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医薬化学におけるファーマコフォアとしてのフタラジン-1(2H)-1コアの合成における最近の進歩
Recent advances in the synthesis of phthalazin-1(2H)-one core as a relevant pharmacophore in medicinal chemistry.
PMID: 30388463 DOI: 10.1016/j.ejmech.2018.10.047.
抄録
フタラジノン-1(2H)-1は、医薬化学を含む化学のいくつかの分野に関連する多種多様な合成分子に見られるジアザヘテロ二環である。創薬におけるフタルアジノンコアの汎用性の高さから、異なる置換基や官能基を持つ誘導体へのアクセスを得るための新しい合成法の探索が促進されてきた。このレビューでは、創薬プロセスに関連するフタルアジノン誘導体の合成における最新の進歩をハイライトし、[4+2] 2成分シクロ縮合に基づく古典的な方法論の修正と、[3+2+1] 3成分戦略に基づく新しい多成分アプローチを分析しています。
Phthalazin-1(2H)-one is a diazaheterobicycle found in a wide variety of synthetic molecules relevant to several branches of chemistry, including medicinal chemistry. The versatility of phthalazinone core in drug discovery has promoted the search for new synthetic methods to get access to differently substituted and functionalized derivatives. This review highlights the latest advances in synthesis of phthalazinone derivatives that have relevance to drug discovery processes, analyzing modifications of classical methodologies based on [4 + 2] two-component cyclocondensations as well as novel multicomponent approaches, mostly based on a [3 + 2+1] three-component strategy and very attractive not only because of its synthetic efficiency but also in the matter of environmental compatibility.
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