Synthesis of carbon-11 labeled diprenorphine: A radioligand for positron emission tomographic studies of opiate receptors

作者：John R. Lever, Robert F. Dannals, Alan A. Wilson, Hayden T. Ravert, Henry N. Wagner · 发表于：Tetrahedron Letters · 年份：1987 · DOI：10.1016/s0040-4039(01)83849-1 · 被引用次数：46 · 研究领域：Pharmacological Receptor Mechanisms and Effects、Neuropeptides and Animal Physiology、Alkaloids: synthesis and pharmacology

Selective alkylation of 3-(O-t-butyldimethylsilyl)-6-(O-desmethyl)-diprenorphine with [11C]-methyl iodide followed by desilylation affords [11C]-dipronorphine labeled at the 6-methoxy position in 10% yield with a specific activity of 1740 mCi/μmol at the end of a 30 minute synthesis.