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Article Abstract
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 C incorporation under mild conditions remains limited. Herein, we report the development of a benzylic C(sp)-H carboxylation method to prepare highly C-labeled α-amino acids, i.e., arylglycines, using near-stoichiometric and user-friendly sodium C-formate. The sequential reaction pathway of in situ C-carbon dioxide (CO) generation followed by C-H carboxylation via 1,2-HAT was suggested by mechanistic studies.
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| http://dx.doi.org/10.1021/acs.orglett.5c03238 | DOI Listing |
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