プロスタグランジンPGF2αのステレオ制御された有機触媒合成が7段階で行われます
Graeme Coulthard1, William Erb, Varinder K Aggarwal
1School of Chemistry, University of Bristol, Cantock’s Close, Bristol BS8 1TS, UK.
Nature
|August 17, 2012
まとめ
研究者は,複雑なホルモンであるプロスタグランジンPGF2αの簡潔な合成を開発しました. この新しい方法は,有機触媒化されたアルドールカスケードを使用して,より手頃な価格のプロスタグランジン薬のステップと浪費を大幅に削減します.
科学分野:
- 有機化学 オーガニック・ケミストリー
- 薬用化学 薬用化学について
- 合成化学 合成化学とは
背景:
- プロスタグランジンは,重要な生理学的機能を調節するホルモンのような重要な化合物です.
- 彼らの複雑な構造は,医薬品の重要性にもかかわらず,合成のための挑戦的なターゲットにします.
- 既存の合成経路は長く,非効率で,大量の廃棄物を生み出しています.
研究 の 目的:
- 複雑なプロスタグランジン,特にPGF2αのより簡潔で効率的な合成を開発する.
- プロスタグランディン合成におけるステレオ化学の制御を改善するために.
- プロスタグランジンベースの薬剤の製造コストと環境への影響を削減するためです.
主な方法:
- 新規の債券解約戦略を活用した.
- 重要なアルドールカスケード反応のプロリン有機触媒を用いた.
- 単一のステップで高エナティオメール過量でバイサイクルエナル中間物質を合成しました.
主要な成果:
- プロスタグランディンPGF2αの非常に簡潔な合成を達成しました.
- 相対的および絶対的立体化学に対する優れた制御を示した.
- 98%のエナティオメリ余剰を持つバイサイクルエナル中間物質を生成した.
結論:
- 新しい合成アプローチは,ステップの数と関連するコストと浪費を大幅に削減します.
- この方法は,既存のプロスタグランジン製薬のより手頃な価格での生産を容易にする.
- 新種のプロスタグランジンアナログの治療の可能性を迅速に探求することを可能にします.
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