{"title":"用碳11标记阿芬太尼的研究","authors":"Anthony L. Feliu","doi":"10.1016/0883-2889(92)90061-I","DOIUrl":null,"url":null,"abstract":"<div><p>Methodology applicable to the synthesis of no-carrier-added [<em>O</em>-methyl-<sup>11</sup>C]alfentanil was developed. The sequence consisted of [<sup>11</sup>C]methylation and propionylation of <em>N</em>-aryl-4-(hydroxymethyl)-4-(<em>N</em>-<em>anilino</em>)-piperidines<strong>1a</strong> and <strong>1c</strong>, followed by the chemoselective hydrolysis of bulk byproducts to facilitate isolation of the NCA carbon-11-labeled product by prep-HPLC. All three steps could be performed without isolation of intermediates in a single reaction vessel.</p></div>","PeriodicalId":14288,"journal":{"name":"International Journal of Radiation Applications and Instrumentation. Part A. Applied Radiation and Isotopes","volume":"43 9","pages":"Pages 1159-1165"},"PeriodicalIF":0.0000,"publicationDate":"1992-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/0883-2889(92)90061-I","citationCount":"3","resultStr":"{\"title\":\"Studies to label alfentanil with carbon-11\",\"authors\":\"Anthony L. Feliu\",\"doi\":\"10.1016/0883-2889(92)90061-I\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><p>Methodology applicable to the synthesis of no-carrier-added [<em>O</em>-methyl-<sup>11</sup>C]alfentanil was developed. The sequence consisted of [<sup>11</sup>C]methylation and propionylation of <em>N</em>-aryl-4-(hydroxymethyl)-4-(<em>N</em>-<em>anilino</em>)-piperidines<strong>1a</strong> and <strong>1c</strong>, followed by the chemoselective hydrolysis of bulk byproducts to facilitate isolation of the NCA carbon-11-labeled product by prep-HPLC. All three steps could be performed without isolation of intermediates in a single reaction vessel.</p></div>\",\"PeriodicalId\":14288,\"journal\":{\"name\":\"International Journal of Radiation Applications and Instrumentation. Part A. Applied Radiation and Isotopes\",\"volume\":\"43 9\",\"pages\":\"Pages 1159-1165\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"1992-09-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://sci-hub-pdf.com/10.1016/0883-2889(92)90061-I\",\"citationCount\":\"3\",\"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/088328899290061I\",\"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/088328899290061I","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
Methodology applicable to the synthesis of no-carrier-added [O-methyl-11C]alfentanil was developed. The sequence consisted of [11C]methylation and propionylation of N-aryl-4-(hydroxymethyl)-4-(N-anilino)-piperidines1a and 1c, followed by the chemoselective hydrolysis of bulk byproducts to facilitate isolation of the NCA carbon-11-labeled product by prep-HPLC. All three steps could be performed without isolation of intermediates in a single reaction vessel.
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