- Method for preparing high-purity 1H-1, 2, 3-triazole
-
The invention relates to the technical field of 1H-1, 2, 3-triazole, and discloses a method for preparing high-purity 1H-1, 2, 3-triazole, and the method comprises the following steps: S1, obtaining raw materials; s2, putting a solvent and a catalyst into the raw materials obtained in the step S1, and carrying out stirring and heating treatment; s3, preserving heat to remove two carboxyl groups until the reaction is finished; s4, cooling treatment, and decolorizing with activated carbon after cooling; and S5, filtering the activated carbon after color removal, and dehydrating and purifying the filtered mother liquor by using a rectifying tower to obtain 1H-1, 2, 3-triazole. Compared with the prior art, the DMF is used for replacing a toxic and harmful solvent, and the technological process of decarboxylation at a relatively low temperature by adding a catalytic amount of copper oxide is adopted, so that green production is realized; 2, the method is low in energy consumption, simple in production process, safe and reliable; and 3, the yield is high, the selectivity is good, byproducts are few, the product purity is high, and unexpected technical effects, economic benefits and social benefits are achieved.
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Paragraph 0025-0095
(2021/07/10)
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- Method for preparing high-purity 1H-1, 2, 3-triazole
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The invention belongs to the technical field of chemicals, and particularly relates to a method for preparing high-purity 1H-1, 2, 3-triazole, 1H-1, 2, 3-triazole is prepared from the following chemical materials: glyoxal, hydrates, hydroxylamine hydrochloride, ethyl acetate, toluene, acetic anhydride and absolute methanol, wherein the concentration ofglyoxal is 40%, the concentration of the hydrate is 85%, the preparation of the 1H-1, 2, 3-triazole comprises four steps, namely, the first step of synthesis of monooxime hydrazone, the second step of synthesis of oxime acylhydrazone, the third step of synthesis of diacyloxime hydrazone and the fourth step of synthesis of triazole, the preparation method is easy to operate, common chemical experiment operation is adopted, the reaction conditions are simple, control is easy, the concentration of the prepared 1H-1, 2, 3-triazole is high, no pollutant is generated in the preparation process, the environment is not polluted, no danger is generated in the preparation process, no danger is generated in the experiment process, and the method is simple, easy to operate and safe.
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Paragraph 0028; 0031-0033; 0036-0038; 0041-0042
(2021/07/17)
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- Synthesis method for continuous flow preparation of 1H-1,2,3-triazole
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The present invention discloses a continuous flow of preparation of 1H-1,2,3-triazole synthesis method, the reaction formula is: comprising the following steps: step 1: in a solvent-free system, at a certain temperature, through the hydrazine hydrate, glydaldehyde reaction, to give intermediate I; step 2: and then pass into a suitable amount of ethanol to intermediate I to obtain an ethanol solution of intermediate I, in manganese dioxideMnO2 Under the action of the catalyst, oxygen is introduced, and the intermediate II is obtained by oxidation ringing reaction; step 3: Intermediate II is reacted with sodium nitrite under acidic conditions to obtain 1H-1,2,3-triazole by diazole; selectively further post-treatment can be obtained to obtain high-purity 1H-1,2,3-triazole. The synthesis method of the continuous flow preparation of the present invention is a continuous synthesis method of continuous flow microreactor, which is safe and controllable, the amount of hazardous waste is small, and the product yield is high, and the product yield is high, and the product quality is good.
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Paragraph 0012; 0041; 0045-0047; 0051-0053; 0057-0059; ...
