'An avalanche of chemistry' was my first impression of this book

The art of drug synthesis 

Douglas S Johnson and Jie Jack Li 

Chichester, UK: John Wiley  2007 | 276pp | ?47.50 (HB) ISBN 978-0-471-75215-8 

Reviewed by Peter W R Caulkett

’An avalanche of chemistry’ was my first impression of this book - there’s a lot of it, and it picks you up and carries you along. However, like an avalanche, it can be overwhelming and indiscriminate. That said, the book has a lot to offer: the creativity, imagination, and sheer hard work that go into drug synthesis are clearly evident, as is the enthusiasm, and in places the exuberance, of the authors for their subject. 

The first two chapters give a flavour, necessarily superficial, of the roles of medicinal chemistry and process chemistry in drug discovery, and the remainder are given over to the syntheses of various classes of marketed (or in some cases withdrawn) drug.  

Does the book fulfil its claim of being a unique and invaluable perspective? Well, probably not, but it is certainly interesting and useful. It is not a particularly good read - the text merely repeats in words what is given in the reaction schemes, thus: ’...ester 16 is then hydrolysed to acid 17 with lithium hydroxide’. This can get a bit tedious. More annoyingly in my view, the reactions are presented without mechanisms or any rationalisation of the outcome - for instance, Chapter 9 is replete with regiospecific N-alkylations of (benz)imidazoles, but nowhere is the observed regiochemical outcome explained. Of course, these, and very many other, reactions could be followed up using the comprehensive references, but nevertheless I was left with a slight sense of dissatisfaction and incompleteness. 

Where I see the book being very useful is as a starting point for student seminars or discussion groups; there is plenty of good chemistry, so aspiring organic and medicinal chemists would benefit equally. Also, it is highly illuminating just to dip into for a browse and to marvel at some of the excellent chemistry that goes on in the pharmaceutical industry. If nothing else, you should read the chapter on flu drugs Relenza and Tamiflu - it is a gem.