Radiochemical labeling of MDL 105725 using the secondary labeling precursor 2-[(18)F]fluoroethyltosylate ([(18)F]FETos) was carried out in yields of approximately 90% synthesizing [(18)F]MHMZ in a specific activity of approximately 50MBq/nmol with a starting activity of approximately 3GBq. Overall radiochemical yield including [(18)F]FETos synthon synthesis, [(18)F]fluoroalkylation and preparin...

R-(-)-[11C]Epinephrine ([11C]EPI) has been synthesized from R-(-)-norepinephrine by direct methylation with [11C]methyl iodide or [11C]methyl triflate. The total synthesis time including HPLC purification was 35-40 min. The radiochemical yields (EOB) were 5-10% for [11C]methyl iodide and 15-25% for [11C]methyl triflate. Radiochemical purity was > 98%; optical purity determined by radio-chiral H...

Current automated radiosynthesizers are designed to produce large clinical batches of radiopharmaceuticals. They not well suited for reaction optimization or novel radiopharmaceutical development since each data point involves significant reagent consumption, and contamination the apparatus requires time radioactive decay before next use. To address these limitations, a platform performing arra...

C-aryl derivatives of DOTA (N,N’,N”,N”’-tetrakis(carboxymethyl)1,4,7,10-tetraazacyclododecane) including phenyl-DOTA and 3-NO2Ph-DOTA were synthesized by a template reductive reaction. GaCl3 or GaCl3 was taken and transformed into Ga-acetylacetone (Ga(acac)3) before labeling to the DOTA derivatives. The Ga or Ga labeled complexes were generated by ligand-ligand exchange of acetylacetonate with ...

We describe a radiochemical method for measuring ferrochelatase activity in the in vitro incorporation of iron into mesoporphyrin-IX to form mesoheme. 59Fe is used to quantify ferrochelatase activity in rat liver. The uptake of iron is linearly related to the time allowed for it to occur, and the reaction proceeds optimally under reducing and anerobic conditions, maintained in sealed lyophiliza...

6-Deoxy-6-[(18)F]fluoro-D-fructose (6-[(18)F]FDF) is a promising PET radiotracer for imaging GLUT5 in breast cancer. The present work describes GMP synthesis of 6-[(18)F]FDF in an automated synthesis unit (ASU) and dosimetry calculations to determine radiation doses in humans. GMP synthesis and dosimetry calculations are important prerequisites for first-in-human clinical studies of 6-[(18)F]FD...