579 results about "Benzonitrile" patented technology

Pharmaceutical compositions comprising 2-[6-(3-Amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethyl]-4-fluoro-benzonitrile and pharmaceutically acceptable salts thereof are provided as well as kits and articles of manufacture comprising the pharmaceutical compositions as well as methods of using the pharmaceutical compositions.

Pharmaceutical compositions comprising 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-benzonitrile and pharmaceutically acceptable salts thereof are provided as well as kits and articles of manufacture comprising the pharmaceutical compositions as well as methods of using the pharmaceutical compositions.

The invention discloses a method for synthesizing 4-(3-chloro-4-fluorophenylamino)-7-methoxy -6-[3-(4-morpholinyl)-propoxy] quinoline. The method comprises the following steps: 1) 3-hydroxide radical-4-methoxybenzaldehyde is used as a raw material to prepare 3-hydroxide radical-4-methoxy-benzonitrile; 2) the 3-hydroxide radical-4-methoxy-benzonitrile and 3- chloropropy morpholinehydrochloride are heated to have reflux reaction to obtain 4- methoxy-3-[3-(4- morpholinyl) propoxy] benzonitrile; 3) the 4- methoxy-3-[3-(4-morpholinyl) propoxy] benzonitrile is subjected to nitration to obtain 2- nitryl-4- methoxy -5-[3-(4-morpholinyl) propoxy] benzonitrile; 4) the 2- nitryl-4- methoxy -5-[3-(4-morpholinyl) propoxy] benzonitrile is subjected to reduction to obtain 2-amido-4- methoxy-5-[3-(4-morpholinyl) propoxy] benzonitrile; and 5) the 2-amido-4- methoxy-5-[3-(4-morpholinyl) propoxy] benzonitrile and an azomethine intermediate of 3-chloro-4-fluoroaniline have rearrangement reaction to obtain 4-(3-chloro-4-fluorophenylamino)-7-methoxy-6-[3-(4-morpholinyl)-propoxy] quinoline. The method has characteristics of environmental protection and high production rate.

The invention discloses an improved process for producing 4-(1H-1,2,4-triazol-1-ylmethyl)benzonitrile of Formula (Structure 2), an intermediate used in the manufacture of 4,4′-[1H-1,2,4-triazol-1-ylmethylene] bisbenzonitrile (Letrozole), the process comprising of reacting salt of 1,2,4-triazole of Formula (Structure 4) with α-halo substituted tolunitrile of Formula (Structure 3) in presence of dimethylformamide, wherein the X represents alkali metals selected from a group of Li, Na, or K, preferably Na and Y represents a halogen group selected from Cl, Br or I, preferably Br.

The invention relates to an industrial production method for semi-crystal poly(aromatic ether nitrile), which belongs to the field of polymer material. The method comprises the following steps: 2, 6-dichloro benzonitrile and hydroquinone are taken as raw materials; anhydrous potassium carbonate is taken as a catalyst; in the presence of a solvent and a dehydrating agent, the raw materials and the catalyst react under atmospheric pressure to obtain the poly(aromatic ether nitrile) homopolymer with low molecular weight and regular chain segments; and then the molecular weight of polymer is increased through pressurization, so as to obtain the semi-crystal poly(aromatic ether nitrile) polymer with high molecular weight. Due to the increase of crystallinity and molecular weight, the mechanical properties and heat resistance of the semi-crystal poly(aromatic ether nitrile) polymer are obviously improved.

The invention provides a high-yield process for the preparation of letrozole having a high purity, without the need for removal of the 4-[1-(1,3,4-triazolyl)methyl]benzonitrile impurity at the intermediate stage. The invention also provides a process for the synthesis of letrozole in which formation of the impurity 4-[1-(1,3,4-triazolyl)methyl]benzonitrile during the first stage is minimized. In the process, a 4-(halomethyl)benzonitrile is reacted with a salt of 1H-1,2,4-triazole, reducing the formation of the impurity. Preferably, the preparation is conducted as a one-pot process.

