- Cu-catalyzed fluorination of diaryliodonium salts with KF
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A mild Cu-catalyzed nucleophilic fluorination of unsymmetrical diaryliodonium salts with KF is described. This protocol preferentially fluorinates the smaller aromatic ligand on iodine(III). The reaction exhibits a broad substrate scope and proceeds with high chemoselectivity and functional group tolerance. DFT calculations implicate a CuI/CuIII catalytic cycle.
- Ichiishi, Naoko,Canty, Allan J.,Yates, Brian F.,Sanford, Melanie S.
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supporting information
p. 5134 - 5137
(2013/10/22)
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- Large-scale preparation of aromatic fluorides via electrophilic fluorination with functionalized aryl- or heteroarylmagnesium reagents
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Functionalized aryl- or heteroarylmagnesium reagents, prepared from the corresponding bromides or iodides using halogen-magnesium exchange or direct magnesium insertion in the presence of lithium chloride, reacted smoothly with N-fluorobenzenesulfonimide, (PhSO2)2NF, in the mixed solvent (4:1 CH2Cl2-perfluorodecalin) to give the corresponding aromatic fluorides in moderate to good yields. Georg Thieme Verlag Stuttgart · New York.
- Yamada, Shigeyuki,Knochel, Paul
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experimental part
p. 2490 - 2494
(2010/09/04)
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- Convenient electrophilic fluorination of functionalized aryl and heteroaryl magnesium reagents
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"Chemical Equation Presented" Cive me an "F": Electrophilic fluorination of various aromatic and heteroaromatic Grignard reagents is smoothly performed with (PhSO2)2NF as fluorinating agent in a 4:1 mixture of CH2Cl2/ perfluorodecalin (see scheme). This solvent system allows minimization of most side reactions.
- Yamada, Shigeyuki,Gavryushin, Andrei,Knochel, Paul
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supporting information; experimental part
p. 2215 - 2218
(2010/06/19)
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- Method For Preparation Of A Fluoroaromatic Compound From An Aminoaromatic Compound
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The invention relates to a method for preparation of fluorinated aromatic compounds from the corresponding amines by replacement of the amino group with a fluorine atom. The method of preparation of a fluoroaromatic compound from an aromatic compound with at least one amino group on the aromatic ring is characterized by the reaction of said aromatic amine compound with a nitrosating agent in the presence of a source of boron trifluoride in an organic medium, and carrying out a thermal treatment of the reaction medium comprising the diazonium salt thus obtained to give the fluoroaromatic compound directly by decomposition of the diazonium salt without intermediate isolation thereof.
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Page/Page column 9
(2008/06/13)
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- Novel nucleosides and related processes, pharmaceutical compositions and methods
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The invention provides novel nucleosides and related processes, pharmaceutical compositions, and methods. The novel nucleosides are useful in a wide variety of antiviral, antineoplastic, and antibacterial applications. Preferred embodiments of the instant invention include novel 2 halogen-substituted, 3 halogen-substituted, and 2′,3′dihalogen-substituted analogues of 3-deazaadenosine, and novel 3 halogen-substituted analogues of 3-deazaguanosine. Compounds of the instant invention, including 4-Amino-6-fluoro-1-(β-D-ribofuranosyl)imidazo[4,5-c]pyridine and 6-Amino-7-bromo-1,5-dihydro-1-β-D-ribofuranosylimidazo[4,5-c]pyridin-4-one, have exhibited potent antiviral and anticancer activity in vitro. The compounds are also useful in the concomitant treatment of bacterial infections associated with viral infections such as AIDS.
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Page/Page column 12; Figure 1
(2010/02/07)
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- Synthesis of halogen-substituted 3-deazaadenosine and 3-deazaguanosine analogues as potential antitumor/antiviral agents
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Various 2-halogen-substituted analogues (38, 39, 43 and 44), 3-halogensubstituted analogues (51 and 52), and 2′,3′ -dihalogen- substituted analogues (57-60) of 3-deazaadenosine and 3-halogen-substituted analogues (61 and 62) of 3-deazaguanosine have been synthesized as potential anticancer and/or antiviral agents. Among these compounds, 3-deaza-3-bromoguanosine (62) showed significant cytotoxicity against L1210, P388, CCRF-CEM and B16F10 cell lines in vitro, producing IC50 values of 3, 7, 9 and 7μM, respectively. Several 3-deazaadenosine analogues (38, 51, 57 and 59) showed moderate to weak activity against hepatitis B virus.
- Liu,Luo,Mozdziesz,Lin,Dutschman,Gullen,Cheng,Sartorelli
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p. 1975 - 2000
(2007/10/03)
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- Method for preparing 2,5-dihalo- and 2,5,6-trihalopyridines
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A method for preparing 2,5-dihalo- and 2,5,6-trihalopyridines corresponding to the formula SPC1 Wherein each X independently represents chloro, fluoro or bromo and R represents hydrogen, chloro, fluoro or bromo which comprises reacting a halohydrazinopyridine of one of the formulas SPC2 With an excess of an aqueous alkali metal hydroxide in the presence of a reaction medium from the group consisting of loweralkanols of 1 to 4 carbon atoms and loweralkylglycols of 2 to 4 carbon atoms.
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