Abstract

HBED-CC is a bifunctional complexing agent that, at ambient temperature, tightly chelates the trivalent radiometal 68Ga (T1/2 = 68 min). This complexing agent has attracted a lot of interest in tumor imaging applications. Depending on the chemical structure, different HBED-CC variants may be employed as radiolabeling precursor for the synthesis of desired radiopharmaceuticals. In this context, HBED-CC-tris(tert-butyl ester) is the only known monovalent variant of HBED-CC which is used for the synthesis of non-symmetric HBED-CC-based radiopharmaceuticals. Commercial HBED-CC-tris(tert-butyl ester) is very ­expensive, with limited availability. Nevertheless, no synthetic procedure for this useful product has been reported to date. This work introduces a convenient and comparatively cost-efficient method for the preparation of HBED-CC-tris(tert-butyl ester).

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