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

Pratsch G, Unfried JF, Einsiedel J, Plomer M, Hübner H, Gmeiner P, Heinrich M (2011)

Publication Language: English

Publication Type: Journal article, Original article

Publication year: 2011

Journal

Original Authors: Pratsch G., Unfried J.F., Einsiedel J., Plomer M., Hubner H., Gmeiner P., Heinrich M.R.

Publisher: Royal Society of Chemistry

Book Volume: 9

Pages Range: 3746-3752

Journal Issue: 10

DOI: 10.1039/c1ob05292f

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 K 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. © 2011 The Royal Society of Chemistry.

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APA:

Pratsch, G., Unfried, J.F., Einsiedel, J., Plomer, M., Hübner, H., Gmeiner, P., & Heinrich, M. (2011). Radical arylation of tyrosine and its application in the synthesis of a highly selective neurotensin receptor 2 ligand. Organic & Biomolecular Chemistry, 9(10), 3746-3752. https://doi.org/10.1039/c1ob05292f

MLA:

Pratsch, Gerald, et al. "Radical arylation of tyrosine and its application in the synthesis of a highly selective neurotensin receptor 2 ligand." Organic & Biomolecular Chemistry 9.10 (2011): 3746-3752.

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