Literature DB >> 3019933

NCA 16 alpha-[18F]fluoroestradiol-17 beta: the effect of reaction vessel on fluorine-18 resolubilization, product yield, and effective specific activity.

J W Brodack, M R Kilbourn, M J Welch, J A Katzenellenbogen.   

Abstract

Although the reported synthesis of the title compound resulted in a high radiochemical yield (43% based on resolubilized 18F), the effective specific activity at EOS was low (166 Ci/mmol). Reduction in the amount of carrier fluoride in the target water improved the effective specific activity of the product, but with a concommitant decrease in the resolubilized yield of the fluoroestradiol (12.7%). A re-examination of the labeling parameters was performed to determine the conditions that would increase the yield of the fluoroestrogen and maintain a high effective activity for the product. Since the amount of resolubilized 18F in THF is important in obtaining high specific activity compounds in this type of synthesis, several types of vessels were investigated to determine their effect on the evaporation of the [18O]H2O target water and subsequent resolubilization of 18F into THF. Of the vessels (Pt crucible, borosilicate glass, siliconized borosilicate glass, Vacutainer), the Vacutainer afforded the highest resolubilization of 18F into THF (90%), resulting in an improved resolubilized yield for the fluoroestradiol (28%) and an increased effective specific activity at EOS for the product (1600-3939 Ci/mmol).

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Year:  1986        PMID: 3019933     DOI: 10.1016/0883-2889(86)90174-7

Source DB:  PubMed          Journal:  Int J Rad Appl Instrum A        ISSN: 0883-2889


  8 in total

1.  Synthesis of [F]Xenon Difluoride as a Radiolabeling Reagent from [F]Fluoride Ion in a Micro-reactor and at Production Scale.

Authors:  Shuiyu Lu; Victor W Pike
Journal:  J Fluor Chem       Date:  2010-10-01       Impact factor: 2.050

2.  Rapid and Efficient Radiosyntheses of Meta-substituted [F]Fluoroarenes from [F]Fluoride Ion and Diaryliodonium Tosylates within a Microreactor.

Authors:  Joong-Hyun Chun; Shuiyu Lu; Victor W Pike
Journal:  European J Org Chem       Date:  2011-08

3.  No-carrier-added [18F]fluoroarenes from the radiofluorination of diaryl sulfoxides.

Authors:  Joong-Hyun Chun; Cheryl L Morse; Frederick T Chin; Victor W Pike
Journal:  Chem Commun (Camb)       Date:  2013-02-07       Impact factor: 6.222

4.  A method of studying pharmacokinetics in man at picomolar drug concentrations.

Authors:  V J Cunningham; V W Pike; D Bailey; C A Freemantle; B C Page; A K Jones; M J Kensett; D Bateman; S K Luthra; T Jones
Journal:  Br J Clin Pharmacol       Date:  1991-08       Impact factor: 4.335

5.  Single-step Radiosyntheses of '18F-Labeled Click Synthons' from Azide-functionalized Diaryliodonium Salts.

Authors:  Chun Joong-Hyun; Victor W Pike
Journal:  European J Org Chem       Date:  2012-08-01

6.  Single-step syntheses of no-carrier-added functionalized [18F]fluoroarenes as labeling synthons from diaryliodonium salts.

Authors:  Joong-Hyun Chun; Victor W Pike
Journal:  Org Biomol Chem       Date:  2013-10-07       Impact factor: 3.876

7.  Feasibility and predictability of perioperative PET and estrogen receptor ligand in patients with invasive breast cancer.

Authors:  Mary L Gemignani; Sujata Patil; Venkatraman E Seshan; Michelle Sampson; John L Humm; Jason S Lewis; Edi Brogi; Steven M Larson; Monica Morrow; Neeta Pandit-Taskar
Journal:  J Nucl Med       Date:  2013-08-22       Impact factor: 10.057

Review 8.  The quest for improving the management of breast cancer by functional imaging: The discovery and development of 16α-[18F]fluoroestradiol (FES), a PET radiotracer for the estrogen receptor, a historical review.

Authors:  John A Katzenellenbogen
Journal:  Nucl Med Biol       Date:  2020-02-22       Impact factor: 2.408

  8 in total

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