Oxidative Functionalization of Peptide Side Chains Enabled by <i>N</i>-Chlorination of Amides
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- Nanjo Takeshi
- Graduate School of Pharmaceutical Sciences, Kyoto University
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- Matsumoto Ayaka
- Graduate School of Pharmaceutical Sciences, Kyoto University
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- Oshita Takuma
- Graduate School of Pharmaceutical Sciences, Kyoto University
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- Takemoto Yoshiji
- Graduate School of Pharmaceutical Sciences, Kyoto University
Bibliographic Information
- Other Title
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- アミドの<i>N</i>-クロロ化を経由するペプチド側鎖の酸化的官能基化
Abstract
Peptides containing unusual motifs such as abnormal amino acids and macrocyclic substructures have recently attracted much attention as a new modality in middle molecule drug discovery. Therefore, it is highly important to realize the methodology of chemical synthesis for a wide variety of such unusual peptide derivatives, and particularly, the direct modification of already-constructed peptide chains would enable the rapid supply of derivatives based on the parent peptide compound already on hand. However, most of the previous methods require reactive functional groups on the peptide side chains and the applicable substrates are limited in exchange for high site specificity of the transformation. In this account, we describe “an N-chloropeptide strategy” which enables the direct transformation for a wide variety of peptides regardless of their amino acid residues by utilizing amides of peptide main chains as a reactive point.
Journal
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- MEDCHEM NEWS
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MEDCHEM NEWS 34 (2), 93-96, 2024-05-01
The Pharmaceutical Society of Japan
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Details 詳細情報について
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- CRID
- 1390581468909753472
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- ISSN
- 24328626
- 24328618
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- Text Lang
- ja
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- Data Source
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- JaLC
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- Abstract License Flag
- Disallowed