Garcia-Vazquez, Rocio published the artcileDevelopment of 18F-labeled bispyridyl tetrazines for in vivo pretargeted PET imaging, Quality Control of 100-70-9, the main research area is bispyridyl tetrazines PET imaging nucleophilic substitution; PET; bioorthogonal chemistry; bispyridyl tetrazines; fluorine-18; molecular imaging; pretargeted imaging; tetrazine ligation.
Pretargeted PET imaging is an emerging and fast-developing method to monitor immuno-oncol. strategies. Currently, tetrazine ligation is considered the most promising bioorthogonal reaction for pretargeting in vivo. Recently, we have developed a method to 18F-label ultrareactive tetrazines by copper-mediated fluorinations. However, bispyridyl tetrazines-one of the most promising structures for in vivo pretargeted applications-were inaccessible using this strategy. We believed that our successful efforts to 18F-label H-tetrazines using low basic labeling conditions could also be used to label bispyridyl tetrazines via aliphatic nucleophilic substitution. Here, we report the first direct 18F-labeling of bispyridyl tetrazines, their optimization for in vivo use, as well as their successful application in pretargeted PET imaging. This strategy resulted in the design of [18F]45, which could be labeled in a satisfactorily radiochem. yield (RCY = 16%), molar activity (Am = 57 GBq/μmol), and high radiochem. purity (RCP > 98%). The [18F]45 displayed a target-to-background ratio comparable to previously successfully applied tracers for pretargeted imaging. This study showed that bispyridyl tetrazines can be developed into pretargeted imaging agents. These structures allow an easy chem. modification of 18F-labeled tetrazines, paving the road toward highly functionalized pretargeting tools. Moreover, bispyridyl tetrazines led to near-instant drug release of iTCO-tetrazine-based â²click-to-releaseâ?reactions. Consequently, 18F-labeled bispyridyl tetrazines bear the possibility to quantify such release in vivo in the future.
Pharmaceuticals published new progress about Alkylation. 100-70-9 belongs to class nitriles-buliding-blocks, name is Picolinonitrile, and the molecular formula is C6H4N2, Quality Control of 100-70-9.
Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts