Tjibbe J. De Groot, Philip H. Elsinga, Gerben M. Visser, Willem Vaalburg
{"title":"1-[18F]氟-2-丙醇对甲苯磺酸:用于制备N-([18F]氟异丙基)胺的合成物","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":null,"pages":null},"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":"{\"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\":null,\"pages\":null},\"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}","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}
1-[18F]fluoro-2-propanol p-toluenesulfonate: a synthon for the preparation of N-([18F]fluoroisopropyl)amines
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.