Citation: Xiao Tang, Erik V. Van der Eycken, Liangliang Song. Transition metal-catalyzed C-H activation/annulation for the construction of unnatural amino acids and peptides[J]. Chinese Chemical Letters, ;2026, 37(2): 111678. doi: 10.1016/j.cclet.2025.111678 shu

Transition metal-catalyzed C-H activation/annulation for the construction of unnatural amino acids and peptides

Xiao Tang ^a ,
Erik V. Van der Eycken ^{b, c, *,} ,
Liangliang Song ^{d, *,}

a.
College of Science, Nanjing Forestry University, Nanjing 210037, China
b.
Laboratory for Organic & Microwave-Assisted Chemistry (LOMAC), Department of Chemistry, University of Leuven (KU Leuven), Celestijnenlaan 200F, Leuven B-3001, Belgium
c.
Peoples’ Friendship University of Russia (RUDN University), Moscow 117198, Russia
d.
Jiangsu Provincial Key Lab for the Chemistry and Utilization of Agro-Forest Biomass, Jiangsu Co-Innovation Center of Efficient Processing and Utilization of Forest Resources, Jiangsu Key Lab of Biomass-Based Green Fuels and Chemicals, International Innovation Center for Forest Chemicals and Materials, College of Chemical Engineering, Nanjing Forestry University, Nanjing 210037, China

erik.vandereycken@kuleuven.be

liangliangsong@njfu.edu.cn

Received Date: 6 April 2025
Revised Date: 25 July 2025
Accepted Date: 6 August 2025
Available Online: 7 August 2025

Figures(27)

Peptides play important roles in chemistry, medicinal chemistry and life science, due to their high efficiency and specificity, unusual biological and therapeutic properties. As naturally occurring peptides often face with their intrinsic limitations including metabolic instability and low membrane permeability, the strategies for synthesizing unnatural amino acids and peptides are explored. Among the methods for modifying amino acids and peptides, chemo- and site-selective approaches are preferred because of the ability to fine-tuning structural features. Recently, transition metal-catalyzed C-H activation has been employed for the functionalization of amino acids and peptides. Through domino C-H activation/annulation, a series of structurally complex and diverse amino acids and peptides is constructed. This review highlights recent advances in the synthesis of unnatural amino acids and peptides via transition metal-catalyzed C-H activation/annulation.
- Amino acid,
- Peptide,
- Transition metal,
- C-H activation,
- Annulation
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