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Coupled heterogeneous photocatalysis using a P-TiO2-αFe2O3 catalyst and K2S2O8 for the efficient degradation of a sulfonamide mixture
Phosphorous-doped Ti-Fe mixed oxide (P-TiO2-αFe2O3) catalysts were prepared by the microwave-assisted sol-gel route and characterized using XRD, SEM, N2 physisorption, UV–vis diffuse reflectance, FTIR, and XPS. P-TiO2-αFe2O3 was evaluated during the degradation of a sulfonamide mixture (5 mg/L, each) under visible light. The photocatalytic process was optimized with a face-centered central composite design. Under optimal conditions (0.5 wt% of αFe2O3, pH 10, and 0.75 g/L of catalyst loading), the sulfate radical advanced oxidation process was carried out using 5 mM K2S2O8 (PS). P doping shifted the light absorption of P-TiO2-αFe2O3 in the visible light range owing to substitutional doping, while the coupling of P-TiO2 with α-Fe2O3 enhanced the absorption in the visible range, which resulted in an increase in the lifetime of the charge carriers and in a superior photoactivity of the P-TiO2-αFe2O3 catalyst in comparison to that of TiO2. The mineralization yield of the sulfonamides (SNs) mixture was enhanced in the presence of an electron acceptor (SO4 ? [rad]), allowing nearly 69 % within 300 min with the P-TiO2-αFe2O3/PS system, while P-TiO2-αFe2O3 and K2S2O8 oxidation achieved only 27 % and 21 %, respectively. The biodegradability index was 0.48 using the P-TiO2-αFe2O3/PS system, indicating a less toxic effluent than the original compounds. Recycling tests demonstrated that P-TiO2-αFe2O3 exhibits good stability in activating PS for SNs degradation during three cycles. Two main intermediates (pyrimidine and hydroquinone) and their hydroxylated re-arrangements were detected during the degradation of the SNs by the coupled process. Oxalic, oxamic, sulfonic, and acetic acids were also identified as by-products from the degradation of the SNs.
Guzmán-Mar, Jorge L.,Hernández-Ramírez, Aracely,Hinojosa-Reyes, Laura,Mendiola-Alvarez, Sandra Y.,Palomino-Cabello, Carlos,Turnes-Palomino, Gemma
(2020/03/18)

Nickel-Catalyzed Electrosynthesis of Aryl and Vinyl Phosphinates
A mild and useful nickel-catalyzed electrochemical phosphonylation of aryl and vinyl bromides is described. We show that alkyl H-phenylphosphinates can be coupled electrochemically with functionalized aryl and vinyl bromides using very simple conditions (Fe/Ni anode, bench-stable nickel pre-catalyst, undivided cell, galvanostatic electrolysis) to furnish the corresponding aryl and vinyl phosphinates in satisfactory to good yields. Couplings can also be applied to heteroaromatic bromides with some limitations like increased propensity to hydro-dehalogenation.
Daili, Farah,Ouarti, Abdelhakim,Pinaud, Marine,Kribii, Ibtihal,Sengmany, Stéphane,Le Gall, Erwan,Léonel, Eric
supporting information
p. 3452 - 3455
(2020/05/25)

Flow hydrodediazoniation of aromatic heterocycles
Continuous flow processing was applied for the rapid replacement of an aromatic amino group with a hydride. The approach was applied to a range of aromatic heterocycles, confirming the wide scope and substituent-tolerance of the processes. Flow equipment was utilized and the process optimised to overcome the problematically-unstable intermediates that have restricted yields in previous studies relying on batch procedures. Various common organic solvents were investigated as potential hydride sources. The approach has allowed key structures, such as amino-pyrazoles and aminopyridines, to be deaminated in good yield using a purely organic-soluble system.
R?der, Liesa,Nicholls, Alexander J.,Baxendale, Ian R.
(2019/06/05)

