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The Art of Process Chemistry. Edited by
Nobuyoshi Yasuda.
Article in Angewandte Chemie International Edition · September 2011
DOI: 10.1002/anie.
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The Art of Process Chemistry
Keen on some excitement from within the world of chemistry? Are you curious to understand how “they” are doing it? If your response to these straight questions is an unambiguous “yes”, then this newly released book really is a must for you. The Process Research Group of Merck Research Laboratories in Rahway, New Jersey, has for many years been regarded by most of its peers in the industry as the world-leading institution engaged in the design and develop- ment of chemical processes for the large-scale manufacture of pharmaceutically active ingre- dients, and it probably still is. How else could you explain the fact that a whole book of 282 pages is entirely devoted to case histories that emanate from work carried out in the Merck facilities (from the 1990s and onwards), now compiled in the form of nine chapters (each consisting of between 20 and 40 pages) for the benefit of all of us “outsiders”? In fact, the title of the book should leave nobody in any doubt— this exemplarily short title shows this to be a piece of work that makes clear its fascination with the subject of process chemistry. The esteem goes so far as to put the discipline on a level where it is seen to be on a par with art in general—a viewpoint developed by the editor in some detail in the preface. Some people outside the core area of process chemistry might not entirely agree, but this excellent book will definitely contribute to raising the profile of what must be regarded as a fascinating topic, which is largely pursued in an industrial environment outside academic institutions. The fact that the work of designing and developing safe, robust, and viable processes has been carried out with the ultimate aim of transferring them to commercial production has traditionally led to a reluctance to present the achievements to an external audience. However, much of that belongs to the past, and over the recent two or three decades a tremendous change has taken place that encourages wider dissemination, albeit this openness to communicate is not embraced by everyone. In this development, Merck has played a seminal role by taking a leading position in the transformation of process research from a low-profile subject (“it s just about the scaling up of laboratory procedures, so what s the big deal?”) to an area that has gained the reputation of operating at the highest scientific level, second to none. We owe Merck a lot for what they have contributed and shared with all of us, and therefore they should be
entitled to our admiration and esteem. Aspects of all this, based on what has become a long tradition within Merck, are treated thoroughly in the book. If you want to gain a deeper insight into the Merck world of chemical processes in order to find out what they are doing so well, and how, then you must read this book! I will now consider the contents in more detail and discuss some particular strengths and weak- nesses. Looking at the specific drug projects that are covered, it becomes evident that they span a broad range in terms of molecular diversity, coupled with a wide variation in the associated chemistry-related challenges. Many of the compounds for which large- scale synthetic processes have been developed, as described in the book, have actually ended up in commercially launched medicines, and a few of these are enjoying a worldwide reputation as the basis of breakthrough therapies offering significant benefit to patients. Thus, branded drugs such as the HIV antiviral Efavirenz, finasteride/Proscar for the treatment of prostatic hypertrophy, the anti- migraine agent rizatriptan/Maxalt, and raltegravir/ Isentress as the first HIV/AIDS integrase inhibitor are thoroughly documented in the book, and in these examples its value becomes especially clear by virtue of our insight that they “made it all the way”. Every project offers some learning, but this is especially pronounced for successful products for two reasons: firstly, the processes developed have been shown to be suitable for commercial produc- tion, not just for pilot scale production, and secondly, because of the extremely high rate of project attrition in the pharmaceutical industry, we rarely get to know the intrinsic details that underlie full-scale manufacturing methods. As the book fulfills the role of conveying a deep understanding of the harsh realities in process research and of the different degrees of success in solving problems— often coupled with a high level of smartness, innovation, and creativity—the work is worthy of attracting a large readership, ranging from profes- sionals in the pharmaceutical business to graduate students who hope to find a position in an industrial development department, and to academics with the ambition to gain invaluable information about “what they are doing in industry and what problems they are grappling with”. Nowadays, reporting on the design and develop- ment of chemical processes is by no means unique, as shown by recently published books on topics such as asymmetric catalysis and green chemistry. How- ever, what differentiates this work is that it homes in on the endeavors and achievements of just one group, providing a learning experience about how a world-leading team goes about performing its tasks. Each of the chapters follows a generic structure divided into two sections: “Project Development” and “Chemistry Development”. In the former
The Art of Process Chemistry Edited by Nobuyoshi Yasu- da. Wiley-VCH, Weinheim
- 282 pp., hardcover E 119.00.—ISBN 978- 3527324705
Books
8784 2011 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim Angew. Chem. Int. Ed. 2011 , 50 , 8784 – 8785
