Synthesis of [18F]SU11248, a new potential PET tracer for imaging cancer tyrosine kinase.
N-[2-(Diethylamino)ethyl]-5-[(Z)-(5-[18F]fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide, a new potential positron emission tomography tracer for imaging cancer tyrosine kinase, has been prepared by the nucleophilic substitution of the nitro-precursor N-[2-(diethylamino)ethyl]-5-[(Z)-(5-nitro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide with K18F/Kryptofix 2.2.2 followed by a simple chromatography methodology combined solid-phase extraction with high-performance liquid chromatography purification procedures in 15-25% radiochemical yields.
Wang
Ji-Quan
JQ
Department of Radiology, Indiana University School of Medicine, Indianapolis, IN 46202, USA.
Miller
Kathy D
KD
Sledge
George W
GW
Zheng
Qi-Huang
QH
D005462:Fluorine Radioisotopes; D007211:Indoles / Q000138:chemical synthesis*; D009363:Neoplasm Proteins / Q000032:analysis*; D049268:Positron-Emission Tomography; D011505:Protein-Tyrosine Kinases / Q000032:analysis*; D011758:Pyrroles / Q000138:chemical synthesis*; D019275:Radiopharmaceuticals / Q000138:chemical synthesis*; D013329:Structure-Activity Relationship; D000077210:Sunitinib
D005462:Fluorine Radioisotopes; D007211:Indoles; D009363:Neoplasm Proteins; D011758:Pyrroles; D019275:Radiopharmaceuticals; D011505:Protein-Tyrosine Kinases; D000077210:Sunitinib