On June 9, 2016, Chiotellis, Aristeidis; Muller Herde, Adrienne; Rossler, Simon L.; Brekalo, Ante; Gedeonova, Erika; Mu, Linjing; Keller, Claudia; Schibli, Roger; Kramer, Stefanie D.; Ametamey, Simon M. published an article.Category: chlorides-buliding-blocks The title of the article was Synthesis, radiolabeling, and biological evaluation of 5-Hydroxy-2-[18F]fluoroalkyl-tryptophan analogues as potential PET radiotracers for tumor imaging. And the article contained the following:
Aiming at developing mechanism-based amino acid 18F-PET tracers for tumor imaging, we synthesized two 18F-labeled analogs of 5-hydroxy-L-[β-11C]tryptophan ([11C]5HTP) whose excellent in vivo performance in neuroendocrine tumors is mainly attributed to its decarboxylation by aromatic amino acid decarboxylase (AADC), an enzyme overexpressed in these malignancies. Reference compounds and precursors were synthesized following multistep synthetic approaches. Radiosynthesis of tracers was accomplished in good radiochem. yields (15-39%), high specific activities (45-95 GBq/μmol), and excellent radiochem. purities. In vitro cell uptake was sodium-independent and was inhibited ≥95% by 2-amino-2-norbornanecarboxylic acid (BCH) and ∼30% by arginine. PET imaging in mice revealed distinctly high tumor/background ratios for both tracers, outperforming the well-established O-(2-[18F]fluoroethyl)tyrosine ([18F]FET) tracer in a head-to-head comparison. Biol. evaluation revealed that the in vivo performance is most probably independent of any interaction with AADC. Nevertheless, the excellent tumor visualization qualifies the new tracers as interesting probes for tumor imaging worthy for further investigation. The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Category: chlorides-buliding-blocks
The Article related to tryptophane hydroxy fluoro alkyl 18f synthesis radiolabeling tumor imaging, hydroxy tryptophane allylation danishevsky reaction protection hydroboration oxidation fluorination, phthaloyl hydroxytrypthophane benzylation krapcho decarboxylation reduction and other aspects.Category: chlorides-buliding-blocks
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