Salicylic Acid-Catalyzed One-Pot Hydrodeamination of Aromatic Amines by tert-Butyl Nitrite in Tetrahydrofuran
A significant acceleration in the hydrodeamination of in situ formed diazonium salts (from aromatic amines) has been observed in the presence of 10-mol% salicylic acid, using tetrahydrofuran as the hydrogen donor. The reaction proceeds efficiently at 20 °C for a wide range of substituted anilines, even at 10-mmol scale, without any other additive. The same protocol has been adapted to the selective deuterodeamination of some aromatic amines. Control experiments clearly show that aryl radicals are involved in the reaction mechanism. (Figure presented.).
Felipe-Blanco, Diego,Alonso, Francisco,Gonzalez-Gomez, Jose C.
supporting information
p. 2857 - 2863
(2017/08/23)

Infrared spectra of pyrazine, pyrimidine and pyridazine in solid argon
The vibrational spectra of monomeric diazines (pyrazine, pyrimidine and pyridazine) isolated in solid argon and of the neat crystalline phase of these compounds, at 10 K, are reported and discussed. Full assignment of the spectra is presented, providing evidence that the assignments of several bands previously undertaken for the compounds under other experimental conditions (e.g., gas phase, neat liquid or solution) shall be reconsidered. The interpretation of the experimental data is supported by extensive DFT calculations performed with the B3LYP functional and the 6-311++G(d,p) basis set and by comparison with the anharmonic vibrational calculations reported by Boese and Martin [J.Phys.Chem. A, 108 (2004) 3085] and Berezin et al. [Russian J.Phys.Chem., 79 (2005) 425; Opt.Spectrosc., 97 (2004) 201]. Spectra/structure correlations were extracted from the data, enabling to conclude that, while the π-electron systems in both pyrazine and pyrimidine rings are strongly delocalized over all heavy-atoms, in pyridazine the canonical form with one CC and two CN double bonds strongly predominates. Finally, the UV-induced photoisomerization of matrix isolated monomeric pyrazine to pyrimidine is reported.
Breda,Reva,Lapinski,Nowak,Fausto
p. 193 - 206
(2007/10/03)

Arylindenopyridines and arylindenopyrimidines and related therapeutic and prophylactic methods
This invention provides novel arylindenopyridines and arylindenopyrimidines of the formula: wherein R1, R2, R3, R4, and X are as defined above, and pharmaceutical compositions comprising same, useful for treating disorders ameliorated by antagonizing adenosine A2a receptors. This invention also provides therapeutic and prophylactic methods using the instant compounds and pharmaceutical compositions.
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(2008/06/13)

Substituted 2-aryl-3-(heteroaryl)-imidazo[1,2-a]pyrimidines, and related pharmaceutical compositions and methods
This invention relates to a series of imidazopyrimidines of Formula I, and pharmaceutical compositions containing them. The compounds of the invention inhibit the production of a number of inflammatory cytokines and are useful in the treatment and prevention of diseases associated with the overproduction thereof.
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(2008/06/13)

Substituted pyrimidine compositions and methods of use
Substituted pyrimidines that have the general structure: in which the symbol R1represents a C1-C6alkyl, C1-C6alkoxy or halogen atom; R2represents a phenyl group, substituted phenyl group, benzyl moiety, substituted benzyl moiety, C3-C7cycloalkyl, or substituted C3-C7cycloalkyl; R3represents a hydrogen or C1-C6alkyl group, R4represents —H, —OH, —N3or —NHCOCH3; and R5represents H are provided. These compounds have activity as inhibitors of phospholipase A2, and are useful in treating disorders mediated by phospholipase A2.
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(2008/06/13)

CRF receptor antagonists and methods relating thereto
CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animals, such as stroke. The CRF receptor antagonists of this invention have the following structure: including stereoisomers and pharmaceutically acceptable salts thereof, wherein n, m, A, B, C, R, R1, R2and Ar are as defined herein. Compositions containing a CRF receptor antagonist in combination with a pharmaceutically acceptable carrier are also disclosed, as well as methods for use of the same
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(2008/06/13)

