687 results about "Ethoxidine" patented technology

The present invention provides an apparatus comprising a device and a means for heat transfer comprising a hydrofluoroether heat-transfer fluid wherein the heat transfer fluid is 3-ethoxy-perfluoro(2-methylhexane). Another embodiment of the present invention is a method therefor.

Stereomerically pure (+)-2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, substantially free of its (-) isomer, and prodrugs, metabolites, polymorphs, salts, solvates, hydrates, and clathrates thereof are discussed. Also discussed are methods of using and pharmaceutical compositions comprising the (+) enantiomer of 2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione are disclosed. The methods include methods of treating and / or preventing disorders ameliorated by the reduction of levels of TNF-alpha or the inhibition of PDE4.

Prodrugs of parent drugs and methods of making and using the same are described. The prodrugs comprise an amine-containing parent drug moiety and a prodrug moiety, such as methoxyphosphonic acid or ethoxyphosphonic acid. The prodrugs may be employed in therapy for the treatment of various indications, such as pain, and in methods of decreasing the abuse potential of abuse-prone drugs and / or delaying the onset of parent drug activity and / or prolonging parent drug activity as compared to administration of a parent drug.

Topically applicable dermatological / cosmetic compositions suited for ungual / peri-ungual administration for the treatment of a variety of pathologies, including fungal pathologies, such as onychomycosis, contain (a) at least one biologically active agent (e.g., antifungal) and (b) at least two of the pro-penetrating agents selected from the group consisting of urea, an organic acid and an ethoxydiglycol, the at least two-pro-penetrating agents respectively being present in effective amounts as to synergistically improve the ungual / peri-ungual bioavailability of the at least one biologically active agent.

A composition is disclosed for treating the skin comprising an acylated short chain bioactive peptide and Lycium barbarum extract product. Also disclosed is a method for topically administering the composition in an amount therapeutically effective to reduce wrinkles by building the dermal fibroblast matrix. The composition may contain dimethylisosorbide or ethoxydiglycol as solubilizing and penetration enhancers for the hydrophobically modified peptide.

The invention provides novel selective estrogen receptor modulator compounds of the general formula:wherein R1 and R2, which are the same or different area) H, halogen, OCH3, OH; or where X is O, NH or S; and n is an integer from 1 to 4; and R4 and R5, which are the same or different, are a 1 to 4 carbon alkyl, H, -CH2C=CH or -CH2CH2OH; or R4 and R5 form an N-containing five- or six-membered ring or heteroaromatic ring; orc) -Y-(CH2)nCH2-O-R6where Y is O, NH or S and n is an integer from 1 to 4; and R6 is H, -CH2CH2OH, or -CH2CH2Cl; ord) 2,3-dihydroxypropoxy, 2-methylsulfamylethoxy, 2-chloroethoxy, 1-ethyl-2-hydroxyethoxy, 2,2-diethyl-2-hydroxyethoxy or carboxymethoxy; andR3 is H, halogen, OH or -OCH3;stereoisomers thereof and their non-toxic pharmaceutically acceptable salts and esters and mixtures thereof, which compounds exhibit valuable pharmacological properties.

Processes for preparing sulfoxides useful as drugs such as acid secretion inhibitors or antiulcer drugs or intermediates for the preparation of drugs in high yields, at high purities, and with safety. Specifically, a process for the preparation of sulfoxides (II) by oxidizing a thio ether (I) with a peroxoborate salt in the presence of an acid anhydride or a metal catalyst; and a process for the preparation of sulfoxides (II) by oxidizing a thio ether (I) with an N-halosuccinimide, 1,3-dihalo-5,5-dimethyl-hydantoin or dichloroisocyanuric acid salt in the presence of a base. In said formulae R1 is hydrogen, methoxy or difluoromethoxy; R2 is methyl or methoxy; R3 is 3-methoxypropoxy, methoxy or 2,2,2-trifluoroethoxy; and R4 is hydrogen or methyl

