TY - JOUR T1 - Fully automated<sup>11</sup>C-Carbonylation using GE TracerLab FX<sub>M</sub>or FX<sub>C </sub>Synthesis Modules JF - Journal of Nuclear Medicine JO - J Nucl Med SP - 1452 LP - 1452 VL - 62 IS - supplement 1 AU - Xia Shao AU - Sean Preshlock AU - Karim Mhanna AU - Peter Scott Y1 - 2021/05/01 UR - http://jnm.snmjournals.org/content/62/supplement_1/1452.abstract N2 - 1452Objectives: The carbonyl group is one of the most widespread functional groups present in many bioactive molecules. That makes [11C]carbon monoxide an attractive precursor for labeling a wide range of compounds. However, 11C-carbonylation remains challenging due to low activity and poor solubility of CO. We report here a highly efficient and fully automated method using commercially available GE TracerLab FXm or FXc suitable for GMP production of radiopharmaceuticals. Both reductants, charcoal and molybdenum, were investigated. Methods: Production of [11C]CO: Method A: [11C]CO2 was passed through a heated charcoal column (950 oC ) at He flow of 100, 250, and 600 mL/min. The produced [11C]CO was trapped in a silica column immersed in liquid nitrogen. Method B: [11C]CO2 was passed through a heated molybdenum column (850 oC ) at He flow of 30 and 55 mL/min. In loop 11C-carbonylation: palladium catalyst [Pd2(π‐cinnamyl)Cl2 or Pd(dba)2] and Xantphos or N-Xantphos were dissolved into THF and mixed with halide. The mixture was kept at room temperature for at least 20 min. Two minutes prior to end of beam, an amine was added. The mixture was loaded onto an HPLC loop through a syringe filter. The [11C]CO trap was then removed from the liquid nitrogen to release [11C]CO into the loop. The loop was sealed for 5 min at room temperature. The reaction mixture was then injected onto a semi-preparative HPLC column for purification. Results: Production of [11C]CO: Method A: The yields of [11C]CO were &gt;90% at the various flow rates. Method B: The yields of [11C]CO were 65-75% at flow rates up to 55 mL/min. In loop 11C-carbonylation: Both model compounds and drug candidates have been labeled. Total synthesis time was 35-50 minutes and radiochemical yields were 3.8-7.2% (non-corrected) based on [11C]CO. The radiochemical purities were 90-98%. Molar activities were less than 0.5 Ci/µmol and greater than 5 Ci/µmol from charcoal and molybdenum method, respectively. Conclusions: We have developed a simple and high yielding 11C-carbonyl labeling process. The 11C-carbonylation was carried out at room temperature and no high pressure or high temperature equipment is required. The fully automated method uses commercially available radiosynthesis modules, which are commonly used for GMP production of radiopharmaceuticals. The optimization and qualification of PET tracers produced with this metheo for preclinical and clinical application is under way. ER -