The Synthesis of Heterocycles

Heterocycles are always an interesting class of compounds due to their immense number of applications in pharmaceuticals, agrochemicals and fine chemicals. Unlike the classical methods for their syntheses, this book gives a concise update on the construction of the second heterocyclic ring using ortho-disubstituted aryl starting materials for accessing both five-membered and six-membered rings (Chapters 2 and 3) using some of the modern transition metal catalysts. I like the systematic approach of this book, starting with a list of frequently used double functionalised arenes (Chapter 1). The technology described in the book seems to be developed and inspired from Larock’s seminal heteroannulation reactions (1). There is a short chapter on macro heterocycle synthesis, showing the synthesis of somewhat larger molecules. Although palladium catalysts are widely used for these transformations, there are examples using other metals such as nickel and copper.

There are several other books available on the synthesis of heterocycles using transition metal catalysts (2, 3).

Conclusion

Since it is a specialised book for those who want to get an idea of how ortho-difunctionalised reagents can be used for five-membered and six-membered rings, this book will be very handy. Typical experimental protocols are listed throughout, although these experiments are taken directly from academic publications, with very little information on their merits in industry. However, this is not a severe criticism of the book. Hopefully this book will inspire those who are in industry to be aware of these methods for practical applications. Overall it is decent book to have in your library, if you are interested in modern methods for the synthesis of certain heterocycles.