The invention relates to a class of carbazole compounds, and synthesis and application thereof in OLEDs (Organic Light-Emitting diodes). A method for synthesizing the series of carbazole compounds in one step is developed, wherein raw materials are cheap and easily available, noble metal catalysts are not needed, the operation is simple, the reaction conditions are mild, the production is low in cost and high in yield, and commercialization can be conveniently realized. The invention relates to the field of organic electroluminescence materials, and in particular relates to a material with bipolar carrier transporting performance, which is synthesized by a one-step method, and preparation of organic electroluminescence devices by using the material as an electrophosphorescence body. The material with the bipolar carrier transporting performance contains both carbazole units with hole transport performance and benzonitrile or benzophenone units with electron transport performance, i.e. n-CzCN and n-CzCO compounds.

The invention provides a synthesis method of crisaborole, belongs to the technical field of drug synthesis, and relates to a synthesis method of a novel boron-containing anti-inflammatory preparation, namely crisaborole. 4-halobenzonitrile and benzo[c][1,2] oxaborolane-1,5(3H)-diol are reacted in an organic solvent in the presence of alkali, and the crisaborole is obtained. The synthesis methoid is simple, and the crisaborole is high in yield and high in purity. (The reaction formula is shown in the description).

The invention relates to a carrier transmission material which is a thermal activation delayed fluorescence material. The thermal activation delayed fluorescence material is selected from compounds formed by matching benzonitrile and carbazole or triphenylamine and compounds formed by matching triazine and carbazole, indole carbazole or triphenylamine. The carrier transmission material, namely thethermal activation delayed fluorescence material (TADF) is small in energy gap among mono-triplet state and high in triplet state, and excitons can be avoided being diffused to a carrier transmissionlayer from an organic light-emitting layer, so that light-emitting efficiency is improved. In addition, the carrier transmission material is high in glass transition temperature Tg and thermostability. Due to bipolarity, electron and hole transmission capacity of the carrier transmission material can be adjusted conveniently by adjusting number and proportion of donor groups and receptor groups.The invention further provides a carrier transmission layer and an organic light-emitting device.

The invention discloses a side group sulfonic acid polyarylether material, a method for preparing the same and application thereof, which belong to the technical field of functional polymer materials. In particular, the method comprises the following steps: performing polycondensation reaction of 2, 5-diphenyl-hydroquinone and dual-halogen monomers such as 4, 4'-difluoro-benzophenone, 4, 4'-difluoro-diphenylsulfone, 2, 6-difluoro-benzonitrile and the like as well as other diphenol monomers, and then preparing a series of side group sulfonic acid polyarylether proton exchange membranes with controllable sulfonation point and sulfonation degree by a moderate post-sulfonation method. The proton exchange membranes prepared by the method have the advantages of high thermal stability, good solubility and film-forming property, excellent hot water dimensional stability, low methanol permeability and high proton conductivity. The membrane materials used by the method have the advantages of simple preparation process, mild and controllable reaction, wide application temperature and excellent performance, thus the membrane materials can be applied to proton exchange membrane fuel cells and direct methanol fuel cells.

The invention refers to a synthetic method of insect growth regulator of substituted benzoyl urea and to be specific involves the synthetic method of fluorin bell urea, fluorin insect urea and diflubenzuron. It chooses the 2, 6-difluoro benzonitrile as the starting material and gets the compound of the substituted benzoyl urea after fluorination, hydrolysis, esterification and addition. The method adopts the potasium fluoride with high activity and quaternary ammonium salt as the catalyzer during the fluorination, which shortens the time of the fluorination reaction greatly, chooses the base catalysis during the hydrolysis, which reduces the special requirement to the equipment, uses the phosgene instead of the oxalyl chloride during the esterification to decrease the reaction cost and employs the catalyzer during the addition to increase the yield of the reaction. The invention is featured by the high yield, simple steps and cheap raw material and is more adaptable to the scale of the industrial production. Through the method, the yield of the diflubenzuron is 97%, which of the fluorin bell urea 93% and that of the fluorin insect urea 86%.