(2022/01/08)
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- Method for continuously synthesizing 1H-1,2,3-triazole by using microchannel reactor
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The invention relates to a method for continuously synthesizing 1H-1,2,3-triazole through a microchannel reactor, and belongs to the technical field of medicine synthesis. The method comprises the following steps: reacting a hydrazine hydrate aqueous solution and a glyoxal aqueous solution in a micro-channel reactor to prepare a material 1, continuously reacting the material 1 with hydrogen peroxide in the micro-channel reactor to prepare a material 2, and continuously mixing the material 2 with concentrated hydrochloric acid in the micro-channel reactor to obtain a material 3; conducting reaction on the material 3 and a sodium nitrite aqueous solution in the micro-channel reactor, and conducting post-treatment to obtian 1H-1,2,3-triazole. No solvent needs to be added or replaced in the reaction process, manganese dioxide and potassium permanganate which can generate solid waste are prevented from being used, and toxic substances such as toluenesulfonyl chloride and dioxane which are harmful to the environment are not used either; and the 1H-1,2,3-triazole can be safely produced.
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Paragraph 0020; 0046; 0049-0052; 0055-0058; 0061-0063
(2021/05/19)
-
- Preparation method of 1H-1, 2, 3-triazole
-
The invention provides a preparation method of 1H-1, 2, 3-triazole, which comprises the following steps: adding glyoxal into an ethanol solution of hydrazine hydrate, and carrying out reduction reaction to obtain a glyoxal dihydrazone solution; adding hydrogen peroxide into the glyoxal dihydrazone solution, carrying out a cyclization reaction to prepare a 1-amino-1, 2, 3-triazole solution; addingpotassium permanganate into the 1-amino-1, 2, 3-triazole solution, and heating to carry out a deamination reaction, so as to obtain a 1H-1, 2, 3-triazole solution. According to the method, the 1H-1, 2, 3-triazole can be prepared by a one-pot method, a solvent does not need to be added or replaced in the reaction process, nitrite and potassium permanganate which can generate solid waste are prevented from being used, and toxic substances such as toluenesulfonyl chloride and dioxane which are harmful to the environment are not used.
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Paragraph 0043; 0046-0048; 0051-0053; 0056-0057
(2020/07/12)
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- 1 H - 1, 2, 3 - triazole preparation method (by machine translation)
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The invention belongs to the field of fine chemical pharmaceutical intermediates, discloses a 1 H - 1, 2, 3 - triazole of the preparation method. The method to replace the halogen animal pen and sodium azide in fat alcohol and water in the mixed solvent of azide, after being extracted by the organic solvent, directly with the acetylene in a pressure reactor in the reaction process for preparing the intermediate, then separating out intermediate, obtained through the strong acid debenzylation 1 H - 1, 2, 3 - triazole, through the rectification is purified to high purity of 1 H - 1, 2, 3 - triazole finished product. The whole synthetic route of the raw materials are cheap and easy to obtain, the process of synthesis of few, simple operation, low operation cost, process and environmental protection, it is very suitable for industrial production, has a very high industrial application value. (by machine translation)
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Paragraph 0039; 0044; 0045; 0053; 0058; 0059
(2019/02/03)
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- 1,2,3-triazole synthesizing method
-
The invention discloses a 1.1,2,3-triazole synthesizing method which comprises the following steps: performing oxidizing reaction on benzotriazole through a potassium permanganate saturated solution to obtain a solution containing 1,2,3-triazole-4,5-dicarboxylic acid; adding a hydrogen peroxide solution into the solution containing 1,2,3-triazole-4,5-dicarboxylic acid, performing suction filtration when purple of the solution fades, concentrating filtrate to obtain a concentrated solution, adding concentrated hydrochloric acid into the concentrated solution, standing, dissolving white solid out, filtering and drying to obtain 1,2,3-triazole-4,5-dicarboxylic acid; adding a solvent and cyclohexanedione into 1,2,3-triazole-4,5-dicarboxylic acid to perform decarboxylic reaction to obtain 1,2,3-triazole. According to the 1,2,3-triazole synthesizing method disclosed by the invention, the raw materials are simple and easy to obtain, reaction conditions are mild, operation is simple, aftertreatment is convenient, a requirement for equipment is not high, reaction is complete, byproducts are few, no solid waste is generated, and purifying means of filtering, centrifuging, recrystallizing andthe like are avoided.
