Paul Edwards

Purification strategies for combinatorial and parallel chemistry.

This review surveys the methods developed for the purification of intermediates and final compounds originating from parallel and combinatorial chemistry. Included will be reviews of polymer-assisted purification, liquid-phase combinatorial chemistry, fluorous synthesis, liquid-liquid and solid-phase extraction, reverse-phase HPLC and supercritical fluid chromatography. A critique of each method is given, highlighting the methodologies strengths and weaknesses.

The synthesis of 2-ketopiperazine acetic acid esters and amides from ethylenediamines with maleates and maleimides

The reaction of substituted ethylenediamines with various fumarates, maleates, and maleimides to form substituted ketopiperazine acetic acid esters and amides was investigated. This method affords a straightforward, high yield approach to a variety of potential peptidomimetics and can yield surprising results with regard to regio- and stereoselectivity.

Moving beyond Combinatorial Chemistry for Greater Efficiency in Lead Discovery

Pfizer Inc. is a research based global pharmaceutical company committed to the discovery and development of innovative medicines that improve the quality of life of individuals throughout the world. In order to gain a competitive advantage over competitor companies in the discovery of new medicines, we must speed up drug discovery and drive down costs. Using non-combinatorial chemistry techniques increases the efficiency with which we discover new ‘leads,’ leveraging our drug discovery efforts through retaining complete control over the properties of each product made. Compound purification, managed through in-house software, augments the quality of data obtained upon biological screening of compounds.

Monitor: molecules and profiles.

Monitor provides an insight into the latest developments in drug discovery through brief synopses of recent presentations and publications together with expert commentaries on the latest technologies. There are two sections: Molecules summarizes the chemistry and the pharmacological significance and biological relevance of new molecules reported in the literature and on the conference scene; Profiles offers commentary on promising lines of research, emerging molecular targets, novel technology, advances in synthetic and separation techniques and legislative issues.