211 results about "1,2,3-Triazole" patented technology

Compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula: wherein j is 0 or 1, k is 0 or 1, m is 0, 1, or 2; n is 1 or 2; A is selected from the partial Formulas: where q is 1, 2, or 3, W3 is -O-; -N(R9)-; or -OC(=O)-; R7 is selected from -H; -(C1-C6) alkyl, -(C2-C6) alkenyl, or -(C2-C6) alkynyl substituted by 0 to 3 substituents R10; -(CH2)u-(C3-C7) cycloalkyl where u is 0, 1 or 2, substituted by 0 to 3 R10; and phenyl or benzyl substituted by 0 to 3 R14; R8 is tetrazol-5-yl; 1,2,4-triazol-3-yl; 1,2,4-triazol-3-on-5-yl; 1,2,3-triazol-5-yl; imidazol-2-yl; imidazol-4-yl; imidazolidin-2-on-4-yl; 1,3,4-oxadiazolyl; 1,3,4-oxadiazol-2-on-5-yl; 1,2,4-oxadiazol-3-yl; 1,2,4-oxadiazol-5-on-3-yl; 1,2,4-oxadiazol-5-yl; 1,2,4-oxadiazol-3-on-5-yl; 1,2,5-thiadiazolyl; 1,3,4-thiadiazolyl; morpholinyl; parathiazinyl; oxazolyl; isoxazolyl; thiazolyl; isothiazolyl; pyrrolyl; pyrazolyl; succinimidyl; glutarimidyl; pyrrolidonyl; 2-piperidonyl; 2-pyridonyl; 4-pyridonyl; pyridazin-3-onyl; pyridyl; pyrimidinyl; pyrazinyl; pyridazinyl; indolyl; indolinyl; isoindolinyl; benzo[b]furanyl; 2,3-dihydrobenzofuranyl; 1,3-dihydroisobenzofuranyl; 2H-1-benzopyranyl; 2-H-chromenyl; chromanyl; benzothienyl; 1H-indazolyl; benzimidazolyl; benzoxazolyl; benzisoxazolyl; benzothiazolyl; benzotriazolyl; benzotriazinyl; phthalazinyl; 1,8-naphthyridinyl; quinolinyl; isoquinolinyl; quinazolinyl; quinoxalinyl; pyrazolo[3,4-d]pyrimidinyl; pyrimido[4,5-d]pyrimidinyl; imidazo[1,2-a]pyridinyl; pyridopyridinyl; pteridinyl; or 1H-purinyl; or A is selected from phosphorous and sulfur acid groups; W is -O-; -S(=O)t-, where t is 0, 1, or 2; or -N(R3)-; Y is =C(R1a)-, or -[N<custom-character file="US20020111495A1-20020815-P00900.TIF" wi="20" he="20" id="custom-character-00001"/>(O)k] where k is 0 or 1; R4, R5 and R6 are (1) -H; provided that R5 and R6 are not both -H at the same time, -F; -Cl; -(C2-C4) alkynyl; -R16; -OR16; -S(=O)pR16; -C(=O)R16, -C(=O)OR16, -C(=O)OR<highlight><sup

The invention discloses a preparation method of a 1H-1,2,3-triazole compound as shown in a formula (I), which comprises the following steps: mixing halide as shown in a formula (III) with alkyne-terminated compound as shown in a formula (II) and sodium azide, reacting for 5-85 hours at 25-80 DEG C in a reaction solvent under the catalytic action of porous copper; after finishing the reaction, performing after-treatment of the reaction solution to obtain the 1H-1,2,3-triazole compound as shown in the formula (I), wherein the solvent is de-ionized water, acetonitrile, anhydrous ethanol, toluene, acetone, N,N-dimethylformamide, tetrahydrofuran or dioxane. The preparation method provided by the invention adopts one-pot operation, the catalyst can be reused for multiple times, the reaction condition is mild, and the operation is easy and simple.

The invention relates to a synthesis of naphthalene nucleus 4-position 1,2,3-triazole containing naphthalimide derivative and application thereof, and belongs to the field of organic synthesis. The derivative has a compound in a general formula A structure; the preparation method of the derivative comprises the following steps: by using 4-bromo-1,8-anhydride naphthalene as raw material, amidating with the corresponding chain amine through azidation, finally reacting with an amido-propyne connected with cyclic amine; the obtained derivative is applied to a tumor cell inhibition drug.

