化学
光催化
衍生化
组合化学
催化作用
有机化学
分子
反应条件
羧酸
选择性
激进的
化学合成
有机合成
作者
Lin Chen,Ming-Qiao Leng,Chuan-Xi Nie,Jun-Ze Zuo,Xiao-Fei Xu,Long-Fu Wang,Li‐Li Liao,Jian‐Heng Ye,Da‐Gang Yu
摘要
β-Amino acids represent vital structural motifs in bioactive molecules, finding broad utility in organic synthesis, pharmaceuticals, and materials science. Although CO2 has been widely exploited as a C1 carboxyl source for the synthesis of carboxylic acids, the direct aminocarboxylation of unactivated alkenes with CO2 to afford β-amino acids remains largely unexplored and faces formidable challenges. Herein, we report the first photocatalytic aminocarboxylation of unactivated alkenes and heteroarenes using CO2 as the ideal one-carbon feedstock, enabling the efficient synthesis of diverse valuable β-amino acid derivatives. This innovative strategy relies on the sequential installation of a CO2 radical anion and a nitrogen-centered radical (NCR) across alkenes. Specifically, commercially available acyl hydrazides serve as key NCR precursors to form captodative hydrazyl radicals, thereby facilitating selective radical-radical cross-coupling governed by the persistent radical effect (PRE). This methodology readily accommodates simple and abundant chemical feedstocks, ranging from unactivated alkenes (including ethylene) to heteroarenes and activated alkenes. Characterized by low catalyst loading, high selectivity, and good functional-group tolerance, this protocol enables the late-stage derivatization of products into bioactive molecules and various heterocycles.
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