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Paragraph 0032; 0035; 0036; 0039; 0040; 0043; 0044; 0047
(2019/02/03)
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- Green environmentally friendly 1-H-1,2,3-triazole preparation method
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The invention discloses a green environmentally friendly 1-H-1,2,3-triazole preparation method. The method uses benzotriazole and hydrogen peroxide as raw materials, 1-H-1,2,3-triazole-4,5-dicarboxylic acid is obtained under the action of a catalyst through oxidative ring opening and then acid adjusting, toluene is subjected to reflux decarboxylation, 1-H-1,2,3-triazole is obtained, the method isgreen, clean and low-cost, the product total yield can reach 80%, the purity is more than 99%, and the method is suitable for industrial production.
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Paragraph 0031; 0033; 0034; 0036; 0037; 0039; 0040; 0042
(2019/04/29)
-
- Method for preparing 1H-1,2,3-triazole
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The invention discloses a method for preparing 1H-1,2,3-triazole. The method comprises the following steps of: in a polar solvent, reacting glyoxal and hydrazine hydrate to obtain an intermediate 1, and then performing cyclization under the action of potassium permanganate to obtain an intermediate 2, reacting the intermediate 2 and potassium nitrite under acidic conditions for deamination to obtain a crude product triazole, and further purifying the crude product to obtain the finished product triazole. The method has the advantages of simple operation, short production cycle, and simple post-treatment, and the product has high yield, good purity and low cost, and is more suitable for industrial large-scale production.
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Paragraph 0033; 0050; 0052; 0055
(2019/04/10)
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- Method for preparing important intermediate 1H-1,2,3-triazole of Tazobactam
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The invention discloses a method for preparing an important intermediate 1H-1,2,3-triazole of Tazobactam. The method comprises the steps: firstly, subjecting glyoxal to a reaction with hydroxylamine hydrochloride, so as to obtain an intermediate I; subjecting the intermediate I and an ammonium salt to cyclization in the presence of a catalyst, so as to obtain an intermediate II; and subjecting the intermediate II to a reaction with nitrite under acidic conditions to deaminate so as to obtain crude triazole, and carrying out further refining, thereby obtaining finished triazole. According to the method, the operation is simple, the production cycle is short, the aftertreatment is simple, few waste gases, waste water and waste residues are produced, and the obtained product is high in yield, good in purity and low in cost, so that the method is more applicable to industrial large-scale production.
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Paragraph 0047; 0051-0053; 0057; 0058
(2019/10/01)
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- A 1 H - 1, 2, 3 - triazole preparation method
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The invention discloses a 1 H - 1, 2, 3 - triazole preparation method, which belongs to the field of fine chemical synthesis, comprising the following steps: tert butyl-bromide and sodium azide as raw materials, the reaction at room temperature to obtain tert-butyl azido, tert-butyl azide in the catalyst, is introduced into the acetylene gas reaction to obtain 1 - tert-butyl - 1, 2, 3 - triazole, 1 - tert-butyl - 1, 2, 3 - triazole in under the condition of strong acid butyl takes off uncle, get 1 H - 1, 2, 3 - triazole, the invention of 1 H - 1, 2, 3 - triazole preparation method solves the previous serious pollution in the route, strong corrosive, high pressure hydrogenation and the like, thereby achieving the energy saving and environmental protection, and the operation is simple, can be large-scale automated production of the requirement of green chemistry.
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Paragraph 0032; 0035; 0036; 0039
(2019/03/28)
-
- Preparation method of 1H-1,2,3-triazole
-
The invention discloses a preparation method of 1H-1,2,3-triazole. According to the method, benzotriazole is taken as a raw material and subjected to oxidation and decarboxylation, then distillation purification is performed, and high-purity 1H-1,2,3-triazole is obtained. Raw materials of the whole synthesis route are cheap and easily available, operation is simple and convenient, operation cost is low, the process is environmentally friendly, and the method is quite suitable for industrial production and has quite high industrial application value.
