B. Czeskis
Jun 1, 1998
Citations
0
Influential Citations
4
Citations
Journal
Journal of Labelled Compounds and Radiopharmaceuticals
Abstract
The 3-[14C]-isotopomer of (S)-1-(1H-indol-4-yloxy)-3-[4-(3-methyoxyphenyl)-4-hydroxypiperidin-1-yl]-propan-2-ol (LY333068), a 5HT1A antagonist, was prepared in 10 steps and 8.2% radiochemical yield from (L)-serine-[3-14C]. Deamination, esterification, and protection of the resulting diol gave methyl (R)-2,2-dimenthyl-1,3-dioxolane-4-carboxylate-[3-14C], as a chiral and radiolabeled building block, which then was subsequently coupled with 4-hydroxyindole and 4-(3-methoxyphenyl)-4-hydroxypiperidine to give the titled product with 99.4% radiochemical purity. © 1998 John Wiley & Sons, Ltd.