The invention relates to compounds of the formula (I), wherein R1, R2, X and Y have the meaning specified in claim 1, are inhibitors of TBK1 and IotaKappaKappaepsilon, and can be used, inter alia, for the treatment of cancer and inflammatory diseases.

The present invention is directed to a new class of 4-oxo-benzonitriles, their use as androgen modulators, and to their use in the treatment of alopecia.

Pharmaceutical compositions comprising 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-benzonitrile and pharmaceutically acceptable salts thereof are provided as well as kits and articles of manufacture comprising the pharmaceutical compositions as well as methods of using the pharmaceutical compositions.

The invention discloses a defect type covalent triazine framework material derivative material catalyst and a preparation method and application thereof. A preparation process of the catalyst comprises the following steps: dissolving a benzonitrile compound and a pyridine derivative in a first organic solvent; adding strong acid, carrying out heating and refluxing reaction under the condition of oil bath; cooling to the room temperature after the reaction is finished, and pouring a cooled reaction solution into ultrapure water; adjusting the pH to be neutral by adding alkali, and carrying outsuction filtration; washing filter residues, and then drying the filter residues to obtain defect type covalent triazine framework carrier powder; placing the obtained powder, a cyano derivative and ruthenium metal salt into a mortar; adding absolute ethyl alcohol, and uniformly grinding until the absolute ethyl alcohol is completely volatilized; drying, and then carrying out high temperature calcination under protection of inert gas; and washing and drying the calcined product with ultrapure water to obtain the defect type covalent triazine framework material derivative material catalyst. Thecatalyst has a high specific surface area and a porous structure, supported ruthenium metal particles are small, the metal ion dispersity is high, and a catalytic hydrogen evolution reaction effect is good.

The invention discloses 2-((2-(3-aminopiperidine-1)-4-oxythiophene (3, 2-d) pyrimidine-3(4H)-methyl) polymorphic benzonitrile, and a preparation method and pharmacological applications thereof. Compared with the prior art, the polymorphic benzonitrile has the advantages of high DPP4 (dipeptidyl peptidase-4) inhibitory activity, high in-vivo sugar reducing activity and fine pharmacokinetic characteristics, and is especially suitable for treatment of type 2 diabetes mellitus.

The invention provides a process method for producing high-purity chlorothalonil. The process method has the characteristics of comprising the steps of: sending raw materials containing chlorothalonilm-phthalodinitrile, trichloro-m-phthalodinitrile, pentachloro benzonitrile, hexachloro benzene and water to a light-component removing tower, collecting a mixture of the chlorothalonil containing light components with a mass fraction of <= 0.01% with heavy components from the tower bottom of the light-component removing tower, sending the mixture to a product tower, and collecting the chlorothalonil product with a mass fraction of >= 99.5% from the tower top of the product tower. According to the process method for producing the high-purity chlorothalonil, a rectification process method is adopted to refine the chlorothalonil, the operation process is simple, and the chlorothalonil product with a mass fraction of 99.5% or above can be obtained.

A regiospecific process for the preparation of 4-[1-(4-cyanophenyl)-1-(1,2,4-triazol-1-yl)methyl]benzonitrile comprising reacting 4-halomethylbenzonitrile with 4-amino-1,2,4-triazole followed by deamination and reaction with 4-fluorobenzonitrile.

The present invention is directed to a new class of 4-cycloalkoxy benzonitriles and to their use as androgen receptor modulators. Other aspects of the invention are directed to the use of these compounds to decrease excess sebum secretions and to stimulate hair growth.