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Page/Page column 6-7
(2019/01/16)
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- Synthesis method for 1H-1,2,3-triazole
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The invention provides a synthesis method for 1H-1,2,3-triazole. The synthesis method comprises the following steps of (a) oxidizing with potassium permanganate in an acid condition by using benzotriazole as a starting material and tetrabutylammonium bromide as a catalyst, so as to obtain 1H-1,2,3-triazole-4,5-dicarboxylic acid; and (b) under catalysis of N,N-diisopropylethylamine, removing the carboxyl group of the 1H-1,2,3-triazole-4,5-dicarboxylic acid, so as to obtain 1H-1,2,3-triazole. In the synthesis method, the oxidization ring-opening reaction of benzotriazole is carried out with potassium permanganate as an oxidant in the acid condition. The potassium permanganate has high oxidization in the acid condition, and the benzotriazole reacts fully, so that the yield of the 1H-1,2,3-triazole-4,5-dicarboxylic acid is improved. In step (b), water is used as a solvent and can be evaporated in post-treatment to be recycled. The synthesis method uses simple materials easy to obtain, the reaction conditions are mild, the operations are simple, the yield is high, the prepared 1H-1,2,3-triazole product has high quality, and the reaction cost is low. The synthesis method is applicable to industrial production.
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Paragraph 0035; 0040; 0041; 0045; 0046; 0050; 0051
(2017/08/31)
-
- Preparation method of 1H-1, 2, 3-triazole
-
The invention discloses a preparation method of 1H-1, 2, 3-triazole. The preparation method comprises the following step: performing a reaction on a compound A and sodium nitrite in a solvent I, wherein the compound A is 1,2-diamido-ethylene, 1,2-diamido-ethylene salt or a mixture of 1,2-diamido-ethylene and 1,2-diamido-ethylene salt. Compared with the prior art, the preparation method has the beneficial effects that (1) a production line is short, the conversion rate of a target product is high, the utilization ratio of atoms is high, and the atom economy is high; (2) the molar yield is high, and the total molar yield is above 90%; (3) the solvent can be recycled and reused, and the discharge amount of waste water is very small; and (4) a production process is safe and controllable.
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Paragraph 0027; 0042-0056
(2018/03/28)
-
- Synthesis process of triazolone
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The invention discloses a synthesis process of triazolone, which includes the steps of: A) preparing triazole; B) dissolving parachlorophenol and potassium carbonate in an organic solvent to form a mixture system, heating the mixture system to 90-100 DEG C and dropwise adding chloropinacolone to the mixture system, and maintaining the temperature for 3-5 h to obtain a first intermediate; C) dropwise adding a chlorine source to an organic solution of the first intermediate, and maintaining the temperature for 3 h at 50-60 DEG C; D) adding the triazole to the mixture system in the step C), heating the mixture system to 100-120 DEG C and maintaining the temperature for 2-3 h to prepare the triazolone. The synthesis process is simple and is low in content of byproducts during synthesis. By adjusting the content of inorganic substances in reaction products, the reaction proceeds towards positive direction, thus increasing reaction yield. The synthesis process is suitable for industrial production.
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Paragraph 0019
(2017/10/07)
-
- Preparation method of high-purity 1H-1,2,3-triazole
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The invention relates to a preparation method of high-purity 1H-1,2,3-triazole. The preparation method comprises steps as follows: step (1), benzotriazole is taken as a raw material, potassium permanganate is taken as an oxidizing agent, water is taken as a solvent, and high-purity 1H-1,2,3-triazole-4,5-dicarboxylic acid is obtained through an oxidation ring-opening reaction, purification and drying under the alkaline condition; step (2), 1H-1,2,3-triazole-4,5-dicarboxylic acid obtained in the step (1) has a decarboxylic reaction in an N,N-dimethylformamide solvent under the catalytic action of a catalyst, a target product, namely, high-purity 1H-1,2,3-triazole is obtained through purification, and the catalyst is quinolone, pyridine or a mixture of quinolone and pyridine. In the step (2), quinolone or pyridine is taken as a catalyst to replace conventional copper powder or oxide of copper, the reaction selectivity is good, the yield is high, the product purity is high, and the stability is better.
