{"title":"On-line [11C]methylation using [11C]methyl iodide for the automated preparation of 11C-radiopharmaceuticals","authors":"Ren Iwata , Claudio Pascali , Mitsuaki Yuasa , Kazuhiko Yanai , Toshihiro Takahashi , Tatsuo Ido","doi":"10.1016/0883-2889(92)90048-J","DOIUrl":null,"url":null,"abstract":"<div><p>A novel method for the efficient preparation of <sup>11</sup>C-radiopharmaceuticals by on-line [<sup>11</sup>C]methylation using [<sup>11</sup>C]methyl iodide has been developed and applied to a rapid, convenient automated system. [<sup>11</sup>C]Methyl iodide is first trapped in a short column, containing an adsorber and coated substrate, which is connected to an HPLC injector. DMF is then introduced. Alternatively the substrate is added with the DMF. A whole reaction mixture can be easily injected onto an HPLC column for purification by switching the injector valve immediately after the reaction. Thus, radiochemical yields in the preparation of <sup>11</sup>C-labeled doxepin, benztropine, cyproheptadine and <em>N</em>-methylspiperone have been improved remarkably and the synthetic procedure simplified.</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":"1992-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/0883-2889(92)90048-J","citationCount":"30","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/088328899290048J","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 30
Abstract
A novel method for the efficient preparation of 11C-radiopharmaceuticals by on-line [11C]methylation using [11C]methyl iodide has been developed and applied to a rapid, convenient automated system. [11C]Methyl iodide is first trapped in a short column, containing an adsorber and coated substrate, which is connected to an HPLC injector. DMF is then introduced. Alternatively the substrate is added with the DMF. A whole reaction mixture can be easily injected onto an HPLC column for purification by switching the injector valve immediately after the reaction. Thus, radiochemical yields in the preparation of 11C-labeled doxepin, benztropine, cyproheptadine and N-methylspiperone have been improved remarkably and the synthetic procedure simplified.