The present invention belongs to chemistry technology field, in particular to a method to synthesize lactone compound with cyclone oxide which is an environmental friendly catalyst. The present invention adopts a composite metal oxide MgO / SnO2compound as the catalyst, adopts hydrogen peroxide as the oxidant, and Benzonitrile together with 1,4-bensodioxanes as the solvents, then the cyclone oxide is catalyzed to synthesize the lactone compound in a specific reaction temperature. The present invention uses ketone adamantine, cyclohexanone, and cyclopentanone available in the market, and the yield can be as high as 90 percent in the mild condition. Meanwhile, because of the hydrogen peroxide adopted ad the oxidant, the oxidation methods in prior art is avoided such as peracid, all of which cause environmental problem, and the aim of environmental friendly catalyzing / conversion is accomplished. The present invention is low in price, but has suitability for industrialized production of lactone compound.

Pharmaceutical compositions comprising 2-[6-(3-Amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethyl]-4-fluoro-benzonitrile and pharmaceutically acceptable salts thereof are provided as well as kits and articles of manufacture comprising the pharmaceutical compositions as well as methods of using the pharmaceutical compositions.

The invention claimed herein relates to an improvement in a process for synthesizing a compound of formula Ib:wherein R1 and R2 are each individually amino or N-alkyl substituted amino; hydroxy; alkoxy; keto; lower alkyl; or a nitrogen or oxygen protecting group;R3 is hydrogen; hydroxy; alkoxy; trifluoromethyl alkoxy; halo; sulfhydryl or alkylthio;R4 is —C(O)—X;X is hydroxy; alkoxy; or an amino acid residue;in which process a 2-amino-5-nitro-benzonitrile starting reagent is cyclized to form 2,4-diamino-6-nitro-quinazoline, which is converted to 2,4,6-triamino-quinazoline, which is converted to 2,4-diamino-6-cyano-quinazoline, which is converted to 2,4-diamino-6-formyl-quinazoline;in which the improvement includes:reacting an R4-p-benzoic acid alkylene moiety with triethyl phosphite to form a 4-R4-carbonyloxyalkyl-phenyl-alkyldiethylphosphite; andreacting the 2,4-diamino-6-formyl-quinazoline with the 4-R4-carbonyloxyalkyl-phenyl-alkyldiethylphosphite to form the compound of formula Ib.

A synthesis method of a compound used to form a self-assembled monolayer used in a semiconductor component is provided. A method includes a first step of replacing a terminal halogen of an ω-haloalk-1-ene with a compound having at least one aromatic group, and a second step of hydrosilylating the reaction product of the first step. Reaction products of the first step include octadec-17-enyloxybenzene, 4-octadec-17″-enyloxy-1,1′-biphenyl, 2-heptadec-16′-enylthiophene, and 2-octadec-17′-enylthiophene. Monolayers provided include 18-phenoxyoctadecyl)trichlorosilane, [18-(1′,1″-biphenyl-4′-yloxy)octadecyl]trichlorosilane, (17-thien-2′-ylheptadecyl)trichlorosilane, (18-thien-2′-yloctadecyl)trichlorosilane, and 4-(18′-trichlorosilyloctadecyloxy)benzonitrile. An organic field effect transistor having monolayers according to embodiments of the invention is provided.

The invention discloses a preparation method of an anti-inflammatory drug boron-containing small molecule 4-(1-hydroxy-1,3-dihydrobenzo[c][1,2]oxaborole-5-yloxy)benzonitrile (compound I). The preparation method comprises that a compound II is used as a starting material and reacts with borate in an organic solvent in the presence of a strong alkali to generate a boric acid intermediate, and a ringclosure reaction is continuously performed without separation to prepare the compound I through a one-pot method. According to the present invention, the compound I is prepared through the one-pot method, such that the cumbersome steps of protection and deprotection are avoided, and the method has advantages of simple operation, environmental friendliness and obvious cost advantage, and is suitable for industrial large-scale production. The formulas I and II are defined in the specification.

