非対称な触媒によって可能になった (-) -ヨルナミシンAと (-) -ヨルミシンの簡潔な全合成
Eric R Welin1, Aurapat Ngamnithiporn1, Max Klatte1
1Warren and Katharine Schlinger Laboratory of Chemistry and Chemical Engineering, California Institute of Technology, Pasadena, CA 91125, USA.
Science (New York, N.Y.)
|December 22, 2018
まとめ
研究者は,従来の方法ではなく,移行金属触媒を用いて,ビス-テトラヒドロイソキノリン (bis-THIQ) の天然製品のための新しい合成戦略を開発しました. このアプローチにより,がんと抗生物質の特性を有する多種多様な非自然な同類物質の合成と生成が可能です.
科学分野:
- 自然製品合成
- 有機化学
- 薬剤化学
背景:
- ビス-テトラヒドロイソキノリン (bis-THIQ) 化合物は強力な抗がんおよび抗生物質作用があることが知られている.
- 伝統的な合成経路は,バイオシンセティック経路を模倣して,電気的芳香化学を用いることが多い.
研究 の 目的:
- ビス-THIQ天然製品,ジョルナミシンAとジョルミシンのための新しい合成戦略を開発する.
- 現代の触媒を用いた生物模倣合成の代替案を探求する.
- 様々な非天然の類似品の製造を可能にします.
主な方法:
- 重要な結合形成の過程で 移行金属の触媒を用いた.
- ジョルナミシンAとジョルミシンを合成するための高効率の経路 (それぞれ15段階と16段階) を開発した.
- 伝統的なピクテ・スペングラー反応に基づく戦略から離れている.
主要な成果:
- ジョルナミシンAとジョルミシンを 新型触媒手法で合成した
- 合成過程で高い効率を達成した.
- バイオミミクリーから抜け出す戦略を示しました
結論:
- 新しい移行金属触媒戦略は,bis-THIQ天然製品への効率的な経路を提供します.
- このアプローチは,より広い範囲の非自然類の合成を容易にする.
- この発見は,bis-THIQ基の新たな治療薬の探求への道を開きます.
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