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Benzo[B]thiophene compounds, intermediates, processes, compositions, and methods

The instant invention provides novel benzo[b]thiophene compounds, intermediates, compositions, pharmaceutical formulations, and methods of use. The novel benzo[b] thiophenes have the formula wherein R1is -H, -OH, -O(C1-C4alkyl), -OCOAr where Ar is phenyl or substituted phenyl, -O(CO)OAr where Ar is phenyl or substituted phenyl, -OCO(C1-C6alkyl), -O(CO)O(C1-C6alkyl), or -OSO2(C4-C6alkyl); R2is -H, -F, -Cl, -OH, -O(C1-C4alkyl), -OCOAr where Ar is phenyl or substituted phenyl, -O(CO)OAr where Ar is phenyl or substitutedphenyl,-OCO(C1-C6alkyl),-O(CO)O(C1-C6alkyl), or -OSO2(C4-C6alkyl); R3and R4are, independently, -H, -F, -Cl, -CH3,-OH, -O(C1-C4alkyl), -OCOAr where Ar is phenyl or substituted phenyl, -OCO(C1-C6alkyl), -O(CO)O(C1-C6alkyl), or -OSO2(C4-C6alkyl), with the proviso that R3and R4are not both hydrogen; n is 2 or 3; and R5is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, or 1-hexamethyleneimino; ???or a pharmaceutically acceptable salt or solvate thereof.

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Reference£º
Copper catalysis in organic synthesis – NCBI,
Special Issue “Fundamentals and Applications of Copper-Based Catalysts”

 

Discovery of Copper(I) oxide

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Thiazolidine derivatives use

A thiazolidine derivative of the formula: STR1 wherein R1 is hydrogen, hydroxyl, lower alkyl having 1 to 4 carbon atoms, lower alkoxy having 1 to 4 carbon atoms, or lower carboxylic acyloxy having 2 to 4 carbon atoms; each of R2 and R3 is hydroxyl, lower alkyl having 1 to 4 carbon atoms, lower alkoxy having 1 to 4 carbon atoms or lower carboxylic acyloxy having 2 to 4 carbon atoms or pharmaceutically acceptable salt thereof a is a novel compound having antiulcer activity and inhibitory effect on gastric acid secretion. The compound is useful as antiulcer agent or inhibitory agent of gastric acid secretion.

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Reference£º
Copper catalysis in organic synthesis – NCBI,
Special Issue “Fundamentals and Applications of Copper-Based Catalysts”

 

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Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. Recommanded Product: 1317-39-1, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 1317-39-1, in my other articles.

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Thiazolidine derivatives

Thiazolidine derivatives of the general formula: STR1 [wherein R1 is alkyl, cycloalkyl, phenylalkyl, phenyl, a five- or six-membered heterocyclic group including one or two hetero-atoms selected from the group consisting of nitrogen, oxygen and sulfur or a group of the formula STR2 (where R3 and R4 are the same or different and each is lower alkyl or R3 and R4 are combined to each other either directly or as interrupted by a hetero-atom selected from the group consisting of nitrogen, oxygen and sulfur to form a five- or six-membered ring); R2 means a bond or a lower alkylene group; L1 and L2 are the same or different and each is lower alkyl or L1 and L2 are combined to form an alkylene group, provided that when R1 is other than alkyl, L1 and L2 may further be hydrogen, respectively] are novel compounds and useful as, for example, remedies for diabetes, hyperlipemia and so on of mammals including human beings.

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Reference£º
Copper catalysis in organic synthesis – NCBI,
Special Issue “Fundamentals and Applications of Copper-Based Catalysts”

 

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Thiazolidine derivatives, their preparation and compositions containing them

The compounds of formula (I): STR1 [in which: R1 and R2 are the same or different and each represents hydrogen or C1 -C5 alkyl; R3 represents hydrogen, an acyl group, a (C1 -C6 alkoxy)carbonyl group or an aralkyloxycarbonyl group; R4 and R5 are the same or different and each represents hydrogen, C1 -C5 alkyl or C1 -C5 alkoxy, or R4 and R5 together represent a C1 14 C4 alkylenedioxy group; n is 1, 2 or 3; W represents the –CH2 –, >CO or >CH–OR6 group (in which R6 represents any one of the atoms or groups defined for R3 and may be the same as or different from R3); and Y and Z are the same or different and each represents oxygen or imino] and pharmaceutically acceptable salts thereof have various valuable therapeutic effects on the blood system and may be prepared by a process which includes reacting a corresponding halopropionic acid derivative with thiourea.

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Reference£º
Copper catalysis in organic synthesis – NCBI,
Special Issue “Fundamentals and Applications of Copper-Based Catalysts”

 

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Beta-lactams and their production

A beta-lactam compound of the formula: STR1 wherein R1 and R2 are, the same or different, each a hydrogen atom or a lower alkyl group, R30 is a hydroen atom or a lower alkyl group having a beta-configuration, R4 is a carboxyl-protecting group, X is a hydrogen atom or a protected hydroxyl group and COZ is a protected thiolcarboxyl group, which is useful as a valuable intermediate in the stereospecific production of 1-alkylcarbapenem compounds.

