- Sunlight induced functionalisation of some heterocyclic bases in the presence of polycrystalline TiO2
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The functionalisation of various heterocyclic bases induced by sunlight is reported. The photoreaction occurred with higher yield in a liquid-solid heterogeneous system in the presence of polycrystalline TiO2 (anatase) than in a homogeneous system under the same experimental conditions.
- Caronna,Gambarotti,Palmisano,Punta,Recupero
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Read Online
- Metal-, Photocatalyst-, and Light-Free Direct C-H Acylation and Carbamoylation of Heterocycles
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Direct C-H acylations and carbamoylations of heterocycles can now be readily achieved without requiring any conventional metal, photocatalyst, electrocatalysis, or light activation, thus significantly improving on sustainability, costs, toxicity, waste, and simplicity of the operational procedure. These mild conditions are also suitable for gram-scale reactions and late-stage functionalizations of complex molecules, including pharmaceuticals, N,N-ligands, and light-sensitive molecules.
- Westwood, Matthew T.,Lamb, Claire J. C.,Sutherland, Daniel R.,Lee, Ai-Lan
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supporting information
p. 7119 - 7123
(2019/09/03)
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- NEW SOMATOSTATIN RECEPTOR SUBTYPE 4 (SSTR4) AGONISTS
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The invention relates to 3-aza-bicyclo[3.1.0]hexane-6-carboxylic acid amide derivatives of general formula (I), which are agonists of somatostatin receptor subtype 4 (SSTR4), useful for preventing or treating medical disorders related to SSTR4. In addition, the invention relates to processes for preparing pharmaceutical compositions as well as processes for manufacture of the compounds according to the invention.
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Page/Page column 108; 109
(2014/12/12)
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- New Somatostatin receptor subtype 4 (SSTR4) agonists
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3-aza-bicyclo[3.1.0]hexane-6-carboxylic acid amide derivatives which are agonists of somatostatin receptor subtype 4 (SSTR4), useful for preventing or treating medical disorders related to SSTR4.
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Paragraph 0455; 0456; 0457; 0458
(2014/12/09)
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- A novel, selective free-radical carbamoylation of heteroaromatic bases by Ce(IV) oxidation of formamide, catalysed by N-hydroxyphthalimide
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The Ce(IV)-NHPI system was used to generate a carbamoyl radical by oxidation of formamide; this nucleophilic radical has been successfully used in the carbamoylation of heteroaromatic bases.
- Minisci, Francesco,Recupero, Francesco,Punta, Carlo,Gambarotti, Cristian,Antonietti, Fabrizio,Fontana, Francesca,Pedulli, Gian Franco
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p. 2496 - 2497
(2007/10/03)
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- Polycyclic N-Hetero Compounds. XXII. . Reaction of Pyridine N-oxides and Pyrazino Di-N-Oxides with Formamide
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Reactions of pyridine N-oxides, pyrazine N-oxides and their benzologues with formamide are described.Carbamoylation mainly occured at aromatic ring with loss of the N-oxide oxygen atom, however, 2,4,6-trimethylpyridine 1-oxide gave 2- and 4-pyrimidinyl derivatives.
- Hirota, Takashi,Namba, Tetsuto,Sasaki, Kenji
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p. 949 - 953
(2007/10/02)
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- POLAR EFFECTS IN FREE-RADICAL REACTIONS. NEW SYNTHETIC DEVELOPMENTS IN THE FUNCTIONALIZATION OF HETEROAROMATIC BASES BY NUCLEOPHILIC RADICALS
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The synthetic interest of the direct substitution of protonated heteroaromatic bases by nucleophilic carbon-centered radicals is furtheron developed by the following new achievements: i) utilization of the redox system N(+)H3OH/Ti(III) in several solvents; ii) utilization of benzoyl peroxide in alcohols; iii) carbamoylation by HCONH2 and H2O2 in the presence of catalytic amounts of Fe(II).These systems allow to obtain either substitution till now tried without success or reactions of industrial interest.Polar effects play a dominat role in determining reactivity, selectivity and synthetic applications; in particular the role of the strongly nucleophilic intermediate radicals of pyridinyl type in the rearomatization step is emphasized.
- Minisci, Francesco,Citterio, Attilio,Vismara, Elena,Giordano, Claudio
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p. 4157 - 4170
(2007/10/02)
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