Visible Light-Driven Benzylic C(sp 3 )–H Carboxylation Enables Synthesis of 13 C-Labeled (±)-α-Amino Acids with 13 C-Formate

作者：Hao Zhang, Xiaoyang Wu, Panpan Gao, Li Zhu, Shangde Ai, Yang-Tong Ma, Zhuofan Jian, Gang Li · 发表于：Organic Letters · 年份：2025 · DOI：10.1021/acs.orglett.5c03238 · 被引用次数：10 · 研究领域：Carbon dioxide utilization in catalysis、Chemical Reactions and Isotopes、Fluorine in Organic Chemistry

13 C-labeled α-amino acids are important molecules in biological studies and drug development. Cost-effective synthesis of α-amino acids with a high level of 13 C incorporation under mild conditions remains limited. Herein, we report the development of a benzylic C(sp 3 )–H carboxylation method to prepare highly 13 C-labeled α-amino acids, i.e., arylglycines, using near-stoichiometric and user-friendly sodium 13 C-formate. The sequential reaction pathway of in situ 13 C-carbon dioxide (CO 2 ) generation followed by C–H carboxylation via 1,2-HAT was suggested by mechanistic studies.