A facile approach towards amidinophenylalanine derivatives as building blocks for the synthesis of non-natural peptides and peptidomimetics
The amidine function is extensively utilized as synthetic intermediate for structurally diverse heterocycles and as a core element in drugs and drug candidates. This study describes a facile and convenient approach for the highly efficient synthesis of amidinophenylalanine derivatives via the reduct...
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| Main Authors: | , , |
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| Format: | Article (Journal) |
| Language: | English |
| Published: |
22 August 2021
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| In: |
Tetrahedron letters
Year: 2021, Volume: 81, Pages: 1-7 |
| ISSN: | 1873-3581 |
| DOI: | 10.1016/j.tetlet.2021.153342 |
| Online Access: | Verlag, lizenzpflichtig, Volltext: https://doi.org/10.1016/j.tetlet.2021.153342 Verlag, lizenzpflichtig, Volltext: https://www.sciencedirect.com/science/article/pii/S0040403921006006 
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| Author Notes: | Somayeh Behrouz, Nikos Kühl, Christian D. Klein |
| Summary: | The amidine function is extensively utilized as synthetic intermediate for structurally diverse heterocycles and as a core element in drugs and drug candidates. This study describes a facile and convenient approach for the highly efficient synthesis of amidinophenylalanine derivatives via the reduction of amidoximophenylalanines in the presence of Ac2O/AcOH/Zn at room temperature. The described process is attractive for process and medicinal chemistry due to its facility, safety, low cost, applicability for hydrogenation-sensitive compounds, and efficiency. Using this method, amidinophenylalanine derivatives as building blocks for peptides were obtained in excellent yields. |
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| Item Description: | Gesehen am 26.11.2021 |
| Physical Description: | Online Resource |
| ISSN: | 1873-3581 |
| DOI: | 10.1016/j.tetlet.2021.153342 |