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Synfacts 2011(11): 1158-1158
DOI: 10.1055/s-0031-1289254
DOI: 10.1055/s-0031-1289254
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag
Stuttgart ˙ New York
Synthesis of Febuxostat, Tafamadis, and Texaline
T. Yamamoto, K. Muto, M. Komiyama, J. Canivet, J. Yamaguchi, K. Itami*
Nagoya University and Teijin Pharma Ltd., Tokyo, Japan
Further Information
Publication History
Publication Date:
19 October 2011 (online)
Significance
Over 50 examples of a new nickel-catalyzed C-H arylation of thiazoles, benzothiazoles, oxazoles, benzoxazoles, and benzimidazoles with haloarenes is described. The practical potential of the reaction was illustrated by the syntheses of febuxostat (Adenuric®, a xanthine oxidase inhibitor), tafamidis (effective for the treatment of TTR amyloid neuropathy) and texaline (a natural product with antitubercular activity).