CCR5 antagonists useful for treating AIDS
Compounds of the formula 1or a pharmaceutically acceptable salt or isomer thereof, wherein: Q, X and Z are CH or N; R, R4-R7 and R13 are H or alkyl; R1 is H, alkyl, fluoroalkyl, R9-arylalkyl, R9-heteroarylalkyl, alkyl—SO2—, cycloalkyl—SO2—, fluoroalkyl—SO2—, R9-aryl—SO2—, R9-heteroaryl—SO2—, N(R22)(R23)—SO2—, alkyl—C(O)—, cycloalkyl—C(O)—, fluoroalkyl—C(O)—, R9-aryl—C(O)—, NH-alkyl—C(O)— or R9-aryl—NH—C(O)—; R2 is H and R3 is H, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, R9-aryl, R9-arylalkyl, R9-heteroaryl, or R9-heteroarylalkyl, and when X and Z are each CH, R3 is alkoxy, R9-aryloxy, R9-heteroaryloxy, alkylC(O)O—, alkylaminoC(O)O—, alkylOC(O)NR13—, alkylOC(O)NR13— or alkylaminoC(O)NR13—; or R2 and R3 together are =O, =NOR10, =N—NR11R12 or =CH-alkyl; R8 is substituted phenyl, substituted heteroaryl, naphthyl, fluorenyl, diphenymethyl, alpha-substituted benzyl or alpha-substituted heteroarylmethyl; R9-R12 are as defined; are disclosed for the treatment of HIV, solid organ transplant rejection, graft v. host disease, inflammatory diseases, atopic dermatitis, asthma, allergies or multiple sclerosis, as well as pharmaceutical compositions and combinations with antiviral or anti-inflammatory agents.
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(2008/06/13)

One-Pot Two-Step Synthesis of Aryl Sulfur Compounds by Photoinduced Reactions of Thiourea Anion with Aryl Halides
(Equation presented) The photoinduced reactions of aryl halides with the thiourea anion afford arene thiolate ions in DMSO. These species without isolation, and by a subsequent aliphatic nucleophilic substitution, S RN1 reaction, oxidation, or protonation, yield aryl methyl sulfides, diaryl sulfides, diaryl disulfides, and aryl thiols with good yields (50-80%). This is a simple and convenient approach which involves the use of the commercially available and inexpensive thiourea in a one-pot two-step process for the synthesis of aromatic sulfur compounds.
Argueello, Juan E.,Schmidt, Luciana C.,Penenory, Alicia B.
p. 4133 - 4136
(2007/10/03)

Aminopyrimidine and aminopyridine anti-inflammation agents
Aminopyrimidine and aminopyridine (I) compounds, compositions and methods useful in the treatment of inflammatory, metabolic or malignant conditions, are provided herein.
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(2008/06/13)

Inhibitors of protein kinase for the treatment of disease
The present invention is directed in part towards methods of modulating the function of protein kinases with phenol- and hydroxynaphthalene-based compounds. The methods incorporate cells that express a protein kinase. In addition, the invention describes methods of preventing and treating protein kinase-related abnormal conditions in organisms with a compound identified by the invention. Furthermore, the invention pertains to phenol- and hydroxynaphthalene-based compounds and pharmaceutical compositions comprising these compounds.
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(2008/06/13)

Adenosine A2a receptor antagonists
This invention relates to compounds having the structural formula I or pharmaceutically acceptable salts or solvates thereof, wherein R, R2 and R3 are as defined in the specification, pharmaceutical compositions thereof, and methods of treating stroke or central nervous system diseases by administering the compound of the present invention to a patient in need of such treatment.
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(2008/06/13)

Inhibitors of c-Jun N-terminal kinases (JNK) and other protein kinases
The present invention provide a compound of formula I or II: or a pharmaceutically acceptable derivative thereof, wherein R1, R2, R3, and R4 are as described in the specification. These compounds are inhibitors of protein kinase, particularly inhibitors of JNK, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli; and Src-family kinases, especially Src and Lck kinases. These compounds are also inhibitors of GSK3 and CDK2 kinases. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.
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(2008/06/13)

Protease inhibitors
The present invention provides bis-aminomethyl carbonyl protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.
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(2008/06/13)

