Synthesis of Metabolites and Related Compounds of 3-Isobutyryl-2-isopropylpyrazolo[1,5-α]pyridine (Ibudilast). II. Metabolites of Pyridine Ring

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概要

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• Novel 6-hydroxylated or methanesulfonylated pyrazolo[1,5-α]pyridine derivatives as an authentic reference of metabolites for 3-isobutyryl-2-isopropylpyrazolo[1,5-α]pyridine (ibudilast) were prepared by the method of substitution with Br^+ on the pyridine ring and subsequent displacement of Br with MeO^- or MeS^-. For this reason, we investigated the orientation of halogenation on the pyridine ring of pyrazolo[1,5-α]pyridine. The reactivity of the pyridine ring was at the 6-position, folowed by the 4-position. We supposed that this finding comes from the electron-donating resonance effect of bridge-head nitrogen. These experimental results were in good agreement with the results of atomic electron densities, but a clear difference was not obtained in those of the Frontier orbitals.

• 社団法人日本薬学会の論文
• 1992-03-25

著者

• 鈴江 清吾

  Central Reseasrch Laboratories Kyorin Pharmaceutical Co. Ltd.

• 粟野 勝也

  Central Research Laboratories, Kyorin Pharmaceutical Co., Ltd.

• 岩瀬 一彦

  Central Research Laboratories, Kyorin Pharmaceutical Co., Ltd.

• 永津 芳雄

  Central Research Laboratories, Kyorin Pharmaceutical Co., Ltd.

• 粟野 勝也

  Central Reseasrch Laboratories Kyorin Pharmaceutical Co. Ltd.

• 永津 芳雄

  Central Research Laboratories Kyorin Pharmaceutical Co. Ltd.

• 岩瀬 一彦

  Central Research Laboratories Kyorin Pharmaceutical Co. Ltd.

関連論文

• Synthesis of Metabolites and Related Compounds of 3-Isobutyryl-2-isopropylpyrazolo[1,5-α]pyridine (Ibudilast). III. 6,7-Dihydrodiol
• Synthesis of Metabolites and Related Compounds of 3-Isobutyryl-2-isopropylpyrazolo[1,5-α]pyridine (Ibudilast). II. Metabolites of Pyridine Ring
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