Palladium chemistry, despite its immaturity, has rapidly become an indispensable tool for synthetic organic chemists. Heterocycles are of paramount importance in the pharmaceutical industry and palladium chemistry is one of the most novel and efficient ways of making heterocycles. Today, palladium-catalyzed coupling is the method of choice for the synthesis of a wide range of biaryls and heterobiaryls. The number of applications of palladium chemistry to the syntheses of heterocycles has grown exponentially.
These developments highlight the need for a monograph dedicated solely to the palladium chemistry in heterocycles and this book provides a comprehensive explanation of the subject. The principal aim of the book is to highlight important palladium-mediated reactions of heterocycles with emphasis on the unique characteristics of individual heterocycles.
1. Palladium chemistry of heterocycles has its “idiosyncrasies” stemming from their different structural properties from the corresponding carbocyclic aryl compounds. Even activated chloroheterocycles are sufficiently reactive to undergo Pd-catalyzed reactions. As a consequence of &agr and &bgr activation of heteroaryl halides, Pd-catalyzed chemistry may take place regioselectively at the activated positions, a phenomenon rarely seen in carbocyclic aryl halides. In addition, another salient peculiarity in palladium chemistry of heterocycles is the so-called "heteroaryl Heck reaction". For instance, while intermolecular palladium-catalyzed arylations of carbocyclic arenes are rare, palladium-catalyzed arylations of azoles and many other heterocycles readily take place. Therefore, the principal aim of this book is to highlight important palladium-mediated reactions of heterocycles with emphasis on the unique characteristics of individual heterocycles.
2. A myriad of heterocycles are biologically active and therefore of paramount importance to medicinal and agri

Key Features

- Contains the most up-to-date developments in this fast-moving field - Includes 3 new chapters - Incorporates material from selected well-respected authors on heterocyclic chemistry


Medicinal Chemists, Organic Chemists

Table of Contents

Chapter 1: Introduction Chapter 2: Pyrroles Chapter 3: Indoles Chapter 4: Pyridines Chapter 5: Thiophenes And Benzo[B]Thiophenes Chapter 6: Furans And Benzo[B]Furans Chapter 7: Thiazoles And Benzothiazoles Chapter 8: Oxazoles And Benzoxazoles Chapter 9: Imidazoles Chapter 10: Pyrazines And Quinoxalines Chapter 11: Pyrimidines Chapter 12: Quinolines Chapter 13: Pyridazines Chapter 14: Industrial Scale Palladium Chemistry


No. of pages:
© 2007
Elsevier Science
Print ISBN:
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About the editors

Jie Jack Li

Affiliations and Expertise

Pfizer Global Research and Development, Ann Arbor, Michigan, USA

Gordon Gribble

Gordon Gribble is the Dartmouth Professor of Chemistry at Dartmouth College, Hanover, USA. His research program covers several areas of organic chemistry, most of which involve synthesis, including novel indole chemistry, triterpenoid synthesis, DNA intercalation, and new synthetic methodology. Prof Gribble also has a deep interest in naturally occurring organohalogen compounds, and in the chemistry of wine and wine making.

Affiliations and Expertise

Department of Chemistry, Dartmouth College, Hanover, NH, USA