Tjibbe J. De Groot, Philip H. Elsinga, Gerben M. Visser, Willem Vaalburg
{"title":"1-[18F]fluoro-2-propanol p-toluenesulfonate: a synthon for the preparation of N-([18F]fluoroisopropyl)amines","authors":"Tjibbe J. De Groot, Philip H. Elsinga, Gerben M. Visser, Willem Vaalburg","doi":"10.1016/0883-2889(92)90005-Y","DOIUrl":null,"url":null,"abstract":"<div><p>The new radiochemical synthon 1-[<sup>18</sup>F]fluoro-2-propanol <em>p</em>-toluenesulfonate <strong>2′a</strong> is prepared with a radiochemical yield of 45% [corrected for decay to beginning of synthesis (BOS), synthesis time 40 min]. This compound is used to prepare the [<sup>18</sup>F]fluoroisopropyl-alkylated derivatives of benzylamine and norephedrine with a yield of 7 and 2% respectively (BOS, synthesis time 90 min). This alkylation reaction with <strong>2′a</strong> gives a good perspective for the preparation of [<sup>18</sup>F]fluoro-labelled analogues of β<sub>1</sub>-adrenergic receptor binding ligands for PET.</p></div>","PeriodicalId":14288,"journal":{"name":"International Journal of Radiation Applications and Instrumentation. Part A. Applied Radiation and Isotopes","volume":"43 11","pages":"Pages 1335-1339"},"PeriodicalIF":0.0000,"publicationDate":"1992-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/0883-2889(92)90005-Y","citationCount":"7","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"International Journal of Radiation Applications and Instrumentation. Part A. Applied Radiation and Isotopes","FirstCategoryId":"1085","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/088328899290005Y","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 7
Abstract
The new radiochemical synthon 1-[18F]fluoro-2-propanol p-toluenesulfonate 2′a is prepared with a radiochemical yield of 45% [corrected for decay to beginning of synthesis (BOS), synthesis time 40 min]. This compound is used to prepare the [18F]fluoroisopropyl-alkylated derivatives of benzylamine and norephedrine with a yield of 7 and 2% respectively (BOS, synthesis time 90 min). This alkylation reaction with 2′a gives a good perspective for the preparation of [18F]fluoro-labelled analogues of β1-adrenergic receptor binding ligands for PET.