NCA 16α-[ 18F]fluoroestradiol-17β: The effect of reaction vessel on fluorine-18 resolubilization, product yield, and effective specific activity

• Published in: International journal of radiation applications and instrumentation. Part A, Applied radiation and isotopes Vol. 37; no. 3; pp. 217 - 221
• Main Authors: Brodack, James W., Kilbourn, Michael R., Welch, Michael J., Katzenellenbogen, John A.
• Format: Journal Article
• Language: English
• Published: England Elsevier B.V 1986
• Subjects: Estradiol - analogs & derivatives; Fluorine; Isotope Labeling - instrumentation; Radioisotopes; Radioligand Assay
• ISSN: 0883-2889
• DOI: 10.1016/0883-2889(86)90174-7

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]H 2O target water and subsequent resolubilization of 18F into THF. Of these vessels (Pt crucible, borosilicate glass, siliconized borosilicate glass, Vacutainer R), 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).