Journal
ORGANIC LETTERS
Volume 21, Issue 23, Pages 9381-9385Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.9b03607
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Funding
- National Natural Science Foundation of China [21502006]
- Beijing National Laboratory for Molecular Sciences
- Beijing Institute of Technology (BIT)
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Site-selective modification of chemically and biologically valuable alpha-amino acids and peptides is of great importance for biochemical study and pharmaceutical development. Few methods based on remote C(sp(3))-H functionalization of aliphatic side-chains of peptides has been disclosed in recent years. In this report, we developed a novel approach for gamma-C(sp(3))-H and gamma-/delta-C(sp(2))-H arylation of alpha-amino acids with alpha-hydrogen by native amine-directed C-H functionalization and further realized the gamma-C(sp(3))-H arylation of N-terminally unprotected peptides.
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