Synfacts 2023; 19(06): 0629
DOI: 10.1055/s-0042-1752676
Peptide Chemistry

Synthesis of Unnatural Peptides by Deaminative Reductive Cross-Coupling Reactions

Rezensent(en):
Hisashi Yamamoto
,
An Wu
Twitty JC, Hong Y, Garcia B, Tsang S, Liao J, Schultz DM, Hanisak J, Zultanski SL, Dion A, *, Kalyani D, *, Watson MP. * Merck & Co., Rahway and Kenilworth and University of Delaware, Newark, USA
Diversifying Amino Acids and Peptides via Deaminative Reductive Cross-Couplings Leveraging High-Throughput Experimentation.

J. Am. Chem. Soc. 2023;
145: 5684-5695
DOI: 10.1021/jacs.2c11451.
 

Significance

Modification of peptides on the side chain of amino acid residues is very important in drug discovery and medicinal chemistry. The authors reported a deaminative reductive cross-coupling strategy to arylate the amino acid residues.


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Comment

Various unnatural peptides are synthesized in moderate to good yields. The arylation of their side chains resulted efficiently from preformed amino acid pyridinium salts by using a ­nickel(II) catalyst.


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Publikationsverlauf

Artikel online veröffentlicht:
11. Mai 2023

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