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Process for preparing aminobenzocyclobutenes

A process for preparing a 3- or 4-aminobenzocyclobutene comprises aminating a 3- or 4-halo- or sulfonyloxybenzocyclobutene reactant with an aminating agent by heating at a temperature from about 80 C. to a temperature at which dimerization or oligomerization of a benzocyclobutene reactant or product is a significant side reaction, in the presence of a metal-containing catalyst, for a time sufficient to aminate the halo- or sulfonyloxybenzocyclobutene reactant. In another aspect, this invention relates to a process for making a 3- or 4-phthalimido- or maleimidobenzocyclobutene, comprising reacting a 3- or 4-halobenzocyclobutene reactant with a phthalimide or maleimide compound in the presence of a metal-containing catalyst. The resulting phthalimido- or maleimidobenzocyclobutene can be hydrolyzed to a 3- or 4-aminobenzocyclobutene.

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

 

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The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.COA of Formula: Cu2O, Name is Copper(I) oxide, molecular formula is Cu2O, COA of Formula: Cu2O. In a Patent, authors is ,once mentioned of COA of Formula: Cu2O

Novel benzotriazoles anti-inflammatory compounds

The present invention relates to novel benzotriazoles of the formula I 1wherein Het is an optionally substituted 5-membered heterocycle containing one to two heteroatoms selected from nitrogen, sulfur and oxygen wherein at least one of said heteroatoms atoms must be nitrogen; R2 is selected from the group consisting of hydrogen, (C1-C6)alkyl or other suitable substituents; R3 is selected from the group consisting of hydrogen, (C1-C6)alkyl or other suitable substituents; s is an integer from 0-5; to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the present invention are potent inhibitors of MAP kinases, preferably p38 kinase. They are useful in the treatment of inflammation, osteoarthritis, rheumatoid arthritis, cancer, repurfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.

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

 

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Carbapenem compounds of the formula STR1 are useful intermediates for preparing antibacterial agents.

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

 

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Ab initio theoretical study of Cu2S, CuS, Cu2O and CuO lead to the determination of their geometrical parameters.These molecules were showed to be strongly polarized.CuS and Cu2S normal modes wavenumbers were also calculated.Theoretical study of Cu2S electronic spectrum showed that all allowed transitions lead to ultraviolet radiations.The determination of the first and the second Cu2X ionization potentials (verticals and adiabatics) as well as the calculation of Cu2X(+) and Cu2X(2+) geometries allowed us to state accurately the Cu2S and Cu2O molecular orbital diagrams.

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

 

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Method of treating estrogen dependent cancers

A method for alleviating the symptoms of post-menopausal syndrome comprising administering to a woman in need thereof an effective amount of a compound of formula I STR1 wherein R1a is –H or –OR7a in which R7a is –H or a hydroxy protecting group; R2a is –H, halo, or –OR8a in which R8a is –H or a hydroxy protecting group; R3 is 1-piperidinyl, 1-pyrrolidino, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidino, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; n is 2 or 3; and Z is –O– or –S–; or a pharmaceutically acceptable salt thereof.

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

 

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Dibenzo[b,d]thiopyran derivatives, pharmaceutical composition and use

The invention relates to compounds having the general formula (I) STR1 wherein R1 is carboxy, esterified carboxy or an amide of formula STR2 in which R9 is hydrogen or C1 -C6 alkyl, A is C2 -C6 alkylene and Ra and Rb are hydrogen or C1 -C6 alkyl or Ra and Rb taken together with the nitrogen atom to which they are linked form a saturated, optionally substituted, heteromonocyclic ring; R2 is hydrogen or C1 -C6 alkyl; each of R3 to R8 is independently hydrogen, halogen, C1 -C6 -alkyl, C3 -C4 alkenyloxy or C1 -C6 alkoxy; and the pharmaceutically acceptable salts thereof, which are useful as immunomodulating and anti-viral agents.

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

 

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THIAZOLIDINE DERIVATIVES, THEIR PREPARATION AND USE

Compounds of formula (I): (in which R1-R7 are hydrogen or various organic groups, n is 1-10, Ar is an aromatic group, U is CH2 or a carbon atom doubly bonded to either one of its adjacent carbons, and W is >CH2, >C=0 , >CHOH, >C=NOH or various derivatives thereof) have the ability to lower the levels of blood lipid peroxides and blood sugars and to inhibit the activity of aldose reductase; they may be used therapeutically for these purposes.

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

 

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Certain substituted imidazo [1,2-a] pyridines

Certain novel substituted imidazo [1,2-a] pyridines with a substituted amino group at the 2- or 3-position are active anthelmintic agents. The novel compounds are prepared from the appropriate substituted 2-aminopyridine precursor. Compositions which utilize said novel imidazo [1,2-a] pyridines as the active ingredient thereof for the treatment of helminthiasis are also disclosed.

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

 

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Hypoglycemic 5-substituted oxazolidine-2,4-diones

Hypoglycemic 5-furyl and 5-thienyl derivatives of oxazolidine-2,4-dione and the pharmaceutically-acceptable salts thereof; certain 3-acylated derivatives thereof; and intermediates useful in the preparation of said compounds.

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

 

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Process for producing tetrahydrophthalimides

A compound of the formula: STR1 wherein R is an isoproyl group or an n-amyloxycarbonylmethyl group, useful as a herbicide, is effectively produced by reacting a compound of the formula: STR2 wherein R is as defined above, with sulfuryl chloride or chlorine in a solvent in the presence of a dehydrohalogenating agent.

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