アリルエーテルを2-アシリミダゾールで非対称的にC-Hアルキル化
Tian-Ci Wang1, Lian-Feng Fan1, Yang Shen1
1Hefei National Laboratory for Physical Sciences at the Microscale and Department of Chemistry , University of Science and Technology of China , Hefei 230026 , China.
Journal of the American Chemical Society
|June 29, 2019
まとめ
キラル・フォスフォラミドイト-パラジウム触媒は,アリルエーサーの非対称的なアリルC−Hアルキル化を可能にします. この方法は,高いエナチオ選択性を持つ機能化されたキラル-2-アシリミダゾールを効率的に生成します.
科学分野:
- 有機化学
- カタリシス
- 非対称合成
背景:
- アリルC-H機能化は有機合成における重要な変換である.
- アリルアルキル化のためのエナンチオセレクティブの方法の開発は,依然として重要な課題です.
研究 の 目的:
- クイラル触媒を用いてアリルエーサーの非対称性C-Hアルキル化を確立する.
- 機能化されたキラル-2-アシリミダゾールを合成する.
主な方法:
- パラジウム触媒を用いたキラル・フォスフォラミドイト・リガンドを使用した.
- 様々なアリルエーテルを非対称なアリルC−Hアルキル化した.
- 顕微鏡法とキラルクロマトグラフィを用いて,得られたキラル-2-アシリミダゾールを特徴づけた.
主要な成果:
- 機能化されたキラル-2-アシリミダゾールの 適度から高い産出率を達成した.
- アルキル化製品に高いレベルのエナチオ選択性があることが示された.
- タチキニン受容体アンタゴニストの前駆体合成に プロトコルが成功しました
結論:
- 非対称性アリルC−Hアルキル化のための新しく効率的な触媒システムを開発した.
- 方法論は価値あるキラル・イミダゾールの構成要素へのアクセスを提供します.
- このプロトコルは,医薬品の中間物質を含む複雑な分子合成に適しています.
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