The invention relates to a preparation method for synthesizing an apremilast intermediate. The preparation method comprises the following steps of: carrying out condensation reaction on 3-ethoxyl-4-methoxyl-benzoate and dimethyl sulfone under an alkaline condition to generate 2-(3-ethoxy-4-methoxyphenyl)-1-methylsulfonyl acetone; reacting the compound II and chiral amine in the presence of an acidic catalyst to obtain 1-N-substituted amino-1-(3-ethoxyl-4-methoxyl) phenyl-2-methylsulfonyl ethylene (III), and directly hydrogenating the obtained compound III in the presence of a hydrogenation catalyst without separating the compound III to obtain a product (S)-1-(3-ethoxyl-4-methoxyl) phenyl-2-methanesulfonyl ethylamine (I), namely the apremilast intermediate, wherein the apremilast intermediate can be further prepared into N-acetyl L-leucinate. The invention also provides a preparation method of apremilast. The preparation method disclosed by the invention has the advantages of simple process flow, safety, environmental friendliness and low cost and is favorable to clean industrialized production.

The present invention provides a fused heterocyclic compound having an RORγt inhibitory action. The present invention relates to a compound represented by the formula (I′):wherein each symbol is as defined in the specification, provided that 2-(2-((4-cyanophenyl)amino)-2-oxoethoxy)-N-(9-ethyl-9H-carbazol-3-yl)acetamide and N-(4-cyanophenyl)-N′-(9-ethyl-9H-carbazol-3-yl)-3-methylpentanediamide are excluded, or a salt thereof.

To provide the compounds inhibiting PDE 7 selectively, and therefore, enhance cellular cAMP level. Consequently, the compound is useful for treating various kinds of disease such as allergic disease, inflammatory disease or immunologic disease. The compound is pyridinylpyrazolopyrimidinone compound represented by the following formula (IA) or (IB): especially, R1 is cyclohexyl or cycloheptyl group, R2 is methyl; R3 is a group: —NR5R6 or —S(O)0-2R8; hydrogen atom; nitro group; cyano group; a halogen atom; heteroaryl group; and R4 is methoxy or ethoxy group.

The present invention is thickener for heat resistant no-harm fracturing fluid and its preparation process and use. The thickener in the general expression of R1-X-(EO)m(PO)n-Y, where, R1 is long chain hydrophobic group, EO is ethoxy group, PO is 2-oxidized propyl group, m and n are average addition molar numbers, X is linking group ether bond, ester bond or amido bond, Y is hydrophilic group quaternary ammonium group, carboxyl group, sulfuric group or sulfonic group, is prepared through esterification or addition and further reaction. When the thickener is applied, the thickener in 1-3 weight portions and high temperature stabilizer in 0.05-0.4 weight portion are added into base fluid compounded with halogen salt in 2-3 weight portions and water in 100 weight portions to obtain heat resistant no-harm fracturing fluid for increasing yield of oil-gas field.

A composition is disclosed for treating the skin comprising an acylated short chain bioactive peptide and Lycium barbarum extract product. Also disclosed is a method for topically administering the composition in an amount therapeutically effective to reduce wrinkles by building the dermal fibroblast matrix. The composition may contain dimethylisosorbide or ethoxydiglycol as solubilizing and penetration enhancers for the hydrophobically modified peptide.

The invention relates to a preparation method for 4-methyl-5-ethyoxyl-oxazole. The preparation method for the 4-methyl-5-ethyoxyl-oxazole comprises the following steps of: performing cyclization reaction on N-ethoxyl oxalyl alanine ethyl ester under the action of phosphorus oxychloride / triethylamine / dimethylformamide used as a cyclization dehydrating agent at the temperature of between 40 and 60 DEG C for 0.5 to 1 hour; heating to 75 to 100 DEG C and reacting for 5 to 10 hours; hydrolyzing the reaction materials and separating out a water layer; adding an aqueous solution of sodium hydroxide into an organic layer to hydrolyze, adjusting the pH value to be 12 to 14, distilling to obtain ethanol and adjusting the pH value to be 2.0 to 3.0 by adding sulfuric acid; heating to 65 DEG C to perform decarboxylation; adjusting the pH value to 8.0 to 10.0 by using alkali; after chloroform extraction, drying the organic layer by using anhydrous sodium sulfate; and distilling the chloroform under normal pressure to obtain the target product 4-methyl-5-ethyoxyl-oxazole. The process is easy to operate and by the preparation method, industrialized production is easy to realize; the reaction condition is mild, side reaction is few, reaction yield is high and the product content is high; and toxic methylbenzene is not used, so physical health of staff and environmental protection are facilitated.

