N-ジフローロメチルチオフタリミド:ジフローロメチルチオ化のための耐久性のある電性反応剤
Dianhu Zhu1, Yang Gu1, Long Lu1
1Key Laboratory of Organofluorine Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences , 345 Lingling Road, Shanghai 200032, People's Republic of China.
Journal of the American Chemical Society
|July 17, 2015
まとめ
新しい反応剤であるN-difluoromethylthiophthalimideは,多様な核愛体の効率的な電離性二酸化メチルチオレーションを可能にします. この方法は,軽度な条件下で二酸化メチルチオ群を導入するための新しい経路を提供します.
科学分野:
- 有機化学
- 合成化学
- 薬剤化学
背景:
- ディフルオロメチルチオ (SCF2H) グループは,薬剤発見における重要な薬剤である.
- SCF2H群を導入するための効率的で穏やかな方法の開発は,医薬品化学にとって極めて重要です.
研究 の 目的:
- 新しい,ユーザーフレンドリーな電離型二酸化メチルチオレート剤を開発する.
- SCF2Hを含む化合物の合成のための開発された反応剤の広範な適用性を実証する.
主な方法:
- N-difluoromethylthiophthalimideとTMSCF2Hから4つのステップで合成する
- ボロン酸,アルキン酸,アミン酸,チオール酸,β-ケトエスター酸,オキシンドール酸,ヘテロアレン酸を含む様々なヌクレオフィルと電気性二酸化チオル化反応.
主要な成果:
- 簡単に入手可能な原料からN-difluoromethylthiophthalimide (3) を成功して合成した.
- 広範囲にわたる核愛者を含む二酸化メチルチオラ化のための基板の範囲を示した.
- 軽度の反応条件下で二酸化メチルチオラ化が達成される.
結論:
- N-difluoromethylthiophthalimide (3) は,強力で汎用的な電離型二酸化メチルチオレート剤である.
- 開発された方法は,価値ある二酸化メチルチオを含む分子の合成のための効率的な経路を提供します.
- この反応剤は,SCF2H分子が様々な有機構造に組み込まれるのを容易にする.
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