The art of drug syntheses

The discovery of efficacious new human therapeutic agents is one of humanity’s most vital

tasks. It is an enormously demanding activity that requires creativity, a vast range of scien-

tific knowledge, and great persistence. It is also an exceedingly expensive activity. In an

ideal world, no education would be complete without some exposure to the ways in which

new medicines are discovered and developed. For those young people interested in science

or medicine, such knowledge is arguably mandatory.

In this book, Douglas Johnson, Jie Jack Li, and their colleagues present a glimpse

into the realities and demands of drug discovery. It is both penetrating and authoritative.

The intended audience, practitioners and students of medicinal and synthetic chemistry,

can gain perspective, wisdom, and valuable factual knowledge from this volume. The

first two chapters of the book provide a clear view of the many complexities of drug dis-

covery, the numerous stringent requirements that any potential therapeutic molecule must

meet, the challenges and approaches involved in finding molecular structures that “hit” a

biological target, and the many facets of chemical synthesis that connect initial small-scale

laboratory synthesis with the evolution of a process for successful commercial production.

The remaining 15 chapters provide a wealth of interesting synthetic chemistry as applied

to the real world of the molecular medicine of cancer, infectious, cardiovascular, and

metabolic diseases. At the same time, each of these chapters illuminates the way in

which a first-generation therapeutic agent is refined and improved by the application of

medicinal chemistry to the discovery of second- and third-generation medicines.

The authors have produced a valuable work for which they deserve much credit. It is

another step in the odyssey of drug finders; a hardy breed that accepts the high-risk nature

of their prospecting task, the uncertainties at the frontier, and the need for good fortune, as

well as focus and sustained hard work. My ability to predict the future is no better than that

of others, but I think it is possible that a highly productive age of medicinal discovery lies

ahead, for three reasons: (1) the discovery of numerous important new targets for effective

disease therapy, (2) the increasing power of high-throughput screening and bio-target

structure-guided drug design in identifying lead molecules, and (3) the ever-increasing

sophistication of synthetic and computational chemistry.

E. J.