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Paragraph 0033; 0034
(2016/10/07)
-
- Synthesis of N-unsubstituted 1,2,3-triazoles via a cascade including propargyl azides, allenyl azides, and triazafulvenes
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About thirty NH-1,2,3-triazoles with at least one additional functional group in a side chain at C-4 were prepared from propargyl substrates. These reactions included propargyl azides and their [3,3]-sigmatropic rearrangement to generate short-lived allenyl azides, which cyclized to form triazafulvenes that could be trapped by addition of N- or O-nucleophiles. In most cases, simple substrates and cheap sodium azide were utilized as starting compounds, and the syntheses were performed by using a one-pot procedure without isolation of any dangerous azides. This method to prepare NH-1,2,3-triazoles turned out to be compatible with quite different substitution patterns of the propargyl substrate.
- Banert, Klaus,Hagedorn, Manfred,Hemeltjen, Claudia,Ihle, Andreas,Weigand, Kevin,Priebe, Hanno
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p. 338 - 361
(2016/11/21)
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- Exploiting the Imidazolium Effect in Base-free Ammonium Enolate Generation: Synthetic and Mechanistic Studies
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N-Acyl imidazoles and catalytic isothiourea hydrochloride salts function as ammonium enolate precursors in the absence of base. Enantioselective Michael addition–cyclization reactions using different α,β-unsaturated Michael acceptors have been performed to form dihydropyranones and dihydropyridinones with high stereoselectivity. Detailed mechanistic studies using RPKA have revealed the importance of the “imidazolium” effect in ammonium enolate formation and have highlighted key differences with traditional base-mediated processes.
- Young, Claire M.,Stark, Daniel G.,West, Thomas H.,Taylor, James E.,Smith, Andrew D.
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p. 14394 - 14399
(2016/11/11)
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- PROCESS FOR THE LARGE SCALE PRODUCTION OF 1H- [1,2,3]TRIAZOLE AND ITS INTERMEDIATE 1-BENZYL-1H-[1,2,3] TRIAZOLE
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The present invention provides a process for the large scale production of 1H-[ 1,2,3]triazole of formula (I) and it's intermediate 1 -benzyl- 1H-[ 1,2,3]triazole of formula (II) by using benzyl azide and vinyl acetate as starting materials. This process is economical, environment friendly and safer by avoiding use of special equipment.
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Page/Page column 6
(2015/03/28)
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- Solid-Phase Supports and Uses Thereof
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The present disclosure relates to solid-phase azide supports, methods for making solid-state azide supports, and methods for capturing alkynes using the same. The present disclosure also relates to kits for solid-phase azide supports
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- COMPOUNDS FOR USE IN THE TREATMENT OF MYCOBACTERIAL INFECTIONS
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The present invention concerns compounds of general formula (I): in which Y and Z are chosen from CH and N; T is chosen from CO or SO2; n is 1 to 3; R1 represents a group chosen, for example, from C1-C3 alkyl chains unsubstituted or substituted by fluorine, the unsubstituted or substituted cyclic, cyano, azido, alkoxy and phenyl groups; and R is chosen from the azido, cyano, alkinyl and 2-benzothiazolyl groups and an optionally substituted aromatic heterocycle with five vertices; and the use thereof in the treatment of bacterial and mycobacterial infections such as, for example, tuberculosis, leprosy and atypical mycobacterial infections. The present invention also concerns pharmaceutical compositions comprising, as the active ingredient, at least one of the abovementioned compounds and optionally an antibiotic activatable via the EthA pathway
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- New spiroepoxide tetrahydrobenzo-triazoles and -imidazoles and their use as MetAP-II inhibitors
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The present invention relates to new spiroepoxide tetrahydrobenzo-triazole and - imidazole compounds, a method for their production and their use as MetAP-II inhibitors, which are particularly useful as inhibitors of angiogenesis. The compounds are characterized by formula (I) X=CorN R1 = OC(O)R2 where R2 is alkyl, cycloalkyl, aryl, heteroaryl, or cinnamyl or R1 = OC(O)NHR3 where R3 is alkyl, cycloalkyl, aryl, or heteroaryl or R1 = NHC(O)OR4 where R4 is alkyl or R1 = OH, NH2 R5 = alkyl, cycloalkyl, CH2R6 where R6 is aryl or heteroaryl
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Page/Page column
(2014/04/04)
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- COMPOUNDS TARGETING THE CATION-INDEPENDENT MANNOSE 6-PHOSPHATE RECEPTOR
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The invention relates to conjugates of products of interest and of compounds targeting the cation-independent mannose 6-phosphate receptor with a high affinity. The invention also relates to their applications, for instance in enzyme replacement therapies.
