The Chan-Lam-type synthesis of thioimidazolium salts for thiol-(hetero)arene conjugation
The design of stable and variable aryl linkers for conjugating drug moieties to the metabolism-related thiols is of importance in drug discovery. We disclosed that thioimidazolium groups are unique scaffolds for the thiol-(hetero)arene conjugation under mild conditions. The drug bound thioimidazolium salts, which are easily accessible via a copper-mediated Chan-Lam process in gram-scale, could be successfully applied to the late-stage coupling of bioactive thiols to construct a broad array of drug-like molecules.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2024 |
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| Erschienen: |
2024 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:60 |
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| Enthalten in: |
Chemical communications (Cambridge, England) - 60(2024), 35 vom: 25. Apr., Seite 4675-4678 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Li, Yue [VerfasserIn] |
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| Links: |
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| Themen: |
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| Anmerkungen: |
Date Revised 25.04.2024 published: Electronic Citation Status PubMed-not-MEDLINE |
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| doi: |
10.1039/d4cc00704b |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM370810155 |
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| 520 | |a The design of stable and variable aryl linkers for conjugating drug moieties to the metabolism-related thiols is of importance in drug discovery. We disclosed that thioimidazolium groups are unique scaffolds for the thiol-(hetero)arene conjugation under mild conditions. The drug bound thioimidazolium salts, which are easily accessible via a copper-mediated Chan-Lam process in gram-scale, could be successfully applied to the late-stage coupling of bioactive thiols to construct a broad array of drug-like molecules | ||
| 650 | 4 | |a Journal Article | |
| 700 | 1 | |a Han, Dongchang |e verfasserin |4 aut | |
| 700 | 1 | |a Luo, Zhibin |e verfasserin |4 aut | |
| 700 | 1 | |a Lv, Xiaomeng |e verfasserin |4 aut | |
| 700 | 1 | |a Liu, Bin |e verfasserin |4 aut | |
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