- Pyridyl Radical Cation for C?H Amination of Arenes
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Electron-transfer photocatalysis provides access to the elusive and unprecedented N-pyridyl radical cation from selected N-substituted pyridinium reagents. The resulting C(sp2)?H functionalization of (hetero)arenes furnishes versatile intermediates for the development of valuable aminated aryl scaffolds. Mechanistic studies that include the first spectroscopic evidence of a spin-trapped N-pyridyl radical adduct implicate SET-triggered, pseudo-mesolytic cleavage of the N?X pyridinium reagents mediated by visible light.
- R?ssler, Simon L.,Jelier, Benson J.,Tripet, Pascal F.,Shemet, Andrej,Jeschke, Gunnar,Togni, Antonio,Carreira, Erick M.
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supporting information
p. 526 - 531
(2019/01/04)
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- Metal-free chemoselective reduction of nitroaromatics to anilines via hydrogen transfer strategy
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A novel protocol for chemoselective reduction of aromatic nitro compounds to aromatic amines has been established. The metal-free reduction goes through a hydrogen transfer process. Various easily reducible functional groups can be well tolerated under the optimized reaction conditions.
- Shuai, Qi,Li, Jun,Zhao, Feng,Su, Weike,Deng, Guojun
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p. 965 - 975
(2019/04/13)
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- Substituent effects on stoichiometric and catalytic cleavage of carbon-nitrogen bonds in aniline derivatives by ruthenium-phosphine complexes
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The reactivity of various o-acylaniline derivatives with ruthenium complexes was examined. The reaction of o-acylanilines with RuH 2(CO)(PPh3)3 (1) or an activated ruthenium species formulated as "Ru(CO)(PPh3)s
- Koreeda, Tetsuro,Kochi, Takuya,Kakiuchi, Fumitoshi
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p. 682 - 690
(2013/03/14)
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- HETEROCYCLIC INHIBITORS OF HISTAMINE RECEPTORS FOR THE TREATMENT OF DISEASE
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The present invention relates to compounds and methods which may be useful as inhibitors of H1R and/or H4R for the treatment or prevention of inflammatory, autoimmune, allergic, and ocular diseases.
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Page/Page column 144
(2011/10/05)
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- HETEROCYCLIC INHIBITORS OF HISTAMINE RECEPTORS FOR THE TREATMENT OF DISEASE
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The present invention relates to compounds and methods which may be useful as inhibitors of H1R and/or H4R for the treatment or prevention of inflammatory, autoimmune, allergic, and ocular diseases.
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Page/Page column 59
(2010/06/11)
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- Synthesis of benzotriazine and aryltriazene derivatives starting from 2-azidobenzonitrile derivatives
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3-Substituted 3,4-dihydro-4-imino-1,2,3-benzotriazine derivatives 7 were formed from 2-azidobenzonitriles 4 as starting materials on treatment with Grignard or lithium organic reagents. In some cases these procedures gave aryltriazenes 10 and 11 as products. All compounds were identified by NMR spectroscopy and the structures of three products, namely 7a, 10a and 11i, were corroborated by X-ray crystallography. The reactions of 2-azidobenzonitrile derivatives with Grignard reagents have been investigated. These reactions, depending on the type of Grignard reagent and the substituents on the 2-azidobenzonitrile derivatives, resulted in benzotriazines and triazenes. Copyright
- Nakhai, Azadeh,Stensland, Birgitta,Svensson, Per H.,Bergman, Jan
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experimental part
p. 6588 - 6599
(2011/02/26)
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- SUBSTITUTED PIPERAZINES AS CB1 ANTAGONISTS
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Compounds of Formula (I) or pharmaceutically acceptable salts, solvates, or esters thereof, are useful in treating diseases or conditions mediated by CB1receptors, such as metabolic syndrome and obesity, neuroinflammatory disorders, cognitive disorders and psychosis, addiction (e.g., smoking cessation), gastrointestinal disorders, and cardiovascular conditions.
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Page/Page column 186
(2009/03/07)
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- A catalytic antibody against a tocopherol cyclase inhibitor
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The cyclic ammonium cation 5 and its guanidinium analogue 4 areinhibitors of tocopherol cyclase. Monoclonal antibodies were raised against protein conjugates of the haptens 1-3 and screened for catalytic reactions with alkene 8, a short chain analogue of
- Manetsch, Roman,Zheng, Lei,Reymond, Martine T.,Woggon, Wolf-Dietrich,Reymond, Jean-Louis
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p. 2487 - 2506
(2007/10/03)
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- EXLUSIVE ORTHO CYANATION AND ALKYLTHIOCARBONYLATION OF ANILINES AND PHENOLS USING BORON TRICHLORIDE
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Use of boron trichloride with or without an aditional Lewis acid makes possible a one-step synthesis of 2-cyano and 2-alkylthiocarbonyl anilines and phenols.
- Adachi, Makoto,Sugasawa, Tsutomu
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- Selective reduction of aromatic nitro compounds with stannous chloride in non acidic and non aqueous medium
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Aromatic nitro compounds are readily reduced by SnCl2, 2 H2O in alcohol or ethyl acetate or by anhydrous SnCl2 in alcohol where other reducible or acid sensitive groups such as aldehyde, ketone, ester, cyano, halogen and O-benzyl remain unaffected.
- Bellamy,Ou
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p. 839 - 842
(2007/10/02)
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- Compositions and process of treatment
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This invention relates to pharmaceutical compositions containing known compounds of the formula SPC1 Wherein M is selected from the group consisting of hydrogen, aluminum, ammonium, sodium, potassium, calcium, tris(hydroxymethyl)methylammonium and lower alkyl of 1 through 4 carbon atoms, R is selected from the group consisting of hydrogen and lower alkyl of 1 through 4 carbon atoms, and R1 and R2 are selected from the group consisting of hydrogen, fluorine, chlorine, bromine, trifluoromethyl, lower alkoxy of 1 through 4 carbon atoms and lower alkyl of 1 through 4 carbon atoms. The compounds (1) above are formulated with pharmaceutical carriers for inhalation or for oral, parenteral or rectal administration, with insufflation being the preferred method. The compositions are useful in the prophylactic treatment of sensitized humans and mammals for allergic and all anaphylactic reactions of a reaginmediated and non-reagin-mediated nature.
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