A surface treated particle comprising a plurality of inorganic, metallic, semi-metallic, and / or metallic oxide particles and a star-graft copolymer with looped and / or linear polymeric structure on a star-graft copolymer, obtainable by a heterogeneous polymerization reaction in the particle surface proximity, encapsulating at least a portion of said particles and a method for making the same. The surface treatment comprises: Si (w, x, y, z), where: w, x, y, and z are mole percent tetrafunctional, trifunctional, difunctional, and monofunctional monomeric units, respectively; w, x, y, and z are about 0-50, 0-50, 5-99, and 0-5, respectively; w is tetraethylorthosilicate; x is selected from the group consisting of γ-glycidoxypropyltrimethoxysilane, γ-methacryloxypropyltrimethoxysilane, methyltrimethoxysilane, n-propyltrimethoxysilane, isobutyltrimethoxysilane, n-hexyltrimethoxysilane, n-octyltrimethoxysilane, n-octadecyltrimethoxysilane, phenyltrimethoxysilane, 3-(trimethoxysilyl)propylsuccinic anhydride, heptadecafluorotrimethoxysilane, 3-isocyanatopropyltrimethoxysilane, 2-(diphenylphosphino)ethyltrimethoxysilane, 3-aminopropyltrimethoxysilane, 3-mercaptopropyltrimethoxysilane, n-(trimethoxysilylpropyl)EDTA, pentafluorophenylpropyltrimethoxysilane, trifluoropropyltrimethoxysilane, and the triethoxy-containing counterparts of these monomers; y is selected from the group consisting of dicyclohexyldimethoxysilane, diethyldiethoxysilane, dimethyldichlorosilane, dimethyldiethoxysilane, dimethyldimethoxysilane, diphenyldiethoxysilane, diphenyldimethoxysilane, di-n-hexyldichlorosilane, n-hexylmethyldichlorosilane, methyldodecyldiethoxysilane, n-octylmethyldimethoxysilane, and the diethoxy-containing counterparts of these monomers; and z is selected form the group consisting of n-octadecyldimethylmethoxysilane, triethylsilanol, trimethylethoxysilane, trimethylmethoxysilane, and the ethoxy-containing counterparts of these monomers. Product(s) per se, defined as surface treated ZnO and / or TiO2, and the use of the product(s) per se in personal care formulations are excluded.

Solid forms comprising (+)-2-[l-(3-Ethoxy-4-methoxyphenyl)-2- methylsulfonylethyl]-4-acetylaminoisoindoline-l,3-dione, compositions comprising the solid forms, methods of making the solid forms and methods of their use are disclosed. The methods include methods of treating and / or preventing disorders ameliorated by the reduction of levels of TNF-alpha or the inhibition of PDE4.

The invention relates to a thermoplastic polyimide (TPI) material used for preparing a two-layer flexible copper clad laminate (2L-FCCL). The excellent dissolvability TPI material is obtained through generating a polyamide acid copolymer by using main reaction components 4-ethoxydiphenol-3,5-diaminobenzoate and 2,2-bis(4-aminophenyl)hexafluoropropane according to a specific molar ratio, a corresponding diamine and a corresponding acid anhydride, and processing the copolymer by utilizing a chemical imidization process. The 2L-FCCL with good comprehensive performances of dimensional stability, dip soldering resistance, peeling performance and the like can be obtained through dissolving powder of the TPI material and compositing the TPI material with a thermosetting polyimide film and copper foil.

