Recent Application of Polystyrene-supported Triphenylphosphine in Solid-Phase Organic Synthesis

Recent years have witnessed a fast development of solid phase synthetic pathways, a variety of solid-supported reagent and its applications in diverse synthetic strategies and pharmaceutical applicability’s. Polymer-supported triphenylphosphine is getting a lot of applications owing to the speed and simplicity in the process. Furthermore, ease of recyclability and reuse of polymer-supported triphenylphosphine added its advantages. This review covers a wide range of useful organic transformations which are accomplished using cross-linked polystyrene-supported triphenylphosphine with the aim of giving renewed interest in the field of organic and medicinal-combinatorial chemistry.

Traceless Solid-Phase Synthesis of Ketones via Acid-Labile Enol Ethers: Application in the Synthesis of Natural Products and Derivatives

In solid-phase organic synthesis, Wang resin is traditionally used for the immobilization of acids, alcohols, phenols, and amines. We report the use of Wang resin for the traceless synthesis of ketones via acid-labile enol ethers. We demonstrate the practicality of this synthetic strategy on the solid-phase synthesis of pyrrolidine-2,4-diones, which represent the core structure of several natural products, including tetramic acid. Base-triggered condensation of pyrrolidine-2,4-diones yielded 4-hydroxy-1,1′,2′,5-tetrahydro-2H,5′H-[3,3′-bipyrrole]-2,5′-diones.

Greener solvents for solid-phase organic synthesis

Solid-phase organic synthesis is an essential method for the rapid synthesis of complex biological structures and libraries of small organic molecules. However, it is often associated with the use of large quantities of problematic solvents for the removal of excess reagents and reaction by-products. Given that solvent will often be the biggest contributor to waste generated in the average pharmaceutical/fine-chemical process, its exchange for a more desirable alternative often presents the biggest gains in terms of reducing environmental impact. This review aims to explore recent approaches to performing solid-phase organic synthesis, and associated solid-phase peptide synthesis, in neoteric solvents and reaction media that present greener alternatives.