoc--Aminooxy--2--Chlorotrityl Polystyrene Resin for High Throughput Synthesis of Hydroxamic Acids. Facile Preparation of Chloromethylaryl Solid Supports. Preparation of Ameba Resin. An Efficient Solid Phase Synthetic Route to 1,3--Distributed 2,4 (1H, 3H)--Quinazolinediones Suitable for Combinatorial Synthesis. Backbone Amide Linker (Bal) Strategy for Solid--Phase Synthesis. The Allylsilyl Linker: Synthesis of Catalytic Binding of Alkenes and Alkynes to and Cleavage from Allyldimethylsilyl Polystyrene. Resin--Bound Isothiocyanates as Intermediates for the Solid--Phase Synthesis of Substituted Thiophenes. Author Index. Subject Index.