The present invention discloses crystalline particles of escitalopram oxalate which either have a broad particle size distribution or comprise at least 0.01% (w / w) of Z-4-(4-dimethylamino-1-(4-fluorophenyl)-but-1-enyl)-3-hydroxymethyl-benzonitrile, said particles being suitable for use in direct compression. Furthermore, the invention discloses a novel pharmaceutical unit dosage form containing such crystalline particles of escitalopram oxalate as well as methods for manufacture of such crystalline particles of escitalopram oxalate Finally, the invention provides a method for reduction of the amount of hydroxyl containing impurities in a solution of citalopram or escitalopram.

The invention belongs to the field of medicament synthesis, and particularly relates to a method for preparing tartrate. The method comprises the following steps of: dissolving an (RS)-4-[4-dimethylamino-1-(4-fluorophenyl)-1-hydroxybutyl]-3-(hydroxymethyl) benzonitrile (I) oily matter into isopropyl alcohol; adding water; controlling temperature; stirring and adding D-(+)-Di-para-toluoyl-tartaric acid (D-DTTA) (II); after a reaction liquid becomes transparent, continuing to stir to crystallize, filtrating, washing and drying to obtain a crude (S)-4-[4-dimethylamino-1-(4-fluorophenyl)-1-hydroxybutyl]-3-(hydroxymethyl) benzonitrile hemi-D-(+)-Di-para-toluoyl-tartaric acid (III) product; heating the crude (S)-4-[4-dimethylamino-1-(4-fluorophenyl)-1-hydroxybutyl]-3-(hydroxymethyl) benzonitrile hemi-D-(+)-Di-para-toluoyl-tartaric acid (III) product in methanol to melt; controlling temperature; dropwise adding isopropyl alcohol to crystallize; decreasing temperature, carrying out suction filtering, washing and drying to obtain the fine product. The method is easy to operate, and the prepared tartrate is high in purity and yield.

Cyanoacrylate-containing compositions that include, in addition to the cyanoacrylate component, a hydrogenated anhydride and optionally a benzonitrile, are provided. Cured products of the inventive cyanoacrylate compositions demonstrate improved heat resistance without compromising fixture time, stability or color.

The invention discloses a method for preparing cyanobenzene by ammonifying benzoic acid gaseous phase. The method comprises the following steps: mixing gaseous benzoic acid and an ammonifying agent and carrier gas, and performing catalysis through a catalyst fixed bed, wherein the mol ratio of the benzoic acid to the ammonifying agent to the carrier gas is 1: (1-5): (5-40); the adopted carrier gas can be reaction raw material gas or inert gas, a condenser is arranged behind the reactor, the crude product is condensed to separate out the water phase, and then the rectifying and purifying are performed. The reaction flow is simple, the cyanobenzene is prepared by ammonifying the benzoic acid gaseous phase, the three wastes are prevented, and the economic benefit and the environment benefit are obvious.

The invention provides a preparation method of 2,4,6-trifluorobenzylamine. The preparation method comprises the following steps: S1, by taking pentachloro benzonitrile as a starting material, adding the pentachloro benzonitrile into anhydrous potassium fluoride for fluorination reaction in a first organic solvent, thus obtaining 3,5-dichloro-2,4,6-trifluoro-cyanophenyl; S2a, adding the 3,5-dichloro-2,4,6-trifluoro-cyanophenyl prepared in the step S1 into a second organic solvent, adding organic alkali, feeding hydrogen, and carrying out dehydrochlorination reaction under the action of a firstcatalyst, thus obtaining 2,4,6-trifluoro-cyanophenyl serving as an intermediate; S3, adding the 2,4,6-trifluoro-cyanophenyl prepared in the step S2a into a third organic solvent, adding acid, feedinghydrogen, and reducing the 2,4,6-trifluoro-cyanophenyl serving as the intermediate through a cyanogroup under the action of a second catalyst, thus obtaining 2,4,6-trifluorobenzylamine. By the adoption of the technical scheme, the preparation method has the advantages that steps of a synthesis route are simple and short, conditions are mild, operation is simple and convenient, the raw materials are low in cost and readily available, and the production cost is low; the catalysts and solvents can be recycled for use, so that pollution is reduced; the preparation method is environmentally friendly and suitable for industrial large-scale production.