Mohammad Namavari , Allyson Bishop , N. Satyamurthy , Gerald Bida , Jorge R. Barrio
{"title":"[18F]F2和[18F]CH3COOF的区域选择性放射性氟去乙酰化:6-[18F]氟-左旋多巴的高收率合成","authors":"Mohammad Namavari , Allyson Bishop , N. Satyamurthy , Gerald Bida , Jorge R. Barrio","doi":"10.1016/0883-2889(92)90217-3","DOIUrl":null,"url":null,"abstract":"<div><p>A protected 6-trimethylstannyl dopa derivative <strong>6</strong> has been synthesized for the first time as a precursor for the preparation of 6-[<sup>18</sup>F]fluoro-<span>l</span>-dopa. The tin derivative <strong>6</strong> readily reacted with electrophilic radiofluorinating agents such as [<sup>18</sup>F]F<sub>2</sub> and [<sup>18</sup>F]AcOF. The [<sup>18</sup>F]fluoro intermediate <strong>7</strong> was easily hydrolyzed with HBr and the product 6-[<sup>18</sup>F]fluoro-<span>l</span>-dopa was isolated after HPLC purification in a maximum radiochemical yield of 25%, ready for human use. The various intermediates, the stannyl precursor <strong>6</strong> and the final product (after <sup>18</sup>F decay) were all fully characterized by <sup>1</sup>H, <sup>13</sup>C, <sup>19</sup>F and <sup>119</sup>Sn NMR as well as high resolution mass spectroscopy.</p></div>","PeriodicalId":14288,"journal":{"name":"International Journal of Radiation Applications and Instrumentation. Part A. Applied Radiation and Isotopes","volume":"43 8","pages":"Pages 989-996"},"PeriodicalIF":0.0000,"publicationDate":"1992-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/0883-2889(92)90217-3","citationCount":"202","resultStr":"{\"title\":\"Regioselective radiofluorodestannylation with [18F]F2 and [18F]CH3COOF: A high yield synthesis of 6-[18F]fluoro-l-dopa\",\"authors\":\"Mohammad Namavari , Allyson Bishop , N. Satyamurthy , Gerald Bida , Jorge R. Barrio\",\"doi\":\"10.1016/0883-2889(92)90217-3\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><p>A protected 6-trimethylstannyl dopa derivative <strong>6</strong> has been synthesized for the first time as a precursor for the preparation of 6-[<sup>18</sup>F]fluoro-<span>l</span>-dopa. The tin derivative <strong>6</strong> readily reacted with electrophilic radiofluorinating agents such as [<sup>18</sup>F]F<sub>2</sub> and [<sup>18</sup>F]AcOF. The [<sup>18</sup>F]fluoro intermediate <strong>7</strong> was easily hydrolyzed with HBr and the product 6-[<sup>18</sup>F]fluoro-<span>l</span>-dopa was isolated after HPLC purification in a maximum radiochemical yield of 25%, ready for human use. The various intermediates, the stannyl precursor <strong>6</strong> and the final product (after <sup>18</sup>F decay) were all fully characterized by <sup>1</sup>H, <sup>13</sup>C, <sup>19</sup>F and <sup>119</sup>Sn NMR as well as high resolution mass spectroscopy.</p></div>\",\"PeriodicalId\":14288,\"journal\":{\"name\":\"International Journal of Radiation Applications and Instrumentation. Part A. Applied Radiation and Isotopes\",\"volume\":\"43 8\",\"pages\":\"Pages 989-996\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"1992-08-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://sci-hub-pdf.com/10.1016/0883-2889(92)90217-3\",\"citationCount\":\"202\",\"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/0883288992902173\",\"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/0883288992902173","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
Regioselective radiofluorodestannylation with [18F]F2 and [18F]CH3COOF: A high yield synthesis of 6-[18F]fluoro-l-dopa
A protected 6-trimethylstannyl dopa derivative 6 has been synthesized for the first time as a precursor for the preparation of 6-[18F]fluoro-l-dopa. The tin derivative 6 readily reacted with electrophilic radiofluorinating agents such as [18F]F2 and [18F]AcOF. The [18F]fluoro intermediate 7 was easily hydrolyzed with HBr and the product 6-[18F]fluoro-l-dopa was isolated after HPLC purification in a maximum radiochemical yield of 25%, ready for human use. The various intermediates, the stannyl precursor 6 and the final product (after 18F decay) were all fully characterized by 1H, 13C, 19F and 119Sn NMR as well as high resolution mass spectroscopy.
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