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- Process for the manufacture of functional PFPE derivative
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A process for the manufacture of a functional (per)fluoropolyether derivative comprising at least one triazole group, such process comprising: (1) reacting a (per)fluoropolyether hydroxyl derivative having at least one hydroxyl group [derivative (PFPE-OH)] with an activating agent, to yield an activated (per)fluoropolyether hydroxyl derivative comprising at least one activated hydroxyl group [derivative (a-PFPE-OH)]; (2) reacting said activated (per)fluoropolyether hydroxyl derivative [derivative (a-PFPE-OH)] with at least one azide salt to yield a functional (per)fluoropolyether derivative comprising at least one azido group [derivative (PFPE-N3)]; and (3) reacting said functional (per)fluoropolyether derivative comprising at least one azido group [derivative (PFPE-N3)] with a hydrocarbon compound having a terminal alkyne group to yield a functional (per)fluoropolyether derivative comprising at least one triazole group [derivative (PFPE-azole)].
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- Compounds and Methods for Treating Mammalian Gastrointestinal Microbial Infections
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Described herein are compounds, and pharmaceutically acceptable salts and prodrugs thereof, which are useful as inhibitors of IMPDH. In certain embodiments, a compound of the invention selectively inhibits a parasitic IMPDH versus a host IMPDH. Further, the invention provides pharmaceutical compositions comprising one or more compounds of the invention. The invention also relates to methods of treating various parasitic and bacterial infections in mammals. Moreover, the compounds may be used alone or in combination with other therapeutic or prophylactic agents, such as anti-virals, anti-inflammatory agents, antimicrobials and immunosuppressants.
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- Olefin Polymerization Catalysts
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The invention relates to transition metal complexes comprising a metal of group 3, 4, or 6 of the Periodic Table of the Elements and one, or two mono-anionic triazole ligands It has been found that these transition metal complexes which comprise at least one triazole fragment having a substituent with an unsaturated fragment are suitable as precatalysts for the polymerization of olefins. In these complexes one carbon atom of the unsaturated fragment is bound directly or via a bridge to a triazole group and the other carbon atom is bound to the transition metal. The complexes are useful as catalysts for olefin polymerization, a catalyst system comprising these complexes and a process for the polymerization of olefins under the use of the catalyst system.
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- Polytriazoles constructed by 1,3-dipolar cycloaddition
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A process of synthesizing hyperbranched polytriazoles, linear and hyperbranched poly(aroyltriazoles) by Huisgen 1,3-dipolar cycloaddition. The polytriazoles were prepared by A2+B3 method to avoid self-polymerization during monomer pr
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- Indazole compounds, compositions thereof and methods of treatment therewith
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This invention is generally directed to the use of Indazole Compounds for treating or preventing diseases associated with protein kinases, including tyrosine kinases, such as proliferative diseases, inflammatory diseases, abnormal angiogenesis and diseases related thereto, atherosclerosis, macular degeneration, diabetes, obesity, pain and others. The methods comprise the administration to a patient in need thereof of an effective amount of an indazole compound that inhibits, modulates or regulates tyrosine kinase signal transduction. Novel indazole compounds or pharmaceutically acceptable salt thereof are presented herein.
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- Substituted azole acid derivatives useful as antidiabetic and antiobesity agents and method
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Compounds are provided which have the structure wherein Q is C or N; R2a, R2b, R2c, X1 to X7, R1, R2, R3, R3a, R4, A, Y, m, and n are as defined herein, which compounds are useful as antidiabetic, hypolipidemic, and antiobesity agents. The present invention further provides a method for treating obesity and dyslipidemia in mammals including humans through simultaneous inhibition of peroxisome proliferator activated receptor-γ (PPARγ) and stimulation of peroxisome proliferator activated receptor-α (PPARα).