The invention relates to a synthesis method of 1-ethoxy-1,3,3,5,5-pentafluorocyclotriphosphonitrile, which comprises the following steps: a. in a catalyst-added organic solvent, substituting six chlorine atoms of hexachlorocyclotriphosphonitrile with fluorate to prepare a hexafluorocyclotriphosphonitrile-containing product, and distilling to remove the byproduct and solvent, thereby obtaining the hexafluorocyclotriphosphonitrile; and b. reacting the hexafluorocyclotriphosphonitrile obtained in the step a with ethylate in a catalyst-added organic solvent to substitute one fluorine atom with one ethoxy group so as to obtain a product containing 1-ethoxy-1,3,3,5,5-pentafluorocyclotriphosphonitrile, and distilling to remove the byproduct and solvent, thereby obtaining the 1-ethoxy-1,3,3,5,5-pentafluorocyclotriphosphonitrile. The synthesis method has the advantages of mild reaction conditions and high reaction controllability, and is convenient for industrial production. The method also has the advantages of simple technical process, low energy consumption, recoverable solvent, higher yield and higher product purity.

The invention provides a multi-functional rubber additive and a method for preparing same. The multi-functional rubber additive has an abovementioned molecular structural formula; wherein, the left side of the formula is provided with a benzothiazolyl radical; R1 is methylene, ethylidene or propylidene; R2 is cymene or ethyl; R3 is ethylidene, propylidene, methoxy or ethoxy. The preparation method comprises the steps as follows: 2-mercaptobenzothiazole (accelerant M) and alkali are dissolved in organic solvent; subsequently, chlorocarbon silane is added and reacts for 0.5-24 hours at the temperature of 20-120 DEG C under the mixing condition; the reaction products are filtrated, washed, and distilled by pressure-reduction so as to gain viscous liquid-shaped target products finally. The multi-functional rubber additive has multi-functions such as plasticizing, dispersing, promoting, reinforcing, and the like, simple preparation flow, high yield and simple separation process.

The invention provides new polymorphs of N—[(R)-1-[(S)-1-(4-aminomethyl-benzylcarbamoyl)-2-phenyl-ethylcarbamoyl]-2-(4-ethoxy-phenyl)-ethyl]-benzamide hydrochloride, pharmaceutical compositions containing them and their use in therapy.

The invention discloses an oxa-phosphaphenanthrene fire retardant as well as a preparation method and application of the oxa-phosphaphenanthrene fire retardant. The fire retardant has a calyx[4]arene structure; p-tert-butyl calyx[4]arene and p-tosylate ethoxy p-benzaldehyde are prepared into an intermediate I in the presence of K2CO3 and acetonitrile, and the intermediate I reacts with DOPO to obtain a target compound; the compound is white in appearance, has the melting point of 198-200 DEG C and the purity of 98.5% and is good in thermal stability and high in flame retarding rate; the used raw materials are easily available, and a process is advanced and easy for industrialized production. The flame retardant not only can serve as a reactive flame retardant to be used in thermosetting resin such as epoxy resin and polyurethane but also can serve as an additive flame retardant to be used for engineering plastics with relatively high requirement on the heat resistance of the flame retardant.

The invention discloses an ethoxydiphenylethane derivative and a synthetic method and uses thereof 4′ position of phenylethane B aromatic ring is chemically modified by ethoxy and hydroxy at position 3′ thereof is simultaneously modified to water soluble prodrug such as phosphate, and similarly, amino acid side chain is introduced to amino at position 3′ to form amino acid amide water soluble prodrug having the structure shown as formula (I)the ethoxydiphenylethane derivative and the prodrug thereof include strong tubulin aggregation inhibiting ability and obvious target damage effect for tumor vessels, selectively cause dysfunction and structural damage of tumor vessels and induce apoptosis of vascular endothelial cells in order to play the role of killing tumor cells or inhibiting tumor metastasis in case that the tumor cells are free from the support of nutrition and oxygen.