The invention discloses an organic semiconductor material. The organic semiconductor material contains a 4, 4'-bi-1H-1, 2, 3-triazolyl dibenzothiophene unit and an aromatic group which are connected by a conjugating manner. The invention further discloses a preparation method of the inorganic semiconductor material. The inorganic semiconductor material is prepared from a bialkynyl-containing dibenzothiophene monomer and an alkyl chain containing azide by click chemistry. Compared with the prior art, the organic semiconductor material is beneficial for pi-pi accumulation of molecules and enables good planarity of a polymer, and the performances of a device can be improved. The preparation method is simple and convenient, high in yield, simple in after-treatment, and convenient to purify.

The invention relates to N2-substituted-1,2,3-triazole ligand auxiliary Cu (I) catalysts and applications thereof in reaction of azides and terminal alkynes. The catalysts comprise N2-substituted-1,2,3-triazole ligands and Cu(I) salts, wherein the molar ratio of N2-substituted-1,2,3-triazole ligands to Cu(I) salts is 1:0.5-1:3. The catalysts are advantaged in that the middle nitrogen on the ring of the N2-substituted-1,2,3-triazole ligand has lower electron cloud density than the other two nitrogens, the middle nitrogen is substituted by a nitrogen heterocyclic ring, and the ligand utilizes triazole nitrogen atom with high electron cloud density and other heterocyclic ring nitrogen atom as a ligand effectively, the coordination capability with monovalent copper ions is enhanced, and monovalent copper ions is stabilized. The synthesis is simple and the properties are stable. In the catalysis of monovalent copper ions to a cycloaddition reaction of terminal alkynes and azides, the catalyst dosage is small, the reaction conditions are mild, the product yield is high and the substrate adaptability is strong.

The invention provides a high yield/isomerically pure synthesis of new 1-amino-3-substituted-1,2,3-triazolium salts and their subsequent transformation into isomerically pure 1-substituted-1,2,3-triazoles. These new 1-amino-3-substituted-1,2,3-triazolium salts are easily isolated and can be stored at ambient conditions with no degradation or isomerization. These quarternary salts are easily converted with appropriate silver salts to a wide array of new quarternary salts with various anions, with many of these new salts having melting points below 100 C, classifying them as ionic liquids. Subsequent diazotization of these 1-amino-3-substituted-1,2,3-triazolium salts results in high yields of isomerically pure 1-substituted-1,2,3-triazoles, that until this invention were problematic to make pure without tedious reagents or workup procedures. Both classes of materials (1-amino-3-substituted-1,2,3-triazolium salts as well as 1-substituted-1,2,3-triazoles) should be of high interest as these classes of materials are known to be very important pharmaceutical materials for a wide array of medical and agricultural applications as well as possible propellant applications.

The invention discloses a 1,2,3-triazole-flavonoid compound-sophocarpidine ternary conjugate and the use. The 1,2,3-triazole-flavonoid compound-sophocarpidine ternary conjugate has a structure as shown in the specification. The 1,2,3-triazole-flavonoid compound-sophocarpidine ternary conjugate has high-efficiency antitumor activity and a potential application value in the aspect of antitumor drug development. The 1,2,3-triazole-flavonoid compound-sophocarpidine ternary conjugate has a remarkable effect in the antitumor aspect, and can be applied to preventing and treating a plurality of clinically common tumors such as breast cancer, lung cancer, cervical cancer and liver cancer.

The invention discloses a combined antibacterial peptide having high stability and anti-drug-resistance activity, and belongs to the biochemical technical field. With precursor peptides containing propargyl glycine and azide lysine as a substrate, CuSO4.5H2O as a catalyst, sodium ascorbate as an antioxidant, and a water-N,N-dimethyl formamide mixed liquid as a solvent, a 1,3-dipolar cycloaddition reaction of click chemistry is carried out for 24-28 hours, and a 1,4-disubstituted-1H-1,2,3-triazole structure is generated and links the two precursor peptide chains to obtain the product. Antibacterial experiments of common standard bacteria and clinically isolated drug-resistant bacteria indicate that the synthesized J-RR-1 peptide has relatively strong antibacterial activity and clinically isolated drug-resistant bacteria resisting activity, and also has relatively high stability on pancreatin. Therefore, the peptide has a good application prospect in preparation of clinical treatment drugs.