Trisubstituted heterocyclic compounds and their use as fungicides
Compounds of general formula (I): in which:Het represents a five or six membered saturated, partially unsaturated or aromatic ring containing between one and six heteroatoms of the group N, O, S, in which the heterocycle is substituted in an adjacent manner with -P-Q1-T-Q2, -GZ and Y, such that the substituant -GZ is adjacent to both. the other substituants being as defined in the description,process for preparing these compounds,fungicidal compositions comprising these compounds,processes for treating plants by applying these compounds or compositions.
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(2008/06/13)

CHEMICAL CONSTRUCTS AND THEIR USES
The invention provides a chemical construct for use in solid phase synthesis comprising a solid support Q having linked thereto groups YR and YR; wherein R is a substrate or a coding tag and the groups Y and Y are connecting groups each having a first cleavage site, at least one of Y and Y having a second cleavage site located between the first cleavage site and group R, the first cleavage site being orthogonally and selectively cleavable with respect to the second cleavage site, and, when both groups Y and Y contain a second cleavage site, the second cleavage site in Y being selectively and orthogonally cleavable with respect to the second cleavage site in Y; the second cleavage site being cleavable to release the substrate; and the first cleavage site being selectively cleavable to release a fragment Fr comprising the substrate R and at least a portion of the connecting group Y; and wherein: (i) the chemical fragment Fr contains a sensitising group G which sensitises the chemical fragment Fr to instrumental, e.g. mass spectroscopic analysis; and/or (ii) the fragment Fr contains a means for imparting a characteristic signature to the mass spectrum of the fragment.
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(2008/06/13)

Novel chain-breaking antioxidants
Compounds, preferably 5-pyrimidinol and 3-pyridinol derivatives, that act as effective chain breaking antioxidants of both the lipid and water-soluble variety (analogous to the natural Vitamins E and C), many of which are more reactive toward peroxyl radicals than the most potent form of Vitamin E. These compounds may exhibit many chemopreventive effects associated with conditions in which free radical-mediated cellular damage or disruption is implicated and Vitamins E and C are shown to have protective effects. Additionally, these compounds should be excellent oxidation inhibitors as additives to fuels, lubricants, rubber, polymers, chemicals, solvents and foodstuffs.
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(2008/06/13)

Inhibitors of glycogen synthase kinase 3
New pyrimidine or pyridine based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of disorders mediated by GSK3 activity, such as diabetes, Alzheimer's disease and other neurodegenerative disorders, obesity, atherosclerotic cardiovascular disease, essential hypertension, polycystic ovary syndrome, syndrome X, ischemia, traumatic brain injury, bipolar disorder, immunodeficiency or cancer.
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(2008/06/13)

Inhibitors of glycogen synthase kinase 3
Novel pyridine and pyrimidine derivatives which selectively inhibit glycogen synthase kinase 3 are provided and methods of preparing these compounds are provided. These compounds are useful in treating certain conditions which may be mediated by glycogen synthase kinase 3.
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(2008/06/13)

CHEMOKINE RECEPTOR BINDING HETEROCYCLIC COMPOUNDS
Tertiary amines containing a multiplicity of heteroaromatic substituents are useful as chemokine receptor modulators.
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(2008/06/13)

5-CYANO-2-AMINOPYRIMIDINE DERIVATIVES
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(2008/06/13)

Adenine based inhibitors of adenylyl cyclase, pharmaceutical compositions, and method of use thereof
The present invention relates to derivatives and analogues of adenine, which inhibit adenylyl cyclase activity. The present invention also relates to a method of preventing and inhibiting a patient's fibroproliferative vasculopathy following vascular injury or a vascular surgical operation which includes administering to the patient, an effective amount of a compound according to the invention subsequent to a vascular injury, or subsequent to a vascular surgical operation, for one to two weeks after the injury or surgical operation, effective to treat or prevent a patient's fibroproliferative vasculopathy such as chronic allograft rejection or vascular restenosis following vascular trauma. The present invention also relates to a method for measuring the inhibition of adenylyl cyclase activity and a method for treating congestive heart failure.
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(2008/06/13)

Imidazopyridine and imidazopyrimidine antiviral agents
The present invention concerns antiviral compounds, their methods of preparation and their compositions, and use in the treatment of viral infections. More particularly, the invention provides imidazopyridine and imidazopyrimidine derivatives (Formula I) for the treatment of respiratory syncytial virus infection.
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(2008/06/13)