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- Methods for treating an inflammatory condition or inhibiting JNK
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This invention is generally directed to Indazole Derivatives having the following structure: 1 or pharmaceutically acceptable salt thereof, wherein R1, R2 and A are as defined herein. Such compounds have utility in the treatment of a wide range of diseases and disorders that are responsive to JNK inhibition, such as an inflammatory disease or disorder. Thus, methods of treating such diseases and disorders are also disclosed, as are pharmaceutical compositions containing one or more compounds of the above compounds.
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- Compounds and methods of treating cell proliferative diseases
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The present invention relates to compounds and their uses, particularly in the pharmaceutical industry. The invention discloses compounds having anti-proliferative activities, as well as methods for treating various diseases associated with abnormal cell proliferation, including cancer, by administering said compounds. It further deals with pharmaceutical compositions comprising said compounds, more particularly useful to treat cancers.
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- Compounds and methods
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Compounds of this invention are non-peptide, reversible inhibitors of type 2 methionine aminopeptidase, useful in treating conditions mediated by angiogenesis, such as cancer, haemangioma, proliferative retinophathy, rheumatoid arthritis, atherosclerotic
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- Substituted 1,2,3-triazolo[1,5-a]quinazolines for enhancing cognition
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The present invention provides a compound of formula (I) in which R1 is generally hydrogen or CF3, R2 is generally hydrogen, W is a cyclic amine, a heterocycle or a group L-Y-X where L-Y is a linking portion and X is generally an aromatic or non-aromatic heterocycle, alkyl or alkylcarbonyl and Z is generally a heterocycle such as 5-methylisoxazol-3-yl, and pharmaceutically acceptable salts thereof for enhancing cognition in conditions such as Alzheimer's Disease, pharmaceutical compositions comprising them, their use for manufacturing medicaments and methods of treatment using them.
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- Ligands of melanocortin receptors and compositions and methods related thereto
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Compounds which function as melanocortin receptor ligands and having utility in the treatment of melanocortin receptor-based disorders. The compounds have the following structure (I): including stereoisomers, prodrugs, and pharmaceutically acceptable salts thereof, wherein A, m, n, R1, R2, R3a, R3b, R4, R5, R6 W1, W2, W3, W4, Y1, Y2, Y3 and Y4 are as defined herein. Pharmaceutical compositions containing a compound of structure (I), as well as methods relating to the use thereof, are also disclosed.
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- Trisubstituted heterocyclic compounds and their use as fungicides
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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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- Substituted amino methyl factor Xa inhibitors
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The present application describes substituted-aminomethyl substituted compounds and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa.
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- Triazole compounds with dopamine-D3-receptor affinity
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Triazole compounds of the following formula where R1, R2, A and B have the meanings given in the description are described. The compounds according to the invention possess a high affinity for the dopamine D3receptor and can therefore be used for treating diseases which respond to the influence of dopamine D3ligands.
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- Substituted azole acid derivatives useful as antidiabetic and antiobesity agents and method
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Compounds are provided which have the structure wherein Q is C or N; R2a, R2b, R2c, X1 to X7, R1, R2, R3, R3a, R4, A, Y, m, and n are as defined herein, which compounds are useful as antidiabetic, hypolipidemic, and antiobesity agents. The present invention further provides a method for treating obesity and dyslipidemia in mammals including humans through simultaneous inhibition of peroxisome proliferator activated receptor-γ (PPARγ) and stimulation of peroxisome proliferator activated receptor-α (PPARα).
