CAS: 956103-76-7; [18F]Florbetapir

该化合物是一种放射制药化合物,主要用于正电子排放断层成像,以检测与阿尔茨海默氏病有关的大脑中的氨基塑料.它是类的衍生物,其特点是能够有选择地与氨基苯甲集成结合.Florbetapir通常作为无线电标签追踪器管理,允许在体内直观地出现氨基体沉积.该化合物的分子重量相对较低,设计用于有效跨越血脑屏障.其药理学学学涉及大脑的快速分布,随后是对于准确的成像至关重要的逐步清除.安全剖面表明,它一般都具有良好的耐受体性,尽管与所有放射性药学一样,由于放射性特性,它需要谨慎处理和管理.总的来说,Florbetapir在老年痴呆症的早期诊断和管理中发挥着关键作用,通过及时干预,有助于更好的病人结果.

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    上下游产品

    (E)-2-[2-[2-[[5-[4-[boc-(甲基)氨基]苯乙烯基]-2-吡啶基]氧基]乙氧基]乙氧基]乙基-4-甲基苯磺酸酯 Av-105 1205550-99-7

    合成工艺路线路线简述

      📜(E)-2-[2-[2-[[5-[4-[boc-(甲基)氨基]苯乙烯基]-2-吡啶基]氧基]乙氧基]乙氧基]乙基-4-甲基苯磺酸酯置于potassium [18F]Fluoride,盐酸体系中,用 二甲基亚砜,水 作为反应溶剂,化学反应 0.25H,反应生成 氟贝他吡[18F]
      参考文献:Preparation And Stability Of Ethanol-Free Solution Of [18F]Florbetapir ([18F]Av-45) For Positron Emission Tomography Amyloid Imaging
      标题:Preparation And Stability Of Ethanol-Free Solution Of [18F]Florbetapir ([18F]Av-45) For Positron Emission Tomography Amyloid Imaging
      摘要:我们使用市售的自动化 Jfe 多功能合成仪开发了[18F]Florbetapir ([18F]Av-45) 的无乙醇制剂方法.我们还通过与传统的[18F]Av-45的10%乙醇溶液比较,评估了[18F]Av-45的无乙醇溶液在可见光照射和黑暗条件下的放射化学稳定性. [18F]Av-45的放射化学产率为55.1+/-2.2%(衰变校正至轰击结束),比活性为591.6+/-90.3Gbq/μmol,放射化学纯度>99%,总合成时间约为73 分钟发现通过溶解无乙醇溶液配制的[18 F]Av-45的放射化学纯度随着暴露于可见光的时间而降低.相反,通过在配方中添加 10% 乙醇或避免暴露在可见光下,可以抑制可见光光解作用.在通过溶解无乙醇溶液配制的[18 F]Av-45的放射合成中,通过避免暴露于可见光,可以获得高放射化学纯度和高稳定性的[18 F]Av-45.版权所有 © 2013 约翰.威利父子有限公司
      DOI:10.1002/jlcr.3021

      海关参考信息

      专利信息


      专利号:US-10109385-B2
      优先权日:2009-09-23
      标题:Dose synthesis card for use with automated biomarker production system
      发明人:MCFARLAND AARON; ANZELLOTTI ATILIO; HILLESHEIM DANIEL; BROWN-PROCTOR CLIVE; KHACHATURIAN MARK HAIG; LAND ANDREW
      权利人:ABT MOLECULAR IMAGING INC
      摘要:Microfluidic radiopharmaceutical production system and process for synthesizing per run approximately, but not less than, ten (10) unit doses of radiopharmaceutical biomarker for use in positron emission tomography (PET). A radioisotope from an accelerator or other radioisotope generator is introduced into a reaction vessel, along with organic and aqueous reagents, and the mixture heated to synthesize a solution of a pre-selected radiopharmaceutical. The solution is purified by passing through a combination of solid phase extraction purification components, trap and release components, and a filter. The synthesis process reduces waste and allows for production of biomarker radiopharmaceuticals on site and close to the location where the unit dose will be administered to the patient. On-site, as-needed production of radiopharmaceuticals in small doses reduces the time between synthesis of the radiopharmaceutical and administration of that radiopharmaceutical, minimizing loss of active isotopes through decay and allowing production of lesser amounts of radioisotopes overall.

      专利号:US-12007376-B2
      优先权日:2014-02-26
      标题 :Method for determining a concentration of a synthesis component in a radiopharmaceutical sample
      发明人:LEBEDEV ARTEM Y; ELIZAROV ARKADIJ M
      权利人:TRACE ABILITY INC
      摘要:A method for determining a concentration of a synthesis component in a radiopharmaceutical sample comprises providing an indicator, a metal or a metal complex, contacting the radiopharmaceutical sample with the indicator, metal or metal complex for a period of time sufficient to obtain an interaction, measuring an optical characteristic of the interacted components, and determining a concentration of the synthesis component in the radiopharmaceutical sample based on the measured optical characteristic.

      专利号:US-2010172836-A1
      优先权日:2008-12-31
      标题 :Synthesis of 18f-radiolabeled styrylpyridines from tosylate precursors and stable pharmaceutical compositions thereof

      专利号:BR-102015020840-B1
      优先权日:2015-08-28
      标题:BIPHENYL-DISULFIDE DERIVATIVES, PROCESS FOR THEIR PREPARATION, AND PROCESS FOR SYNTHESIS OF BENZOTHIAZOLIC DERIVATIVES

      专利号:EP-2381967-B1
      优先权日:2008-12-31
      标题 :Synthesis of 18f-radiolabeled styrylpyridines from tosylate precursors and stable pharmaceutical compositions thereof
      发明人:BENEDUM TYLER; GOLDING GEOFF; LIM NATHANIEL; ZHANG WEI
      权利人:AVID RADIOPHARMACEUTICALS INC

      专利号:EP-2381967-A1
      优先权日:2008-12-31
      标 题:Synthesis of 18f-radiolabeled styrylpyridines from tosylate precursors and stable pharmaceutical compositions thereof

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      ✅ COA系统入驻 | 共享模式

      合成参考文献


      参考文献:10.1001/archneurol.2011.152
      摘要:Jagust WJ. Amyloid imaging: liberal or conservative Let the data decide. Arch Neurol. 2011 Nov;68(11):1377–8. doi: 10.1001/archneurol.2011.152.
      参考文献:10.1001/archneurol.2011.150
      摘要:Fleisher AS, Chen K, Liu X, Roontiva A, Thiyyagura P, Ayutyanont N, Joshi AD, Clark CM, Mintun MA, Pontecorvo MJ, Doraiswamy PM, Johnson KA, Skovronsky DM, Reiman EM. Using positron emission tomography and florbetapir F18 to image cortical amyloid in patients with mild cognitive impairment or dementia due to Alzheimer disease. Arch Neurol. 2011 Nov;68(11):1404–11. doi: 10.1001/archneurol.2011.150.
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