N-heterocyclic derivatives as NOS inhibitors
N-Heterocyclic derivatives of the formula (I): are described herein, as well as other N-heterocycles, as inhibitors of nitric oxide synthase. Pharmaceutical compositions containing these compounds, methods of using these compounds as inhibitors of nitric oxide synthase and processes for synthesizing these compounds are also described herein.
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(2008/06/13)

Process for preparing MeO-Peg-protected dihydroquinine or dihydroquinidine derivatives, new dihydroquinine or dihydroquinidine derivatives and their use
Process for the formation of MeO-Peg-protected dihydroquinine or dihydro quinindine derivatives, new dihydroquinine-or dihyroquinidine derivatives as well as the use thereof. It is known that dihydroquinine or dihydroquinidine derivatives can be successfully used as ligands in the enantioselective dihydroxylation. The new disclosed ligand systems based on dihydroquinine/quinidine, unlike the prior art ligands, can be recycled after enantioselective dihydroxylation by precipitating and filtering the reaction medium, and be reused in the reaction medium. Also disclosed are the ligand systems (I) and (IV), process for preparing the same and their use in the enantioselective dihydroxiation of double bonds.
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(2008/06/13)

Fragrance precursors
The invention relates to fragrance precursors, In particular, the invention relates to the use of several classes of compounds which may act as fragrance precursors, e,g., in cosmetic products such as deodorants and antiperspirants and in laundry products such as detergents and fabric softners. These compounds are odorless, but upon contacting the skin as example, in skin care compositions or in personal care compositions, produce fragrances. The compounds also produce fragrances when used in the presence of lipases, e.g. as used in (laundry) detergents, thus providing a prolongation of the fabric scenting effect. The compounds under consideration are compounds of the formula I: The substituents are defined in the specification.
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(2008/06/13)

Heteroaryl azole herbicides
Compounds of Formula I, and their N-oxides and agriculturally suitable salts, are disclosed which are useful for controlling undesired vegetation and Q, W, X, Y, Z, and R1 through R8 are as defined in the disclosure.Also disclosed are compositions containing the compounds of Formula I and a method for controlling undesired vegetation which involves contacting the vegetation or its environment with an effective amount of a compound of Formula I.
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(2008/06/13)

Substituted thiadiazolesulfonamides
Compounds of the formula (I): are suitable for the preparation of pharmaceuticals for prophylaxis and treatment of all those diseases where an increased concentration of interleukin-1β participates in their course, for example septic shock, leukemia, hepatitis, muscular degeneration, HIV infections or degenerative joint diseases (such as osteoarthrosis, spondylosis, chondrolysis following joint trauma or prolonged immobilization of joints following meniscus or patella injuries, or torn ligaments), diseases of the connective tissue (such as collagenosis, periodontal diseases, or wound-healing disturbances), and chronic diseases of the locomotor system (such as inflammatory or immunologically or metabolism-related acute and chronic arthritis, arthropathies, rheumatoid arthritis, myalgias and disturbances in bone metabolism).
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(2008/06/13)

Alpha-substituted pyrimidine-thioalkyl and alkylether compounds as inhibitors of viral reverse transcriptase
The subject invention relates to pyrimidine-thioalkyl and alkylether compounds of Formula (I) and pyrimidine-thioalkyl and alkylethers of Formula (IA), namely the compounds of Formula (I) where R 4 is selected from the group consisitng of --H or --NR 15 R 16 where R 15 is --H and R 16 is --H, C 1 -C 6 alkyl, NH 2 or R 15 and R 16 taken together with the --N form 1-pyrrolidino, 1-morpholino or 1-piperidino; and R 6 is selected from the group consisting of --H, or halo (preferably --Cl); with the overall proviso that R 4 and R 6 are not both --H. The compounds of Formula (IA) are useful in the treatment of individuals who are HIV positive being inhibitors of viral reverse transcriptase. STR1
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(2008/06/13)

