Practical application of 3-substituted-2,6-difluoropyridines in drug discovery: Facile synthesis of novel protein kinase C theta inhibitors |
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Authors: | Taisuke Katoh Yoshihide Tomata Masaki Setoh Satoshi Sasaki Takafumi Takai Yayoi Yoshitomi Tomoya Yukawa Hideyuki Nakagawa Shoji Fukumoto Tetsuya Tsukamoto Yoshihisa Nakada |
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Affiliation: | Pharmaceutical Research Division, Takeda Pharmaceutical Company, Ltd, 26-1, Muraokahigashi 2-chome, Fujisawa, Kanagawa 251-8555, Japan |
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Abstract: | We previously reported a facile preparation method of 3-substituted-2,6-difluoropyridines, which were easily converted to 2,3,6-trisubstituted pyridines by nucleophilic aromatic substitution with good regioselectivity and yield. In this study, we demonstrate the synthetic utility of 3-substituted-2,6-difluoropyridines in drug discovery via their application in the synthesis of various 2,3,6-trisubstituted pyridines, including macrocyclic derivatives, as novel protein kinase C theta inhibitors in a moderate to good yield. This synthetic approach is useful for the preparation of 2,3,6-trisubstituted pyridines, which are a popular scaffold for drug candidates and biologically attractive compounds. |
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Keywords: | 3-Substituted-2,6-difluoropyridine 2,3,6-Trisubstituted pyridine Macrocyclic derivatives Drug design |
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