スフィンゴシン-1-リン酸受容体作働薬CS-0777の開発研究

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タイトル別名
  • Exploratory and Process Research on S1P<sub>1</sub> Receptor Agonist CS-0777
  • スフィンゴシン-1-リンサン ジュヨウタイ サドウヤク CS-0777 ノ カイハツ ケンキュウ
  • Exploratory and Process Research on S1P1 Receptor Agonist CS-0777

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CS-0777 (4) is phosphorylated in vivo, and the phosphate of CS-0777 (CS-0777-P) (25) acts as a selective S1P1 receptor agonist, which is known as a novel mechanism of action to be able to provide a potent immunosuppressant agent. We report herein the primary synthetic route of CS-0777 and CS-0777-P using asymmetric desymmetrization of prochiral-diol precursor as a key reaction along with the biological activity of those compounds, and in the later part of the manuscript, we also describe an extensive process research effort to establish the scalable synthetic method to prepare CS-0777 at tens of kilogram scale.

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