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- Substituted azole acid derivatives useful as antidiabetic and antiobesity agents and method
-
Compounds are provided which have the structure wherein Q is C or N; R2a, R2b, R2c, X1 to X7, R1, R2, R3, R3a, R4, A, Y, m, and n are as defined herein, which compounds are useful as antidiabetic, hypolipidemic, and antiobesity agents. The present invention further provides a method for treating obesity and dyslipidemia in mammals including humans through simultaneous inhibition of peroxisome proliferator activated receptor-γ (PPARγ) and stimulation of peroxisome proliferator activated receptor-α (PPARα).
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- Cyclopentyl modulators of chemokine receptor activity
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The present invention is directed to compounds of the formula I: (wherein R1, R2, R3, R4, R5, R6 and X are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.
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- Heteroaryl-phenyl substituted factor Xa inhibitors
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The present application describes heteroaryl-phenyl substituted compounds and derivatives thereof, or pharmaceutically acceptable salt or prodrug forms thereof, which are useful as inhibitors of factor Xa.
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- Heteroaryl- phenyl heterobicyclic factor Xa inhibitors
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The present application describes heteroaryl-phenyl heterobicycles and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa.
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- 3-(substituted pyridyl)-1,2,4-triazole compounds
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Compounds of the formula wherein one of X and Y is lower alkyl, haloalkyl, lower alkenyl, lower alkynyl, or alkoxyalkyl; and the other of X and Y is optionally substituted phenyl, pyridyl, thienyl, cyclopropyl, or thiazolyl; and Z is subtituted pyridyl are useful as insecticides and acaricides. New synthetic procedures and intermediates for preparing the compounds, pesticide compositions containing the compounds, and methods of controlling insects and mites using the compounds are also provided.
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- Indazole derivatives as JNK inhibitors and compositions and methods related thereto
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Compounds having activity as selective inhibitors of JNK are disclosed. The compounds of this invention are indazole derivatives having the following structure: wherein R1, R2 and A are as defined herein. Such compounds have utility in the treatment of a wide range of conditions that are responsive to JNK inhibition. Thus, methods of treating such conditions are also disclosed, as are pharmaceutical compositions containing one or more compounds of the above compounds.
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- Synthesis of N-vinyl-1,2,3-triazole derivatives
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Nitro-substituted N-vinyl-1,2,3-triazole derivatives were synthesized by the vinyl exchange reaction. The process was promoted by the catalytic system mercury(II) acetate-trifluoroacetic acid. This system is universal, and it can be used in the synthesis of vinylazoles having two, three, and four nitrogen atoms in the ring.
- Kizhnyaev,Pokatilov,Tsypina,Ratovskii,Vereshchagin,Smirnov
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p. 1056 - 1059
(2007/10/03)
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- Benzimidazolinones, benzoxazolinones, benzopiperazinones, indanones, and derivatives thereof as inhibitors of factor Xa
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The present application describes inhibitors of factor Xa of formula I: or pharmaceutically acceptable salt forms thereof, wherein W, W1, W2, and W3may be N or C and J, Ja, and Jbcombine to form a substituted carbocycle or heterocycle.
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- Substituted thiadiazolesulfonamides
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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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- 6-membered aromatics as factor Xa inhibitors
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The present application describes 6-membered aromatics of formula I: or pharmaceutically acceptable salt forms thereof, wherein D may be CH2NH2 or C(=NH)NH2, which are useful as inhibitors of factor Xa.
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- Triazole derivatives
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Triazole derivatives represented by formula (IIA), and salts and prodrug thereof, wherein R1 represents C1-6 alkoxy(C1-6)alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-7 cycloalkyl, C3-7 cycloalkyl(C1-6)alkyl, aryl, aryl(C1-6)alkyl, aryloxy(C1-6)alkyl, aryl(C2-6)alkenyl, aryl(C2-6)alkynyl, C3-7 heterocycloalkyl(C1-6)alkyl, heteroaryl, heteroaryl(C1-6)alkyl, heteroaryl(C2-6)alkenyl or heteroaryl(C2-6)alkynyl, any of which groups may be optionally substituted; are selective agonist of 5-HT1 -like receptors and are therefore useful in the treatment of clinical conditions, in particular migraine and associated disorders, for which a selective agonist of these receptors is indicated. STR1
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