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Tubulin binding ligands and corresponding prodrug constructs

A diverse set of tubulin binding ligands have been discovered which are structurally characterized, in a general sense, by a semi-rigid molecular framework capable of maintaining aryl-aryl, pseudo pi stacking distances appropriate for molecular recognition of tubulin. In phenolic or amino form, these ligands may be further functionalized to prepare phosphate esters, phosphate salts, and phosphoramidates capable of demonstrating selective targeting and destruction of tumor cell vasculature.

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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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Process for the preparation of 4-arylthioanilines

A process for the preparation of a 4-arylthioaniline from the corresponding 4-unsubstituted aniline which comprises reacting the latter with an alkali metal thiocyanate in the presence of halogen to provide the 4-thiocyanoaniline, reacting it with an alkali metal sulfide to convert the thiocyano moiety to an alkali metal mercaptide group followed by heating with cuprous oxide then with an aryl halide to form the desired product.

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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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BENZENEALKANOIC ACIDS FOR CARDIOVASCULAR DISEASES

Compounds of formula (I) wherein R 1, R 2, R 3 and R 4 are each H or C 1-C 4 alkyl; R 5 is (CH 2) m NHSO. sub.2 R 6 or (CH) m NHCOR 6 ; R 6 is C 1-C 6 alkyl, C 3-C 6 cycloalkyl optionally substituted by aryl, aryl or heteroaryl; R 7 is H, C 1-C 4 alkyl, C 1-C 4 alkoxy, halo, CF. sub.3, OCF 3, CN, CONH 2, or S(O) n (C 1-C 4 alkyl); X is CH 2, CHCH 3, CH(OH), C(OH)CH 3, C= CH 2, CO or O; m is 0 or 1 and n is 0, 1 or 2, and their pharmaceutically acceptable salts and biolabile esters, are antagonists of thromboxane A 2 of utility, particulary in combination with a thromboxane synthetase inhibitor, in the treatment of atherosclerosis and unstable angina and for prevention of reocclusion after percutaneous transluminal angioplasty.

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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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Note that a catalyst decreases the activation energy for both the forward and the reverse reactions and hence accelerates both the forward and the reverse reactions.Electric Literature of 1317-39-1, you can also check out more blogs aboutElectric Literature of 1317-39-1

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N,N-DI-ALKYL(PHENOXY)BENZAMIDE DERIVATIVES

The present invention relates to compounds of the formula: STR1 and the pharmaceutically acceptable salts thereof, wherein Z can be: STR2 wherein R 3 is alkyl having 1 to 6 carbon atoms and, when n is greater than 1, each R 3 can be the same or different; and n is an integer from 1 to 3;

R 1 and R 2 can each independently be hydrogen, straight or branched chain alkyl, or cycloalkyl having 3 to 8 carbon atoms which can optionally be substituted at one or more positions by alkyl of 1 to 6 carbon atoms; X is oxygen, sulfur, NR 4, wherein R 4 is hydrogen or alkyl having 1 to 4 carbon atoms, C=O, CHOH, or CH 2 ; Y is hydrogen, alkoxy, halogen, alkyl, or hydroxy; and m is an integer from 0 to 3. The compounds are antagonists of platlet-activating factor (PAF).

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

 

Extracurricular laboratory:new discovery of Copper(I) oxide

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Imidazo [1,2-a] pyridines substituted with a thienyl, thiazolyl, or thiadiazolyl group

Certain novel substituted imidazo [1,2-a] pyridines with a substituted amino group at the 2- or 3- position and a heterocyclic moiety on the pyrido portion of the molecule are active anthelmintic agents. The heterocyclic moiety is connected to the imidazo [1,2-a] pyridine molecule through an oxygen, sulfur, sulfinyl or sulfone. The novel compounds are prepared from the appropriately substituted 2-amino pyridine 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£º
Copper catalysis in organic synthesis – NCBI,
Special Issue “Fundamentals and Applications of Copper-Based Catalysts”

 

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Disubstituted xanthone carboxylic acid compounds

Compositions containing and methods employing, as the essential ingredient, novel disubstituted xanthone carboxylic acid compounds which are useful in the treatment of allergic conditions. Methods for preparing these compounds and compositions and intermediates therein are also disclosed. 5-Methylsulfinyl-7-isopropoxyxanthone-2-carboxylic acid and 5,7-di(methylsulfinyl)xanthone-2-carboxylic acid are illustrated as representative compounds.

