スタイレンの非対称銅触媒型分子間アミノアリレーション:光学的2,2-ダイアリエチアミンへの効率的なアクセス
Dinghai Wang1, Lianqian Wu1, Fei Wang1
1State Key Laboratory of Organometallic Chemistry, Shanghai Institute of Organic Chemistry, University of Chinese Academy of Sciences, Chinese Academy of Sciences , 345 Lingling Road, Shanghai 200032, China.
Journal of the American Chemical Society
|May 5, 2017
まとめ
研究者は,アルケンのエナチオ選択的アミノアリレーションのための新しい銅触媒方法を開発した. このアプローチは,薬剤発見のための高光学純度の有価な2,2-ダイアリエチラミンを効率的に合成します.
科学分野:
- 有機化学
- カタリシス
- 合成方法論
背景:
- 2,2-ダイアリエチラミンのエナンチオセレクティブ合成は,複雑な生物活性分子へのアクセスに不可欠です.
- 既存の方法はしばしば厳しい条件を必要とし,広範囲の基板が欠けています.
研究 の 目的:
- アルケンの新種の銅触媒によるエナチオ選択的分子間アミノアリレーションを開発する.
- 新しいN-fluoro-N-alkylsulfonamideをアミンの源として使用する.
主な方法:
- N-フッ素-N-アルキルスルフォナミドとのアルケンの銅 ((I) 触媒反応.
- アミノラジカルの生成とその後のスタイレンへの添加
- チラルのL*Cu(II) Ar複合体とのエナントオセレクティブカップリング.
主要な成果:
- 様々な光学的2,2-ダイアリエチラミンの 効率的な合成
- スタイロンのアミノアリレーションで得られた高いエナンチオ選択性.
- バイオアクティブ分子のためのシントンとして製品の有用性を証明した.
結論:
- アルケンのエナチオ選択的アミノアリレーションのための新しい効率的な銅触媒法が確立されています.
- 開発された方法論は,医薬品合成のための貴重なキラル中間物質へのアクセスを提供します.
- N-fluoro-N-alkylsulfonamidesの使用は,根基ベースのC-N結合形成のための新しい経路を提供します.
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