Method for manufacturing semiconductor wafers having at least one through-base wafer via, the said method comprising the steps of (1) providing a semiconductor wafer having at least one electrically conductive via comprising an electrically conductive metal and extending from the front side of the semiconductor wafer at least partially through the semiconductor wafer; (2) affixing the frontside of the semiconductor wafer to a carrier; (3) contacting the backside of the semiconductor wafer with a polishing pad and an aqueous chemical mechanical polishing composition having a pH of equal to or greater than 9 and comprising (A) abrasive particles; (B) an oxidizing agent containing at least one peroxide group; and (C) an additive acting both as metal chelating agent and metal corrosion inhibitor; (4) chemically mechanically polishing the backside of the semiconductor wafer until at least one electrically conductive via is exposed. Preferably, the additive (C) is 1,2,3-triazole.

The present invention is directed to pharmaceutical compositions and methods of using combination therapies containing a SYK inhibitor, or a pharmaceutically acceptable salt thereof, and a antineoplastic or antiinflammatory agent for the treatment of inflammatory, autoimmune and cell proliferative diseases, such as allergic reaction, transplant rejection, rheumatoid arthritis (RA), lupus, multiple sclerosis (MS) or psoriasis undesired acute myeloid leukemia (AML), chronic lymphocytic leukemia (CLL), non-Hodgkin lymphoma (NHL) (including diffuse large B cell lymphoma (DLBCL)), mantle cell lymphoma, acute lymphocytic leukemia (ALL), follicular lymphoma, Burkitt's lymphoma, small Lymphocytic (SLL), Lymphoma, multiple myeloma, asthma, vasculitis, Idiopathic thrombocytopenic purpura (ITP), Heparin Induced Thrombocytopenia (HIT) and hemolytic anemia.

The invention relates to an N1 substituted 1,2,3-triazole derivative for a ligand of Cu(I) as well as a preparation method and application of the N1 substituted 1,2,3-triazole derivative. The structural general formula I of the N1 substituted 1,2,3-triazole derivative is as shown in the specification: R is alkyl or aryl; R' is an H atom, alkyl or aryl; X is a CH or N atom. The preparation method comprises the steps of mixing nitrogen-containing heterocyclic ring substituted terminal alkyne with azide, CuSO4 and sodium ascorbate, stirring based on absolute methanol as a solvent in the air under room temperature, reacting for 0.5-1 hour, and then directly generating a solid namely the N1 substituted 1,2,3-triazole derivative. Compared with the prior art, the N1 substituted 1,2,3-triazole derivative disclosed by the invention has the advantages that compared with other ligands, the ligand is simple in synthesis and stable in property. In a cycloaddition reaction between mono-valent copper ion catalytic terminal alkyne and azide, the ligand is small in catalyst dose, mild in reaction condition, high in product yield and strong in substrate adaptability.

A polymer for imparting repellency and stain resistance to substrates is disclosed of Formula 1:

(W)_a(R²)_b—Si(R¹)₂—O—[Si(R¹)₂—O]_n—[Si(W)_c(R¹)_d(R²)_e—O]_m—Si(R¹)₂—(W)_f(R²)_g

wherein: a, b, c, d, e, f and g are each independently 0 or 1, provided that (a+b) is 1, (f+g) is 1, and (c+d+e) is 2,

• • each R¹ is divalently a C₁ to C₈ alkyl,
  • each R² is independently H or C₁ to C₈ alkyl, optionally containing oxygen, nitrogen, or sulfur, or a combination thereof, n=0 to 500, m=1 to 100, each W is independently

(R_f—X-A-X)_p—Y

wherein:

R_f is a straight or branched perfluoroalkyl group having from about 2 to about 20 carbon atoms, or a mixture thereof, which is optionally interrupted by at least one oxygen atom, each X is independently an organic divalent linking group having from about 1 to about 20 carbon atoms, optionally containing oxygen, nitrogen, or sulfur, or a combination thereof, A is a 1, 2, 3-triazole, p=0 to 2, and

Y is O, OR, N, NR or N(R)₂ wherein R is H or C₁ to C₂₀ alkyl, optionally containing oxygen, nitrogen, or sulfur, or a combination thereof.

The invention relates to a 5-chlorol-2-hydroxyl-3-(4-substituted-1H-1,2,3-triazole) benzoic acid compound expressed in the formula (I) as well as a preparation method and application thereof. The definition of R is shown as the specification. In the preparation method, 5-chlorolsalicylic acid used as a raw material is nitrified and reduced, is subjected to azidation and reacts with end alkyne to obtain the corresponding 5-chlorol-2-hydroxyl-3-(4-substituted-1H-1,2,3-triazole) benzoic acid compound. The compound has the inhibiting function on HIV-1 integrase, and the IC50 of part of the compound reaches 1.6 mircograms/mL, therefore, the compound is a stronger HIV-1 integrase inhibiting agent and is expected to be developed into a new HIV virus resistant medicament.