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Issue 10, 2011
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Radical arylation of tyrosine and its application in the synthesis of a highly selective neurotensin receptor 2 ligand

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Abstract

A small library of Fmoc-protected 3-arylated tyrosines was created by radical arylation. The new building blocks were successfully applied in the synthesis of two novel neurotensin receptor ligands. Both isomers showed high affinity for the human NTS2 receptor with Ki values in the nanomolar range. Interestingly, subtype selectivity strongly depends on the configuration of the peptide in position 11. Isomer (11R)-3 displayed an excellent preference for NTS2 compared to NTS1.

Graphical abstract: Radical arylation of tyrosine and its application in the synthesis of a highly selective neurotensin receptor 2 ligand

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Publication details

The article was received on 23 Feb 2011, accepted on 14 Mar 2011 and first published on 14 Mar 2011


Article type: Paper
DOI: 10.1039/C1OB05292F
Citation: Org. Biomol. Chem., 2011,9, 3746-3752
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    Radical arylation of tyrosine and its application in the synthesis of a highly selective neurotensin receptor 2 ligand

    G. Pratsch, J. F. Unfried, J. Einsiedel, M. Plomer, H. Hübner, P. Gmeiner and M. R. Heinrich, Org. Biomol. Chem., 2011, 9, 3746
    DOI: 10.1039/C1OB05292F

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