TY - JOUR
T1 - One-step synthesis of N-succinimidyl-4-[18F]Fluorobenzoate ([18F]SFB)
AU - Petersen, Ida Nymann
AU - Madsen, Jacob
AU - Poulie, Christian Bernard Matthijs
AU - Kjær, Andreas
AU - Herth, Matthias Manfred
PY - 2019/9/22
Y1 - 2019/9/22
N2 - Herein, we present a one-step labeling procedure of N-succinimidyl-4-[18F]-fluorobenzoate ([18F]SFB) starting from spirocyclic iodonium ylide precursors. Precursor syntheses succeeded via a simple one-pot, two-step synthesis sequence, in yields of approximately 25%. Subsequent 18F-nucleophilic aromatic labeling was performed, and radiochemical incorporations (RCCs) from 5-35% were observed. Purification could be carried out using HPLC and subsequent solid phase extraction. Radiochemical purity (RCP) of >95% was determined. The total synthesis time, including purification and formulation, was no longer than 60 min. In comparison to the established 3-step synthesis route of [18F]SFB, this one-step approach avoids formation of volatile radioactive side-products and simplifies automatization.
AB - Herein, we present a one-step labeling procedure of N-succinimidyl-4-[18F]-fluorobenzoate ([18F]SFB) starting from spirocyclic iodonium ylide precursors. Precursor syntheses succeeded via a simple one-pot, two-step synthesis sequence, in yields of approximately 25%. Subsequent 18F-nucleophilic aromatic labeling was performed, and radiochemical incorporations (RCCs) from 5-35% were observed. Purification could be carried out using HPLC and subsequent solid phase extraction. Radiochemical purity (RCP) of >95% was determined. The total synthesis time, including purification and formulation, was no longer than 60 min. In comparison to the established 3-step synthesis route of [18F]SFB, this one-step approach avoids formation of volatile radioactive side-products and simplifies automatization.
KW - Fluorine-18
KW - Iodonium ylides
KW - N-succinimidyl-4-[F]fluorobenzoate
KW - PET
KW - [F]SFB
U2 - 10.3390/molecules24193436
DO - 10.3390/molecules24193436
M3 - Journal article
C2 - 31546683
AN - SCOPUS:85072572804
VL - 24
JO - Molecules (Print Archive Edition)
JF - Molecules (Print Archive Edition)
SN - 1431-5157
IS - 19
M1 - 3436
ER -