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

 

Extracurricular laboratory:new discovery of Copper(I) oxide

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6H-Dibenz[b,e][1,4]oxathiepin derivatives

Novel 6H-dibenz[b,e][1,4]oxathiepin derivatives of the formulae I and IA are employed in the treatment and control of allergic conditions such as allergic asthma. STR1

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

 

Final Thoughts on Chemistry for Copper(I) oxide

I hope this article can help some friends in scientific research. I am very proud of our efforts over the past few months and hope to 1317-39-1, help many people in the next few years.Quality Control of Copper(I) oxide

Catalysts are substances that increase the reaction rate of a chemical reaction without being consumed in the process. Quality Control of Copper(I) oxide, Name is Copper(I) oxide, molecular formula is Cu2O, Quality Control of Copper(I) oxide, In a Patent, authors is £¬once mentioned of Quality Control of Copper(I) oxide

Potential anticancer agents derived from acridine

The compounds of the subject invention can be represented as follows: STR1 wherein each of R1, R2, R3, R4, are the same or different and are hydrogen (H), or a lower alkyl group of from about 1-4 carbon atoms, or a lower alkoxy group of from about 1-4 carbon atoms. R is a substituted aniline STR2 wherein one of R5, R6, R7 is an alkanol having the formula –(CH2)n OH, n=1-4, or its carbamate ester having the formula –(CH2)n OCONR’R”, n=1-4, and wherein R’ and R” the same or different lower alkyl groups of from about 1 to 4 carbon atoms, one of R’ and R” may be hydrogen (H), and the remaining groups are hydrogen. Additionally, the subject invention provides methods for synthesizing the above-identified compounds, physiologically acceptable compositions containing these compounds and methods for using these compounds to inhibit the growth of tumor cells.

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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 via stereospecific hydrogenation

A beta-lactam compound of the formula: STR1 wherein R1 is a hydrogen atom, a lower alkyl group or a 1-hydroxy(lower)alkyl group wherein the hydroxyl group is optionally protected, R2 is a hydrogen atom or a protective group for the nitrogen atom and R3 is a methyl group, a halomethyl group, a hydroxymethyl group, a protected hydroxymethyl group, a formyl group, a carboxyl group, a lower alkoxycarbonyl group or an ar(lower)alkoxycarbonyl group wherein the aryl group is optionally substituted, or R2 and R3 are combined together to form an oxaalkylene group and, when taken together with one nitrogen atom and two carbon atoms adjacent thereto, they represent a six-membered cyclic aminoacetal group, which is useful as a valuable intermediate in the stereospecific production of 1-methylcarbapenem compounds.

A reaction mechanism is the microscopic path by which reactants are transformed into products. Each step is an elementary reaction. In my other articles, you can also check out more blogs about 1317-39-1

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

 

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One of the oldest and most widely used commercial enzyme inhibitors is aspirin, Electric Literature of 1317-39-1, which selectively inhibits one of the enzymes involved in the synthesis of molecules that trigger inflammation. you can also check out more blogs about 1317-39-1

Electric Literature of 1317-39-1, Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics.In a document type is Patent, and a compound is mentioned, 1317-39-1, Copper(I) oxide, introducing its new discovery.

Benzothiphene compounds, intermediates, compositions, and methods

The invention provides benzothiophene compounds, formulations, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, and cardiovascular-related pathological conditions, including hyperlipidemia, and estrogen-dependent cancer.

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