Abstract
Tritium-labelled fluoroazomycin arabinoside, [3H]-FAZA, is a useful probe for the investigation of hypoxia, furthermore it is safer and easier to handle than the PET tracer [18F]-FAZA when used in cell based assays. The only known synthesis of deuterium- and tritium-labelled FAZA was re-investigated and optimized. Then, a new and improved synthesis of [2H]-FAZA was developed as a model process for tritium radiolabelling. This novel synthesis is expected to greatly facilitate access to [3H]-FAZA.
Highlights
Most tumour types feature hypoxic regions, and in some neoplastic pathology hypoxia may be present in up to 60% of patients [1]
We have conducted a detailed study on the synthesis of one of the most important fluorine-containing compounds in the realm of molecular imaging, FAZA (1)
Tritium-labelled FAZA had previously been obtained by means of the same reducing agent used here albeit in tritiumlabelled form, i.e. NaB3H3CN [7], we envisage that our synthesis will be used for the preparation of [3H]-FAZA
Summary
Most tumour types feature hypoxic (low oxygen) regions, and in some neoplastic pathology hypoxia may be present in up to 60% of patients [1]. Tumours with high hypoxic volumes have a poor prognosis because they are associated with an aggressive phenotype and increased risk of metastasis [2]. These tumours tend to respond poorly to radiotherapy and/or chemotherapy [3]. Among the fluorinated hypoxia PET tracers, [18F]-FAZA, (fluoroazomycin arabinoside 1, Fig. 1) developed by Kumar in 1998 [7], was found to be useful for imaging hypoxia in various tumours such as glioblastoma, with a remarkably high tumour-tobackground and it can be considered the ‘‘gold standard’’ for the measurement of tissue hypoxia [8]. Groups, which should represent a more efficient access to [3H]FAZA 3
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