自由基途径的[1.1.1]螺桨烷官能化研究进展

doi:10.6023/cjoc202512007

摘要/Abstract

双环[1.1.1]戊烷(BCP)作为一种具有三维立体结构的桥环骨架,因其可作为苯环、叔丁基及炔烃等基团的生物电子等排体,已在药物化学领域得到广泛应用. 目前,通过[1.1.1]螺桨烷的自由基开环反应,已成为构建BCP衍生物最常用的策略. 传统[1.1.1]螺桨烷自由基官能团化反应的条件苛刻,官能团兼容性较差. 近年来,随着光催化在有机合成中的迅速发展,多种光催化的[1.1.1]螺桨烷官能团化策略相继被报道,并成功应用于药物分子的合成. 本文旨在对基于自由基途径的[1.1.1]螺桨烷官能化研究进展进行简要综述.

关键词: [1.1.1]螺桨烷, 双环[1.1.1]戊烷, 自由基, 光催化, 官能团化

Bicyclo[1.1.1]pentane (BCP), a three-dimensional bridged ring scaffold, has been widely used in medicinal chemistry due to its role as a bioisostere for groups such as benzene rings, tert-butyl groups, and alkynes. Currently, the radical ring-opening reaction of [1.1.1]propellane has become the most common strategy for constructing BCP derivatives. Traditional radical functionalization of [1.1.1]propellane typically requires harsh conditions and exhibits poor functional group compatibility. In recent years, with the rapid development of photocatalysis in organic synthesis, various photocatalytic functionalization of [1.1.1]propellane have been reported and successfully applied in the synthesis of drug molecules. This review aims to provide a concise overview of recent advances in radical-based functionalization of [1.1.1]propellane.

Key words: [1.1.1]propellane, bicyclo[1.1.1]pentane, radical, photocatalysis, functionalization

引用此文

董建洋, 薛东. 自由基途径的[1.1.1]螺桨烷官能化研究进展[J]. 有机化学, doi: 10.6023/cjoc202512007.

Dong Jianyang, Xue Dong. Research Progress on the Functionalization of [1.1.1]Propellane via Radical Pathways[J]. Chinese Journal of Organic Chemistry, doi: 10.6023/cjoc202512007.

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