{"title":"捕获溶剂法合成匹兹堡化合物B的优化","authors":"G. Clemente, V. Alves, A. Abrunhosa","doi":"10.1109/ENBENG.2012.6331358","DOIUrl":null,"url":null,"abstract":"Carbon-11 is a positron emitting nuclide that has been used extensively to label compounds destined for molecular targets in the brain. Pittsburgh compound B ([11C]PiB) is a benzothiazole derivative of thioflavin T that is used to image beta-amyloid deposits in Alzheimer's disease patients with Positron Emission Tomography (PET). In this paper we report on the optimization of a fully automated synthesis, purification and reformulation of [11C]PiB suitable for use in human PET studies. [11C]PiB was prepared from 2-(4'-aminophenyl)-6-hydroxybenzothiazole by [11C]-methylation with methyl triflate reacting in an high-performance liquid chromatography (HPLC) loop, purified and reformulated by solid phase extraction. The specific activity of [11C]PiB was 25 ± 10 GBq/μmol, and radiochemical purity was better than 95%.","PeriodicalId":399131,"journal":{"name":"2012 IEEE 2nd Portuguese Meeting in Bioengineering (ENBENG)","volume":"40 1","pages":"0"},"PeriodicalIF":0.0000,"publicationDate":"2012-10-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"2","resultStr":"{\"title\":\"Synthesis optimization of pittsburgh compound B by the captive solvent method\",\"authors\":\"G. Clemente, V. Alves, A. Abrunhosa\",\"doi\":\"10.1109/ENBENG.2012.6331358\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"Carbon-11 is a positron emitting nuclide that has been used extensively to label compounds destined for molecular targets in the brain. Pittsburgh compound B ([11C]PiB) is a benzothiazole derivative of thioflavin T that is used to image beta-amyloid deposits in Alzheimer's disease patients with Positron Emission Tomography (PET). In this paper we report on the optimization of a fully automated synthesis, purification and reformulation of [11C]PiB suitable for use in human PET studies. [11C]PiB was prepared from 2-(4'-aminophenyl)-6-hydroxybenzothiazole by [11C]-methylation with methyl triflate reacting in an high-performance liquid chromatography (HPLC) loop, purified and reformulated by solid phase extraction. The specific activity of [11C]PiB was 25 ± 10 GBq/μmol, and radiochemical purity was better than 95%.\",\"PeriodicalId\":399131,\"journal\":{\"name\":\"2012 IEEE 2nd Portuguese Meeting in Bioengineering (ENBENG)\",\"volume\":\"40 1\",\"pages\":\"0\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2012-10-18\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"2\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"2012 IEEE 2nd Portuguese Meeting in Bioengineering (ENBENG)\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.1109/ENBENG.2012.6331358\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"2012 IEEE 2nd Portuguese Meeting in Bioengineering (ENBENG)","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.1109/ENBENG.2012.6331358","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
Synthesis optimization of pittsburgh compound B by the captive solvent method
Carbon-11 is a positron emitting nuclide that has been used extensively to label compounds destined for molecular targets in the brain. Pittsburgh compound B ([11C]PiB) is a benzothiazole derivative of thioflavin T that is used to image beta-amyloid deposits in Alzheimer's disease patients with Positron Emission Tomography (PET). In this paper we report on the optimization of a fully automated synthesis, purification and reformulation of [11C]PiB suitable for use in human PET studies. [11C]PiB was prepared from 2-(4'-aminophenyl)-6-hydroxybenzothiazole by [11C]-methylation with methyl triflate reacting in an high-performance liquid chromatography (HPLC) loop, purified and reformulated by solid phase extraction. The specific activity of [11C]PiB was 25 ± 10 GBq/μmol, and radiochemical purity was better than 95%.
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