Incorporation of Heterocycles into Combinatorial Chemistry

The author has summarized a decade of teaching combinatorial chemistry into this timely brief. The solid phase synthesis of unnatural heterocyclic alpha-amino acids is illustrated by practical examples starting from the ABCs of peptide synthesis explored in chapter one. Chapter two is concerned with the solid phase synthesis which is shown on various techniques BillBoard, tea-bag, and Lantern devices, and demonstrated on heterocyclic examples and protocols. In the third chapter the tools for accelerating chemical synthesis solid phase and liquid phase are reviewed. Here the techniques of parallel refluxing (including microwave and flow technique) and parallel separation (filtration, centrifugation, evaporation, and chromatography) are described. In the chapters 4 and 5 the author goes on to describe how the liquid phase synthesis of heterocycles (reductive amination and Ugi reaction of heterocycles) is illustrated with the use of semi-automated protocols. Finally, the designof combinatorial libraries of heterocycles is reviewed including the original author's findings.

Numerous step-by-step instructions and protocols on preparation of heterocyclic libraries Review of techniques for solid phase synthesis (including tea-bags, lanterns etc.) Various techniques of liquid phase parallel synthesis illustrated by photos Includes supplementary material: sn.pub/extras

Autorentext

Prof. Eugene V. Babaev is a Professor at Moscow University, working as the Head of the Combinatorial chemistry Center. He contributed chapters in the following books: Fluorine in Heterocyclic Chemistry (Springer, Wien, 2014) 23 pages, Chemical Topology: Introduction and Fundamentals (Gordon & Breach, 1999) 98 pages; Targets in Heterocyclic Systems - Chemistry and Properties (Soc.Chim. Ital., Rome, 1997) 34 pages; Concepts in Chemistry: a Contemporary Challenges(John Wiley, 1996) 58 pages; Graph Theoretical Approaches to Chemical Reactivity" (Kluwer, 1994) 12 pages; Principles of Symmetry and Systemology in Chemistry (MSU Press, 1987) 25 pages; Philosophical Problems of Chemistry(MSU Press, 1988) 20 pages., Prof. Babaev is also the author of 10 reviews, the scientific editor of the special issue of Mendeleev Chemistry Journal (Vol.53, No.5, 2009) on combinatorial chemistry, author of 150+ scientific papers and 100+ abstracts at scientific meetings.

Inhalt
Introduction.- Peptide Synthesis of Libraries of Non-Natural Amino Acids.- The choice of tools for implementing multi-stage transformations. SPOS for Beginners.- Secrets of Parallel Liquid-Phase Synthesis.- Most Combinatorial LPOS Reactions: Reductive Amination with a Scavenger.- A Parallel Ugi Reaction.- Combinatorial Heterocyclic Chemistry in Higher School.