An enantioselective total synthesis of Tofacitinib (CP-690,550), a Janus tyrosine kinase (JAK3) specific inhibitor has been achieved from the readily available 4-piperidone. Proline catalysed hydroxylation is the key step for the synthesis of enantiopure 1-benzyl-4-methylpiperidin-3-ol. (C) 2021 Elsevier Ltd. All rights reserved.
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Univ Tokyo, Grad Sch Agr & Life Sci, Dept Appl Biol Chem, Bunkyo Ku, 1-1-1 Yayoi, Tokyo 1138657, JapanUniv Tokyo, Grad Sch Agr & Life Sci, Dept Appl Biol Chem, Bunkyo Ku, 1-1-1 Yayoi, Tokyo 1138657, Japan
Okada, Shoko
Mori, Naoki
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Univ Tokyo, Grad Sch Agr & Life Sci, Dept Appl Biol Chem, Bunkyo Ku, 1-1-1 Yayoi, Tokyo 1138657, JapanUniv Tokyo, Grad Sch Agr & Life Sci, Dept Appl Biol Chem, Bunkyo Ku, 1-1-1 Yayoi, Tokyo 1138657, Japan
Mori, Naoki
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Ishigami, Ken
Watanabe, Hidenori
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Univ Tokyo, Grad Sch Agr & Life Sci, Dept Appl Biol Chem, Bunkyo Ku, 1-1-1 Yayoi, Tokyo 1138657, JapanUniv Tokyo, Grad Sch Agr & Life Sci, Dept Appl Biol Chem, Bunkyo Ku, 1-1-1 Yayoi, Tokyo 1138657, Japan