Organic Synthesis on Solid Phase: Support, Linkers and Reactions

Solid-Phase Organic Synthesis

Safety-Catch and Multiply Cleavable Linkers in Solid- Phase Synthesis

This review article focuses on concepts that incorporate safety-catch and multiply cleavable linkers in solid-phase synthesis. Discussed are specific applications of such linkers in the synthesis of peptides, peptide mimetics, and “small” organic molecules, as well as their limitations for particular chemistries and reaction conditions. © 1999 John Wiley & Sons, Inc. Biopoly 47: 353–363, 1998

Linkers, resins, and general procedures for solid-phase peptide synthesis.

This chapter describes the basic protocols for solid-phase peptide synthesis using the Fmoc group as the N (α)-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...

Solid-Phase Organic Chemistry: Synthesis of 2β-(Heterocyclylthiomethyl)Penam Derivatives on Solid Support

The impact of combinatorial chemistry of small molecules on the drug discovery process is now widely recognized by the scientific community [1]. Solid-phase organic synthesis (SPOS) is a valuable tool for the generation of structurally diverse compounds for combinatorial libraries. In our work dealing with the solid-phase synthesis of biologically interested compounds, we have developed methodo...

Understanding solid/solid organic reactions.

The concept of an organic reaction between two macroscopic solid particles is investigated. Thus, we study several reactions that have been recently reported to proceed "in the solid phase" and clearly show that, in most cases, grinding the two solid reactants together results in the formation of a liquid phase. This is true both for catalytic transformations (e.g., aldol condensations and olig...