Divergent unprotected peptide macrocyclisation by palladium-mediated cysteine arylation† †Electronic supplementary information (ESI) available. See DOI: 10.1039/c6sc05454d Click here for additional data file.
نویسندگان
چکیده
1. General Experimental Details 2. Oxidative Addition Complexes and Synthetic Procedures 3. Peptide Synthesis and LC-MS Characterisation 4. Macrocyclisation Reactions and LC-MS Characterisation 5. C-CA Protein Expression 6. BioLayer Interferometry Binding 7. Lipophilicity, Phospholipid Affinity, Volume of Distribution, and Human Serum Albumin Binding Data 8. ICP-MS Analysis 9. References 10. NMR Spectra
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Taddol-based phosphoramidite ligands enable enantioselective palladium(0)-catalyzed C–H arylation of cyclopropanes. The cyclized products are obtained in high yields and enantioselectivities. The reported method provides efficient access to a broad range of synthetically attractive cyclopropyl containing dihydroquinolones and dihydroisoquinolones as well as allows for an efficient enantioselect...
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Synthesis of S peptides......................................................................................................................... 4 WT-S peptide – 8 ................................................................................................................................ 5 OX-S-Cys peptide – 2c ...................................................................................
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