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Development of a new precursor‐minimizing base control method and its application for the automated synthesis and SPE purification of [ 18 F]fluoromisonidazole ([ 18 F]FMISO)
Author(s) -
Lee Sang Ju,
Hyun Ji Suk,
Oh Seung Jun,
Yu Kook Hyun,
Ryu Jin Sook
Publication year - 2013
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.3115
Subject(s) - chemistry , radiochemistry , base (topology) , radiosynthesis , nuclear medicine , positron emission tomography , mathematical analysis , mathematics , medicine
Bases such as potassium carbonate and potassium bicarbonate (KHCO 3 ) are essential for the elution of trapped [ 18 F]fluoride from ion exchange cartridges and for the prevention of [ 18 F]fluoride adsorption on the silica glass vial during the preparation of radiopharmaceuticals for positron emission tomography imaging. However, these bases promote the chemical decomposition of precursor compounds and the creation of unwanted organic impurities. Thus, the goal of the current study was to develop a new method for synthesizing [ 18 F]fluoride‐labeled radiopharmaceuticals (e.g., [ 18 F]fluoromisonizadole ([ 18 F]FMISO)) that permits the fine control of base concentrations while minimizing adverse events. Non‐decay‐corrected radiochemical yields of 25.1 ± 5.0% and 13.3 ± 5.1% ( n = 3) were achieved after solid‐phase extraction purification using automatic synthesis with GE TRACERlab MX and KHCO 3 at concentrations of 14.1 and 33.0 µmol, respectively, and 1 mg of precursor (1‐(2′‐nitro‐1′‐imidazolyl)‐2‐ O ‐tetra‐hydropyranyl‐3‐ O ‐toluenesulfonyl propanediol (NITTP)). The newly developed synthesis protocol with fine base control and low precursor content permits high radiochemical yields with minimal impurities. Copyright © 2013 John Wiley & Sons, Ltd.