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Updated: Nov 12, 2025

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Cobalt-Catalyzed C(sp2)-H Carbonylation of Amino Acids Using Picolinamide as a Traceless Directing Group
Lukass Lukasevics1, Aleksandrs Cizikovs1, Liene Grigorjeva1
1Latvian Institute of Organic Synthesis, Aizkraukles Street 21, Riga LV-1006, Latvia.
Abstract:
Herein we report an efficient protocol for the C(sp2)-H carbonylation of amino acid derivatives based on an inexpensive cobalt(II) salt catalyst. Carbonylation was accomplished using picolinamide as a traceless directing group, CO (1 atm) as the carbonyl source, and Co(dpm)2 as the catalyst. A broad range of phenylalanine derivatives bearing diverse functional groups were tolerated. Moreover, the method can be successfully applied for the C(sp2)-H carbonylation of short peptides thereby allowing access for peptide late-stage carbonylation.
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