Journal
EUROPEAN JOURNAL OF ORGANIC CHEMISTRY
Volume 2016, Issue 22, Pages 3700-3704Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/ejoc.201600742
Keywords
Amino acids; Arylation; C-H activation; Ruthenium; Drug design
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Funding
- European Research Council under the European Community's Seventh Framework Program [307535]
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Versatile ruthenium(II) complexes derived from amino acids enabled the first general C-H arylations of aryltetrazoles with inexpensive aryl chlorides. The user-friendly Piv-Val-OH-based ruthenium(II) catalyst was characterized by a broad substrate scope, excellent functional group tolerance, and high catalytic activity. Thereby, the ruthenium(II) catalysis set the stage for the step-economical preparation of the blockbuster antihypertension drug Valsartan, while displaying unique robustness in the C-H arylation regime.
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