オレフィン系1,3-ジオールのC2対称硫化物による触媒的非対称ブロモエテル化および非対称化
Zhihai Ke1, Chong Kiat Tan, Feng Chen
1Department of Chemistry, National University of Singapore , 3 Science Drive 3, Singapore 117543.
Journal of the American Chemical Society
|April 5, 2014
まとめ
新しいサイクル硫化物触媒は,ダイオルのエナチオセレクティブブロモエセリフィケーションとデシンメトリゼーションを可能にします. この方法は,抗真菌薬ポサコナゾール (ノクサフィル) を合成するための鍵です.
科学分野:
- 有機化学 オーガニック・ケミストリー
- カタリシス カタリシス カタリシス
- 薬用化学 薬用化学について
背景:
- オレフィン系1,3-ジオールは,汎用性の高い合成前駆体である.
- エナチオセレクティブおよびダイアステレオセレクティブ反応の開発は,薬物合成において極めて重要です.
- ポサコナゾール (ノクサフィル) は,重要な口服活性抗真菌薬である.
研究 の 目的:
- オレフィン系1,3-ジオルのエナチオセレクティブおよびダイアステロセレクティブブロモエセリフィケーションおよびデシンメトリゼーションのための新しい触媒方法の開発.
- この方法論をポサコナゾールの重要な中間物質の合成に適用する.
主な方法:
- C2対称サイクリック硫化ガスの触媒を用いた.
- エナチオセレクティブブロモエセリフィケーションを行いました.
- オレフィン系1,3-ジオルのダイアステロ選択的脱対化が達成されました.
主要な成果:
- 高度にエナチオセレクティブとダイアステレオセレクティブのブロモエセリフィケーションと脱対称化プロトコルを開発しました.
- 開発した方法を用いてポサコナゾールの重要な中間物質を成功して合成した.
結論:
- 開発された触媒システムは,複雑な分子合成のための効率的な経路を提供します.
- この方法論は,ポサコナゾールなどの抗真菌剤の製剤に価値があります.
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