SMase阻害剤を指向した新規SMA-7類縁体の合成研究
書誌事項
- タイトル別名
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- Synthesis of 2-amino alcohol derivatives oriented for a potent sphingomyelinase inhibitor
説明
Various alpha-amino ketones bearing a difluoromethylenephosphonate (DFMP) group at beta-position was synthesized by Liebeskind-Srogl reaction from the thioester of alpha-amino acid derivatives with boronic acids. Reduction of the obtained alpha-amino ketones with LiAlH(OtBu)3 proceeded in excellent diastereoselectivity to give anti-amino alcohols. These alcohol derivatives were readily converted into gamma-palmitoylamino-delta-hydroxy-alpha,alpha-difluorophosphonate, which would be useful as a vehicle for structure-activity relationship (SAR) studies on SMA-7, a potent spingomyelinase inhibitor. This synthetic method features high diversity and efficiency in replacement of the terminal substituent of SMA-7 for SAR studies.
収録刊行物
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- 反応と合成の進歩シンポジウム 発表要旨概要
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反応と合成の進歩シンポジウム 発表要旨概要 35 (0), 109-109, 2009
日本薬学会化学系薬学部会
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詳細情報 詳細情報について
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- CRID
- 1390282680612484224
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- NII論文ID
- 130006998328
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- 本文言語コード
- ja
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- データソース種別
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- JaLC
- CiNii Articles
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- 抄録ライセンスフラグ
- 使用不可
