123412-95-3Relevant articles and documents
Electrolytic partial fluorination of organic compounds: Part 26. Anodic monofluorination of ethyl isonicotinate
Konno, Akinori,Shimojo, Moriyasu,Fuchigami, Toshio
, p. 137 - 140 (1998)
Anodic fluorinations of ethyl isonicotinate (1) and related compounds have been attempted. Desired fluorinated product, 2-fluoroisonicotinate (2) was obtained in reasonable yield by direct anodic monofluorination of ethyl isonicotinate 1. The yield of 2 and the conversion of the electrochemical reaction could be improved by applying relatively lower anodic potential and by increasing the concentration of supporting electrolyte Et3N · 3HF.
C-H FLUORINATION OF HETEROCYCLES WITH SILVER (II) FLUORIDE
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Paragraph 0073; 00102; 00103, (2015/02/19)
The present invention provides compositions and methods for the selective C-H fluorination of nitrogen-containing heteroarenes with AgF2, which has previously been considered too reactive for practical, selective C-H fluorination. Fluorinated heteroarenes are prevalent in numerous pharmaceuticals, agrochemicals and materials. However, the reactions used to introduce fluorine into these molecules require pre-functionalized substrates or the use of F2 gas. The present invention provides a mild and general method for the C-H fluorination of nitrogen-containing heteroarene compounds to 2-fluoro-heteroarenes with commercially available AgF2. In various embodiments, these reactions occur at ambient temperature within one hour and occur with exclusive selectivity for fluorination at the 2-position. Exemplary reaction conditions are effective for fluorinating diazine heteroarenes to form a single fluorinated isomer.
Single photon emission computed tomography/positron emission tomography imaging and targeted radionuclide therapy of melanoma: New multimodal fluorinated and iodinated radiotracers
Maisonial, Aurélie,Kuhnast, Bertrand,Papon, Janine,Boisgard, Rapha?l,Bayle, Martine,Vidal, Aurélien,Auzeloux, Philippe,Rbah, Latifa,Bonnet-Duquennoy, Mathilde,Miot-Noirault, Elisabeth,Galmier, Marie-Josèphe,Borel, Michèle,Askienazy, Serge,Dollé, Frédéric,Tavitian, Bertrand,Madelmont, Jean-Claude,Moins, Nicole,Chezal, Jean-Michel
experimental part, p. 2745 - 2766 (2011/06/24)
This study reports a series of 14 new iodinated and fluorinated compounds offering both early imaging (123I, 124I, 18F) and systemic treatment (131I) of melanoma potentialities. The biodistribution of each 125I-labeled tracer was evaluated in a model of melanoma B16F0-bearing mice, using in vivo serial γ scintigraphic imaging. Among this series, [125I]56 emerged as the most promising compound in terms of specific tumoral uptake and in vivo kinetic profile. To validate our multimodality concept, the radiosynthesis of [18F]56 was then optimized and this radiotracer has been successfully investigated for in vivo PET imaging of melanoma in B16F0- and B16F10-bearing mouse model. The therapeutic efficacy of [131I]56 was then evaluated in mice bearing subcutaneous B16F0 melanoma, and a significant slow down in tumoral growth was demonstrated. These data support further development of 56 for PET imaging (18F, 124I) and targeted radionuclide therapy ( 131I) of melanoma using a single chemical structure.