The ImmunoPET program makes use of a novel class of radiolabelled conjugates to provide a valuable tool for evaluating the success of ADC and mAb development molecules in the clinic. By administering this new class of radiolabeled conjugates to patients, PET imaging can show localization of the antibody in tumors as well as tumor uptake in a non-invasive manner. The small molecule linker-chelator G-605 (DFO-Suc-Fe-TFP) has been synthesized under cGMP conditions to provide a key component for the production of an ImmunoPET imaging agent. In order to provide this critical material, we developed a new synthesis and isolation procedure to address the liabilities of this molecule relating to its instability as room temperature and susceptibility to hydrolysis. By telescoping the synthetic steps, minimizing the time of contact with the aqueous phase during work-up and implementing a capture-and-release mobile phase gradient during C18, we were able to produce gram quantities of linker-chelator in high chemical purity for the first time.

Process development of the synthesis and purification of a reactive Immuno-PET conjugate intermediate

256th National Meeting (2018)

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