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Reference£º
Copper catalysis in organic synthesis – NCBI,
Special Issue “Fundamentals and Applications of Copper-Based Catalysts”

 

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N2O decomposition over CuO/CeO2 catalyst: New insights into reaction mechanism and inhibiting action of H2O and NO by operando techniques

In this work, a combination of ex situ (STEM-EELS, STEM-EDX, H2-TPR and XPS), in situ (CO-DRIFTS) and operando (DR UV?vis and DRIFTS) approaches was used to probe the active sites and determine the mechanism of N2O decomposition over highly active 4?wt.% Cu/CeO2 catalyst. In addition, reaction pathways of catalyst deactivation in the presence of NO and H2O were identified. The results of operando DR UV?vis spectroscopic tests suggest that [Cu?O?Cu]2+ sites play a crucial role in catalytic N2O decomposition pathway. Due to exposure of {1?0?0} and {1?1?0} high-energy surface planes, nanorod-shaped CeO2 support simultaneously exhibits enhancement of CuO/CeO2 redox properties through the presence of Ce3+/Ce4+ redox pair. Its dominant role of binuclear Cu+ site regeneration through the recombination and desorption of molecular oxygen is accompanied by its minor active participation in direct N2O decomposition. NO and H2O have completely different inhibiting action on the N2O decomposition reaction. Water molecules strongly and dissociatively bind to oxygen vacancy sites of CeO2 and block further oxygen transfer as well as regeneration of catalyst active sites. On the other hand, the effect of NO is expressed through competitive oxidation to NO2, which consumes labile oxygen from CeO2 and decelerates [Cu+ Cu+] active site regeneration.

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Reference£º
Copper catalysis in organic synthesis – NCBI,
Special Issue “Fundamentals and Applications of Copper-Based Catalysts”

 

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Microbicidal N-sulfonylglycin alkynyloxyphenethyl amide derivatives

The invention relates to novel pesticidally active compounds of the general formula I as well as possible isomers and mixtures of isomers thereof,whereinn is a number zero or one; andR1 is C1-C12alkyl that is unsubstituted or may be substituted by C1-C4alkoxy, C1-C4alkylthio, C1-C4alkylsulfonyl, C3-C8cycloalkyl, cyano, C1C6alkoxycarbonyl, C3-C6alkenyloxycarbonyl or by C3-C6alkynyloxycarbonyl; C3-C8cycloalkyl; C2-C12alkenyl; C2-C12alkynyl; C1-C12haloalkyl: or a group NR11R12 wherein R11 and R12 are each independently of the other hydrogen or C1-C8alkyl, or together are tetra- or penta-methylene;R2 and R3 are each independently of the other hydrogen; C1-C8alkyl; C1-C8alkyl substituted by hydroxy, C1-C4alkoxy, mercapto or by C1-C4alkylthio; C3-C8alkenyl; C3-C8alkynyl; C3-C8cycloalkyl; C3-C8cycloalkyl-C1-C4alkyl; or the two groups R2 and R3 together with the carbon atom to which they are bonded form a three- to eight-membered ring;R4, R5, R6 and R7 are identical or different and are each independently of the others hydrogen or C1-C4alkyl;R8 is C1-C6alkyl, C3-C6alkenyl or C3-C6alkynyl;A is C1-C6alkylene; andB is optionally mono- or poly-nuclear, unsubstituted or substituted aryl; optionally mono- or poly-nuclear, unsubstituted or substituted heteroaryl; C4-C12alkyl; or C3-C8cycloalkyl.The novel compounds have plant-protecting properties and are suitable for protecting plants against infestation by phytopathogenic microorganisms.

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Reference£º
Copper catalysis in organic synthesis – NCBI,
Special Issue “Fundamentals and Applications of Copper-Based Catalysts”

 

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Use of N-substituted sulfoximines for control of invertebrate pests

Methods to control certain invertebrates including insects in agricultural, urban, animal health, and industrial systems by directly or systemically applying to a locus where control is desired an effective amount of a compound of N-substituted sulfoximines.

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Reference£º
Copper catalysis in organic synthesis – NCBI,
Special Issue “Fundamentals and Applications of Copper-Based Catalysts”

 

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Antidiabetic furancarboxylic and thiphenecarboxylic acids

Compounds of the structure STR1 wherein Z is oxygen or sulfur; R is (C1 -C2)alkoxy; phenoxy; benzyl; phenylthiomethyl; phenylthio; phenylthio monosubstituted in the 2-, 3- or 4-position with (C1 -C3)alkyl, phenyl, methoxy, chloro, fluoro or trifluoromethyl; phenylthio disubstituted in the 2,5- or 3,5- positions with methyl, methoxy, chloro, or fluoro; 2,3,5,6-tetrafluorophenylthio; 1- or 2-naphthylthio; (C2 -C6)alkylthio; or halo (bromo or chloro); and the pharmaceutically-acceptable salts thereof are useful in lowering the blood glucose levels of hyperglycemic mammals.

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Reference£º
Copper catalysis in organic synthesis – NCBI,
Special Issue “Fundamentals and Applications of Copper-Based Catalysts”

 

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Effect of surface treatment of the support on co oxidation over carbon-supported Wacker-type catalysts

The impact of surface treatment of the support on the oxidation of CO over carbon-supported Wacker-type catalyts was studied. This study focused on the effect of the chemical properties of activated carbon on CO oxidation over supported PdCl2-CuCl2 and PdCl2-CuCl2-Cu(NO)32 catalyts. The surface of active carbon used to prepare supported Wacker-type catalysts was enriched with carboxylic acid and carbonyl groups by pretreating with HNO3 or adding Cu(NO3)2 as a supplementary copper precursor. These surface groups improved the hydrophilicity and facilitated the formation of an active copper phase (Cu2Cl(OH)3). The effects were stronger, particularly on the formation of Cu2Cl(OH)3, when Cu(NO3)2 was combined with CuCl2 as catalyst precursors. The acceleration of CO oxidation can be attributed to the formation of the active copper phase and the improved hydrophilicity.

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Reference£º
Copper catalysis in organic synthesis – NCBI,
Special Issue “Fundamentals and Applications of Copper-Based Catalysts”