期刊
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
卷 55, 期 42, 页码 13174-13179出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.201607657
关键词
Boc-SPPS; cyclic peptide; peptide ligation; peptide thioester; post-translational modification
资金
- Francis Crick Institute from cancer research UK [FC001070, FC001156]
- UK Medical Research Council [FC001070, FC001156]
- Wellcome Trust [FC001070, FC001156]
- European Research Council Advanced Grant RASTARGET
- MRC [MC_U117584228, MC_U117592730] Funding Source: UKRI
- Cancer Research UK [15680] Funding Source: researchfish
- Medical Research Council [MC_U117584228, U117531954, 1254166] Funding Source: researchfish
- The Francis Crick Institute [10070, 10156, 10074, 10071] Funding Source: researchfish
We have developed a convenient method for the direct synthesis of peptide thioesters, versatile intermediates for peptide ligation and cyclic peptide synthesis. The technology uses a modified Boc SPPS strategy that avoids the use of anhydrous HF. Boc in situ neutralization protocols are used in combination with Merrifield hydroxymethyl resin and TFA/TMSBr cleavage. Avoiding HF extends the scope of Boc SPPS to post-translational modifications that are compatible with the milder cleavage conditions, demonstrated here with the synthesis of the phosphorylated protein CHK2. Peptide thioesters give easy, direct, access to cyclic peptides, illustrated by the synthesis of cyclorasin, a KRAS inhibitor.
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