26154-20-1Relevant articles and documents
REAGENT AND PROCESS FOR THE SITE-SPECIFIC DEOXYFLUORINATION OF PEPTIDES
-
Page/Page column 18, (2020/01/31)
The present invention refers to reagents and methods for preparing a peptide sequence having a [18F]fluoro-aromatic amino acid side which may be further substituted, in particular a 4-[18F]fluoro-phenylalanine side chain in peptide sequences, by chemoselective radio-deoxyfluorination of an aromatic amino acid residue, in particular a tyrosine residue using a traceless-activating group and the reagents used in said process.
Site-Specific Deoxyfluorination of Small Peptides with [18F]Fluoride
Rickmeier, Jens,Ritter, Tobias
supporting information, p. 14207 - 14211 (2018/10/02)
Radiolabeled receptor-binding peptides are an important class of positron emission tomography tracers owing to achievable high binding affinities and their rapid blood clearance. Herein, a method to introduce a 4-[18F]fluoro-phenylalanine residue into peptide sequences is reported, by chemoselective radio-deoxyfluorination of a tyrosine residue using a traceless activating group. The replacement of only one hydrogen atom with [18F]fluoride results in minimal structural perturbation of the peptide, which is desirable in the labeling of tracer candidates.
ORGANIC SYNTHESIS APPLICATIONS OF NON-AQUEOUS FLUORIDE SALT SOLUTIONS
-
Paragraph 0149, (2017/03/21)
Processes and reaction mixtures including non-aqueous solvent mixtures are presented. Non-aqueous solvent mixtures including fluoride salt and non-aqueous solvent combinations are provided that possess high fluoride ion concentrations useful for a range of applications, including organic synthesis. Further non-aqueous solvent mixtures are provided including a salt possessing a non-fluoride anion and a non-aqueous solvent that, when contacted with aqueous fluoride-containing reagents, extract fluoride ions to form non-aqueous fluoride-ion solutions possessing high fluoride-ion concentrations. The salts include an organic cation that does not possess a carbon in the β-position or does not possess a carbon in the β-position having a bound hydrogen. This salt structure facilitates its ability to be made anhydrous without decomposition. Example anhydrous fluoride salts include (2,2-dimethylpropyl)trimethylammonium fluoride and bis(2,2-dimethylpropyl)dimethylammonium fluoride. The combination of these fluoride salts with at least one fluorine-containing non-aqueous solvent (e.g., bis(2,2,2-trifluoroethyl)ether; (BTFE)) promotes solubility of the salt within the non-aqueous solvents.
Reactions of the "Naked" Fluoride Ion: Syntheses and Structures of SeF6(2-) and BrF6(1-)
Mahjoub, Ali Reza,Zhang, Xiongzhi,Seppelt, Konrad
, p. 261 - 265 (2007/10/02)
1,1,3,3,5,5-Hexamethylpiperidinium fluoride (pip(1+)F(1-)) and 1,2-dimethylpropyltrimethylammonium fluoride have been prepared.They dissolve in fluorohydrocarbons (CH2F2, CF3-CHF-CF3, CHF3) even at very low temperatures.The nature of these solutions is indicated by the crystal structure of the adduct pip(1+)F(1-)*4CH2F2, which shows (C)H...F bridging.The high fluoride activity is exemplified by the previously unknown reaction between SeF5(1-) and F(1-) to yield SeF6(2-).The salt pip(1+)BrF6(1-) is obtained by a metathesis reaction of Cs(1+)BrF6(1-) with pip(1+)F(1-).The distortion of the SeF6(2-) structure from octahedral symmetry is intermediate between IF6(1-) (strongly distorted) and BrF6(1-) (octahedral).The electron-pair repulsion model is checked against these results. - Keywords: crystal structure; fluorides; hexafluorobromate(V); hexafluoroselenate(IV); naked fluoride