1310056-01-9Relevant academic research and scientific papers
Radical arylation of tyrosine and its application in the synthesis of a highly selective neurotensin receptor 2 ligand
Pratsch, Gerald,Unfried, Johannes F.,Einsiedel, Juergen,Plomer, Manuel,Huebner, Harald,Gmeiner, Peter,Heinrich, Markus R.
, p. 3746 - 3752 (2011)
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.