2-Pyrimidineamine derivatives and processes for their preparation
Compounds of general formula (1) are described wherein: Ar is an optionally substituted aromatic group; R2 is a hydrogen or halogen atom or a group -X1-R2a where X1 is a direct bond or a linker atom or group, and R2a is an optionally substituted straight or branched chain alkyl, alkenyl or alkynyl group; R3 is an optionally substituted heterocycloalkyl group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are selective protein tyrosine kinase inhibitors, particularly the kinases ZAP-70 and syk and are of use in the prophylaxis and treatment of immune or allergic diseases and diseases involving inappropriate platelet activation.
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(2008/06/13)

Pyrimidine compounds
5-Bromo-2-iodopyrimidine is used to synthesize a range of chemical compounds including liquid crystalline compounds.
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(2008/06/13)

Fragrance precursor compounds for preventing human malodor
The invention relates to agents preventing (the formation of) human malodor. In particular, the invention relates to the use of several classes of compounds which can act as such agents in cosmetic products, such as deodorants and antiperspirants. These compounds are normally odorless or nearly so, but upon contacting the skin as for example, in skin care compositions or in personal care compositions, they prevent malodor. The compounds under consideration are compounds of the formula The definition of the substituents is given in the specification.
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(2008/06/13)

SUBSTITUTED 6- AND 7- AMINOTETRAHYDROISOQUINOLINECARBOXYLIC ACIDS
Compounds of the formula I STR1 are suitable for the preparation of pharmaceuticals for the prophylaxis and therapy of disorders involving increased activity of matrix-degrading metalloproteinases.
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(2008/06/13)

Debromination of 8-bromo-2'-deoxyguanosine by methylene blue and visible light
Debromination of 8-bromo-2'-deoxyguanosine was accomplished in high yield under neutral conditions in aqueous methanol by irradiating with visible light in the presence of methylene blue as a sensitizer and triethylamine as an electron donor. The method can be extended for the debromination of other bromoaromatic compounds.
Venkatarangan, Lata,Yang, Dan-Hui,Epling, Gary A.,Basu, Ashis K.
p. 1441 - 1444
(2007/10/03)

Thermodynamics of electron attachment to pyrimidine and styrene in supercritical ethane
The reaction of excess electrons with pyrimidine and styrene was studied in supercritical ethane. The equilibrium constant for attachment was large when the solute was pyrimidine and small for styrene, although their electron affinities are comparable. At pressures above 100 bar, the rate constant for electron attachment to pyrimidine (ka) was time resolved using the short pulse of the laser-electron accelerator facility (LEAF). The rate constant, ka, is large and nearly independent of pressure and temperature; thus, the volume of activation is close to zero. At lower pressures, the equilibrium constants for this reaction were derived from the changes in the mobility of excess electrons. The free energy is a function of the polarization energy, which was evaluated with a compressible continuum model. The small equilibrium constant in the case of styrene is attributed to a smaller polarization energy. Values of ΔVr, obtained from changes of ΔGr with pressure, range from -9.0 to -0.4 L/mol. The observed volume changes are compared to electrostriction volumes calculated by the model. Electron attachment occurs with a large decrease in entropy associated with clustering of ethane molecules around the ion formed. Observed values of ΔSr are comparable to expected values calculated from ΔSr = (α/χT)ΔVr.
Holroyd, Richard A.,Nishikawa, Masaru,Itoh, Kengo
p. 9205 - 9210
(2007/10/03)

