http://rdf.ncbi.nlm.nih.gov/pubchem/patent/WO-2022189304-A3

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filingDate 2022-03-04-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_fe90bb6c9ba25c4fa79c99ecf5ed8241
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publicationDate 2022-10-20-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber WO-2022189304-A3
titleOfInvention Aliphatic 18f-radiolabeling of a tetrazine precursor
abstract Up ontil now, only low reactivity Tzs can be radiolabeled via direct aliphatic SN2. Unfortunately, these structures display too low reactivity for in vivo bioorthogonal chemistry approaches. Highly reactive structures such as mono-unsubstituted tetrazines (H-Tzs) have been reported to be highly sensitive to base. Extensive degradation is observed which prevents isolation of meaningful amounts for imaging studies. In the present invention there is provided a method providing the possibility to radiolabel base sensitive tetrazine structures with significantly improved RCYs. Even tetrazines that were previously not accessible by applying "standard" aliphatic 18F-labeling strategies can be radiolabeled. This places new classes of 18F-fluorinated compounds within reach for application in PET imaginge studies such as for diagnosis of cancers.
priorityDate 2021-03-11-04:00^^<http://www.w3.org/2001/XMLSchema#date>
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Total number of triples: 29.