ヘテロアリルハリドとヘテロアリルトリフラートから一般的な多金属クロスウルマンビヘテロアリル合成
Kai Kang1, Nathan L Loud1, Tarah A DiBenedetto2
1University of Wisconsin-Madison, Madison, Wisconsin 53706, United States.
Journal of the American Chemical Society
|December 17, 2021
まとめ
ビヘテロアリルの合成は,新しいNiとPd触媒の多金属クロスウルマンカップリングにより容易になりました. この方法は,様々なヘテロアリルハリドとトリフラートを効率的に結合し,多様な用途のための一般的なアプローチを提供します.
科学分野:
- 有機化学
- キャタリシス
- 薬剤化学
背景:
- ビヘテロアリルは医学と材料科学において極めて重要です.
- ビヘテロアリル合成のための既存のクロスカップリング方法には課題があります.
研究 の 目的:
- ビヘテロアリルを合成するための一般的で効率的な方法を開発する.
- 現在のクロスカップリング戦略の限界を克服する.
主な方法:
- ニッケル (Ni) とパラジウム (Pd) で触媒化されたマルチメタリッククロスウルマンカップリングを使用しています.
- 基質としてヘテロアリルハリド (ブロミド,塩化物) とトリフラートを使用しています.
- 多種多様な5基,6基,溶融ヘテロアリル系を試験した.
主要な成果:
- 平均63%±17%のビヘテロアリルのサンプルを成功して合成した.
- 様々なヘテロアリルハライドとトリフラートを含む,広範な基板の範囲を示した.
- 96種類の製品で90%以上のヒット率を達成しました. 96個の穴のプレート形式です.
結論:
- 開発されたNiとPd触媒のクロス・ウルマン結合は,ビヘテロアリル合成の汎用的で一般的なアプローチを提供します.
- この方法は,高通量スクリーニングと迅速な最適化が可能で,発見を加速します.
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