L. Hsin, E. Webster, G. Chrousos
Aug 1, 2000
Citations
0
Influential Citations
10
Citations
Journal
Journal of Labelled Compounds and Radiopharmaceuticals
Abstract
[3H](4-Fluorobutyl)propyl[2,5,6-trimethyl-7-(2,4,6-trimethylphenyl)pyrrolo[2,3-d]pyrimidin-4-yl]amine ([3H]LWH-154), a novel potent radiolabelled analog of the nonpeptide corticotropin-releasing hormone type 1 receptor (CRHR1) selective antagonist, butylethyl[2,5,6-trimethyl-7-(2,4,6-trimethylphenyl)pyrrolo[2,3-d]pyrimidin-4-yl]amine (antalarmin), was prepared for the development of positron emission tomography radiotracers for CRHR1 and evaluation as a nonpeptide radioligand for use in pharmacological studies. The precursor (4-fluorobutyl)prop-2-enyl[2,5,6-trimethyl-7-(2,4,6-trimethylphenyl)pyrrolo[2,3-d]pyrimidin-4-yl]amine (6) for tritiation was prepared in two steps from 3 in 76% total yield. Catalytic reduction of unsaturated fluoride 6 using tritium gas and palladium as catalyst gave [3H]LWH-154. After HPLC purification, [3H]LWH-154 of high radiochemical purity was obtained with a specific activity of 69 Ci/mmol. Copyright © 2000 John Wiley & Sons, Ltd.