Editorial pubs.acs.org/OPRD
Catalytic C−H Arylations as a Tool for Making Pharmaceuticals
F
ollowing on from previous Invited Academic Reviews that have appeared over the years in this journal, it is our pleasure to present you with an outstanding paper in this series authored by Prof. Lutz Ackermann from the Georg-August University in Göttingen, Germany. The topic addressed is concerned with a synthetically efficient methodology to create biaryl motifs of a type commonly encountered across a plethora of functionally important molecules. Many of these display a high degree of industrial significance in such diverse areas as pharmaceuticals, crop protection, and materials science. Where “conventional” organic synthesis has not been able to deliver methods in this regard with wider, more general applicability, the method at the centre-point of this review is catalytic C−H activation. This approach to achieving the desirable connection of two aromatic rings is far from novel but has enjoyed an enormous boom over the past two decades or so by virtue of catalyst development coupled with mechanistic understanding, which in itself qualifies the area as a truly hot topic both in academic and industrial settings. Thus, Ackermann presents an overview of recent results where a catalytic ruthenium(II) protocol building on the assistance of chelating groups such as carboxylates is utilized for the key aryl−aryl forming step in the preparation of a variety of angiotensin-II receptor blockers. This class of cardiovascular drugs is in wide clinical usage as medicines for the treatment of hypertension, with many famous branded products available to provide an efficacious control of a life-threatening condition. The features of the synthetic procedure include robustness, efficient C−H activation, functional group tolerance, low catalyst loading, and not the least, scalability. We would like to convey our sincere gratitude to Prof. Ackermann for having found the time to prepare such a splendid and timely paper for Organic Process Research & Development, and we hope that it will attract the interest from our broad readership as an example of how fundamental academic research is able to eventually cross-fertilize with industrial manufacture.
Hans-Jürgen Federsel*
Pharmaceutical Development, AstraZeneca, Macclesfield, Cheshire SK10 2NA, United Kingdom
Stefan Abele
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Process R&D, Actelion Pharmaceuticals Ltd., CH-4123 Allschwil, Switzerland
AUTHOR INFORMATION
Corresponding Author
*E-mail:
[email protected]. Notes
Views expressed in this editorial are those of the author and not necessarily the views of the ACS.
Published: January 16, 2015 © 2015 American Chemical Society
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DOI: 10.1021/op500391g Org. Process Res. Dev. 2015, 19, 259−259