First Examples of Reactions of Azole N-Oxides with Thioketones: A Novel Type of Sulfur-Transfer Reaction
The reactions of 1,4,5-trisubstituted imidazole 3-oxides 1a-k with cyclobutanethiones 5a,b in CHCl3 at room temperature give imidazole-2(3H)-thiones 9a-k in high yield. The second product formed in this reaction is 2,2,4,4-tetramethylcyclobutane-1,3-dione (6a; Scheme 2). Similar reactions occur with 1 and adamantanethione (5c) as thiocarbonyl compound, as well as with 1,2,4-triazole-4-oxide derivative 10 and 5a (Scheme 3). A reaction mechanism by a two-step formation of the formal cycloadduct of type 7 via zwitterion 16 is proposed in Scheme 5. Spontaneous decomposition of 7 yields the products of this novel sulfur-transfer reaction. The starting imidazole 3-oxides are conveniently prepared by heating a mixture of 1,3,5-trisubstituted hexahydro-1,3,5-triazines 3 and α-(hydroxyimino) ketones 2 in EtOH (cf. Scheme 1). As demonstrated in the case of 9d, a 'one-pot' procedure allows the preparation of 9 without isolation of the imidazole 3-oxides 1. The reaction of 1c with thioketene 12 leads to a mixture of four products (Scheme 4). The minor products, 9c and the ketene 15, result from an analogous sulfur-transfer reaction (Path a in Scheme 5), whereas the parent imidazole 14 and thiiranone 13 are the products of an oxygen-transfer reaction (Path b in Scheme 5).
Mloston, Grzegorz,Gendek, Tomasz,Heimgartner, Heinz
p. 1585 - 1595
(2007/10/03)

Pesticidal pyrimidine compounds
Compounds of formula (I) in which X1 and X2 each represents oxygen; S(O)n, n being 0, 1 or 2; or CO, CH2 or NR, R being hydrogen or alkyl; R1 and R10 are each hydrogen or halogen; R2 and R9 are each hydrogen, halogen, cyano, nitro, alkyl, halo-alkyl, alkoxy, alkylthio, amino, mono- or di-alkylamino, alkoxyalkyl, haloalkoxyalkyl or alkoxycarbonyl; R3 and R8 are each hydrogen, chlorine, alkyl, haloalkyl, haloalkenyl, halo-alkynyl, haloalkoxy, haloalkoxycarbenyl, haloalkylthio, haloalkoxyalkyl, haloalkylsulphinyl, or haloalkylsulphonyl, nitro or cyano; R4 and R7 are each hydrogen, halogen, alkyl or alkoxy; R5 is hydrogen, halogen, cyano, alkyl, haloalkyl, alkoxy, alkylthio, alkylsulphonyl or phenyl; and R6 is hydrogen or, when R5 is hydrogen, alkyl; provided that either each phenyl is unsubstituted or at least one of R3 and R8 is not hydrogen, have useful pesticidal activity.
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(2008/06/13)

Palladium catalyzed nucleoside modifications methods using nucleophiles and carbon monoxide
This invention discloses a method for the preparation modified nucleosides using a palladium catalyst, a nucleophile and carbon monoxide.
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(2008/06/13)

CRF receptor antagonists and methods relating thereto
CRF receptor antagonists are disclosed. Such receptor antagonists are thiadiazole-, pyrimidine-, triazine-, and triazole-containing compounds substituted with both a C3-C14 monocyclic or fused, homoaryl or heteroaryl group and a substituted amine group. The CFR receptor antagonists have utility in the treatment of a variety of disorders, including disorders associated with the hypersecretion of CRF.
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(2008/06/13)

Pyrimidine bisphosphonate esters and (alkoxymethylphosphinyl)alkyl phosphonic acids as anti-inflammatories
Compounds useful in the treatment of inflammation structurally represented as STR1 wherein X,X1 and R groups are as herein defined.
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(2008/06/13)

Pharmaceutically active bicyclic-heterocyclic amines
The pharmaceutically active bicyclic heterocyclic amines (XXX) STR1 where W1 is --N= or --CH=; W3 is --N= or --CH=; W5 is --N= or --CR5 -- with the proviso that W5 is --CR5 -- when both W1 and W3 are --N= which are useful as pharmaceuticals in treating mild and/or moderate to severe head injury, subarachnoid hemorrhage and subsequent ischemic stroke, asthma and reduction of mucous formation/secretion in the lung and other diseases and injuries.
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(2008/06/13)

HYDROXAMIC ACID AND CARBOXYLIC ACID DERIVATIVES, PROCESS FOR THEIR PREPARATION AND USE THEREOF
This disclosure relates to a novel class of hydroxamic and carboxylic acid based matrix metalloproteinase inhibitor derivatives. The disclosure further relates to pharmaceutical compositions containing such compounds and to the use of such compounds and compositions in the treatment of matrix metalloproteinase induced diseases.
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(2008/06/13)

