Expedient and Divergent Synthesis of Unnatural Peptides through Cobalt-Catalyzed Diastereoselective Umpolung Hydrogenation

X. Qin and Q. Ren show a diastereo- and regioselective Co-catalyzed umpolung hydrogenation to create unnatural peptides.

In recent years, there has been a growing interest in harnessing peptides as therapeutic agents for treating various diseases. Currently, the global market boasts more than 80 commercially available peptide drugs, with approximately 170 in diverse stages of clinical trials and an additional 500 undergoing preclinical studies. Unnatural peptides with amino acid residues beyond the 20 canonical amino acids have demonstrated superior proteolytic stability, bioactivity and pharmacokinetics compared with their natural counterparts. Among them, noncanonical aryl alanines are notably prevalent in pharmaceuticals due to their exceptional versatilities.
Here, the group of Professors Xurong Qin and Qiao Ren at Southwest University (P. R. of China) developed a diastereo- and regioselective Co-catalyzed umpolung hydrogenation for the divergent and expedient synthesis of unnatural aryl alanine peptides. They disclosed that commercially available acetic acid and methanol can serve as safe and cheap hydrogen sources, avoiding the safety hazards associated with the storage and usage of high-pressure hydrogen gas.

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