Efficient synthesis of Azabicyclo[3.1.1]heptanes via Strain-release Cycloadditions of Bicyclo[1.1.0]butanes

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  • Tagami Takuma
    Graduate School of Pharmaceutical Sciences, Kyushu University

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  • ビシクロブタン骨格の開裂を起点とする高効率アザビシクロ[3.1.1]ヘプタン合成

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<p>Azabicyclo[3.1.1]heptanes are recognized as bioisosteres of the meta-substituted pyridine scaffold, as their bridgehead substitution mimics the arrangement of substituents on the meta-substituted pyridine. However, the synthesis of azabicyclo[3.1.1]heptanes remains underdeveloped. This mini-review highlights recent advances in their synthesis through strain-release cycloadditions of bicyclo[1.1.0]butanes.</p>

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