Effect of pressure on the e- + pyrimidine ? pyrimidine equilibrium in nonpolar solvents
The thermodynamics of the equilibrium reaction e- + pyrimidine ? pyrimidine was studied in tetramethylsilane (TMS) and 2,2,4-trimethylpentane (TMP) as solvents. In hexane, only the forward attachment reaction could be observed. The attachment rate constants (ka) increase with temperature in all solvents. The equilibrium shifts to the right with increasing pressure because of the large, negative reaction volumes (-200 to -330 cm3/mol). The volume changes are consistent with electrostriction by the pyrimidine anion when a glass shell of solvent molecules is included. The free energy of reaction at 298 K is -0.43 eV in tetramethylsilane at 1 bar and -0.70 eV in 2,2,4-trimethylpentane at 150 bar. The solution free energies indicate the gas-phase (adiabatic) electron affinity of pyrimidine is -0.24 eV.
Chen, Pingyun,Holroyd, Richard A.
p. 4491 - 4495
(2007/10/03)

Facile desulfurization of cyclic thioureas by hydrogen peroxide in acetic acid.
A simple, mild and synthetically useful method for the desulfurization of cyclic thioureas and related compounds, existing as thiol-thione tautomeric mixtures, by hydrogen peroxide in acetic acid is proposed. The effect of substituting different solvents for the acetic acid was investigated.
Grivas,Ronne
p. 225 - 229
(2007/10/02)

Oxidation of substituted 2-thiouracils and pyrimidine-2-thione with ozone and 3,3-dimethyl-1,2-dioxirane
Ozone and 3,3-dimethyl-1,2-dioxirane react with substituted 2-thiouracils and pyrimidine-2-thione to afford several interesting desulfurized products. The effect of the solvent, protic as opposed to nonprotic, on the course of oxidation was striking.
Claudia, Crestini,Mincione, Enrico,Saladino, Raffaele,Nicoletti, Rosario
p. 3259 - 3272
(2007/10/02)

OXIME DERIVATIVES
The invention concerns oxime derivatives of the formula I wherein R4 includes hydrogen, carboxy, carbamoyl, amino, cyano, trifluoromethyl, (1-4C)alkylamino, di(1-4C)alkylamino and (1-4C)alkyl; RS includes hydrogen, (1-4C)alkyl, (3-4C)alkeny1,(3-4C)alkynyl, (2-5C)alkanoyl, halogeno-(2-4-C)alkyl and hydroxy-(2-4C)alky1;Arl is phenylene or a hetercaryl diradical; Al is a direct link to XI, or Al is (1-4C)alkylene; XI is oxy, thio, sulphinyl or sulphonyl; Ar2 is phenylene or a heteroaryl diradical; RI is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkyny1; and R2 and R3 together form a group of the formula -A2. X2-A3- which together with the carbon atom to which A2 and A3 are attached define a ring having 5 or 6 ring atoms, wherein each of A2 and A3 is (1-3C)alkylene and X2 is oxy, thio, sulphinyl, sulphonyl or imino; or a pharmaceutically-acceptable sah thereof; processes for their manufacture; pharmaceutical compositions containing them and their use as 5-lipoxygenase inhibitors.
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(2008/06/13)

Ozonation of substituted 2-thiouracils and pyrimidine-2-thione
The ozonation of substituted 2-thiouracils and pyrimidine-2-thione is reported; this provides a new method for the synthesis of several pyrimidine derivatives.
Crestini, Claudia,Saladino, Raffaele,Nicoletti, Rosario
p. 1631 - 1634
(2007/10/02)

6-fluoro-3,5-dihydroxy carboxylic acids and derivatives thereof
6-Fluoro-3,5-dihydroxy carboxylic acid derivatives of the formula I and the corresponding lactones of the formula II STR1 in which R1 and R2 have the specified meanings, a process for the preparation of these compounds, the use thereof as medicinal agents and pharmaceutical products are described. In addition, new intermediates for the preparation of the compounds of the formula I or formula II are described.
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(2008/06/13)