Automated, Resin-Based Method to Enhance the Specific Activity of Fluorine-18 Clicked PET Radiotracers was written by Pisaneschi, Federica;Kelderhouse, Lindsay E.;Hardy, Amanda;Engel, Brian J.;Mukhopadhyay, Uday;Gonzalez-Lepera, Carlos;Gray, Joshua P.;Ornelas, Argentina;Takahashi, Terry T.;Roberts, Richard W.;Fiacco, Stephen V.;Piwnica-Worms, David;Millward, Steven W.. And the article was included in Bioconjugate Chemistry in 2017.SDS of cas: 14396-90-8 This article mentions the following:
Radiolabeling of substrates with 2-[18F]fluoroethylazide exploits the rapid kinetics, chem. selectivity, and mild conditions of the copper-catalyzed azide-alkyne cycloaddition reaction. While this methodol. has proven to result in near-quant. labeling of alkyne-tagged precursors, the relatively small size of the fluoroethylazide group makes separation of the 18F-labeled radiotracer and the unreacted precursor challenging, particularly with precursors >500 Da (e.g., peptides). We have developed an inexpensive azide-functionalized resin to rapidly remove unreacted alkyne precursor following the fluoroethylazide labeling reaction and integrated it into a fully automated radiosynthesis platform. We have carried out 2-[18F]fluoroethylazide labeling of four different alkynes ranging from <300 Da to >1700 Da and found that >98% of the unreacted alkyne was removed in less than 20 min at room temperature to afford the final radiotracers at >99% radiochem. purity with specific activities up to >200 GBq/μmol. We have applied this technique to label a novel cyclic peptide previously evolved to bind the Her2 receptor with high affinity, and demonstrated tumor-specific uptake and low nonspecific background by PET/CT. This resin-based methodol. is automated, rapid, mild, and general allowing peptide-based fluorine-18 radiotracers to be obtained with clin. relevant specific activities without chromatog. separation and with only a minimal increase in total synthesis time. In the experiment, the researchers used many compounds, for example, 2-(But-3-yn-1-yl)isoindoline-1,3-dione (cas: 14396-90-8SDS of cas: 14396-90-8).
2-(But-3-yn-1-yl)isoindoline-1,3-dione (cas: 14396-90-8) belongs to indole derivatives. Indole, first isolated in 1866, and it is commonly synthesized from phenylhydrazine and pyruvic acid, although several other procedures have been discovered. Indole plays a fundamental role for QS in E. coli, being one of the signal molecules responsible for the transcription of a variety of genes (gabT, and tnaB ASTD). SDS of cas: 14396-90-8
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Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles