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Synthesis of [3H]-labelled 4-[Ethyl[2,5,6-trimethyl-7-(2,4,6-trimethylphenyl)pyrrolo[2,3-d]pyrimidin-4-yl]amino]-2,3-[3H]-butan-1-ol: a high affinity radioligand for the corticotropin-releasing hormone type 1 receptor

✍ Scribed by Anne-Cécile Hiebel; John S. Partilla; Richard B. Rothman; Arthur E. Jacobson; Kenner C. Rice

Publisher: John Wiley and Sons
Year: 2006
Tongue: French
Weight: 117 KB
Volume: 49
Category: Article
ISSN: 0022-2135
DOI: 10.1002/jlcr.1082

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✦ Synopsis

3 H]-Labelled 4- [ethyl[2,5,6-trimethyl-7-(2,4,6-trimethylphenyl)pyrrolo[2,3-d]pyrimidin-4-yl]amino]-2,3-[ 3 H]-butan-1-ol (3b) was prepared as a novel non-peptidic radiolabelled high affinity antagonist of the corticotropin-releasing hormone type 1 receptor (CRHR 1 ) that could be useful as a more stable and receptor-selective alternative to the radiolabelled peptides now used to label the CRHR 1 receptor for displacement studies in cell-based binding assays. The precursor (Z)-4- [ethyl[2,5,6trimethyl-7-(2,4,6-trimethylphenyl)pyrrolo[2,3-d]pyrimidin-4-yl]amino]but-2-en-1-ol (2) was reduced with tritium gas using palladium as the catalyst. After HPLC purification 3b was obtained with a specific activity of 35 Ci/mmol in high radiochemical purity (>97%).

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