The invention provides a preparation method of 2-(2', 2'-difluoroethoxyl)-6-trifluoromethyl phenyl propyl sulfide, having the following processes: reacting m-trifluoromethyl phenol with p-toluenesulfonyl chloride, trifluoromethanesulfonic anhydride or 3, 5-dinitrobenzol sulfonyl chloride in a solvent containing organic base or a solvent containing triethylamine hydrochloride and organic base, andthen, collecting a compound having a formula (III) from reaction products, dissolving the compound in butylene oxide, adding tetramethyl ethylene diamine and diisopropylamine, at a temperature range from -25 DEG C to -100 DEG C, adding butyl lithium cyclohexane solution for reaction, and then, adding dipropyldisulfide, and collecting a compound having a formula (II); reacting the compound having the formula (II) with 4-nitrogen, nitrogen-dimethyl pyridine and difluoroethanol for catalytic reaction in the solvent, and then, collecting a compound having a formula (I) from the reaction products.The invention simplifies reaction conditions, optimizes the technology, reduces production cost, and improves synthesis effects. The general formula of the reaction is as follows.

The invention relates to a catalyst which is used for selecting hydroxymethyl in catalytic phenolic compound to be oxidized into aldehyde group and the preparation method thereof, in particular to a supported catalyst used in vanillin (3-methoxy-4-hydroxy benzaldehyde) compounded by 3-methoxy-4-hydroxy benzalcohol and 3-ethoxy-4-hydroxy benzalcohol and ethyl vanillin (3-methoxy-4-hydroxy benzaldehyde) and the preparation method thereof. The catalyst of the invention with one or more transition metal oxides as active components, which comprises cobalt, molybdenum, aluminum, silver, iron, copper, manganese, nickel, zinc and other oxides; one or more rare earth elements are added to be cocatalysts which comprise praseodymium, lanthanum, scandium, cerium, neodymium, etc., one or more composite materials among alumina, silicon dioxide, titanium dioxide, activated carbon are as carriers. Under the function of the catalyst, 3-methoxy-4-hydroxy benzalcohol can choose to be oxidized into vanillin. After 3-methoxy-4-hydroxy benzalcohol reacts under a temperature of 70 DEG C for 4h, the conversion rate of the 3-methoxy-4-hydroxy benzalcohol is up to 95.4 percent, and the yield rate of vanillin is 83.0 percent. The catalyst has the advantages of low cost, easy separation and recycling use after reaction, simple post-processing, low amount of by-products, friendly environment and wide prospect of industrialization application.

The invention discloses a novel technology for synthesizing an intermediate of trityl candesartan; the synthesis steps thereof comprise: (1) a preparation method of 2-menthyl formate-6-nitryl-benzoic acid; (2) a preparation method of 2-amido-3-nitryl-methyl benzoate; (3) a preparation method of 2, 3-diaminobenzene menthyl formate; (4) a preparation method of 2-oxethyl-4-menthyl formate-3-H-benzimidazole; and (5) the preparation method of the intermediate of trityl candesartan.

The invention provides a 1-(7-ethoxycoumarin)-4-(2-methyl-8-methoxyquinoline)-1, 2, 3-triazole ratiometric fluorescence or ratiometric ultraviolet absorption probe agent and preparation and application thereof, and belongs to the technical fields of organic synthesis and analytic chemistry. The preparation method is characterized in that an intermediate, namely, 2-methyl-8-(propyn-2-yl alkoxy) quinoline, reacts with 7-(2-azidoethoxy)-coumarin to obtain a compound a of which triazolyl is connected with two fluorophores, namely, coumarin and quinoline, wherein the compound is 1-(7-ethoxycoumarin)-4-(2-methyl-8-methoxyquinoline)-1, 2, 3-triazole. The preparation method has the advantages that the reaction raw materials are easy to obtain, the synthesis method is simple, and the compound can be obtained by three-step reaction; the compound a generates ratiometric fluorescence at 480nm and 390nm in alcohol / aqueous solution, and trace Al<3+> can be measured accordingly; ratiometric ultraviolet absorption is produced at 253nm and 243nm, and trace Al<3+> can be measured accordingly. The probe agent is the probe agent being high in sensitivity, high in accuracy and high in selectivity and used for detecting Al<3+> ions through ratiometric fluorescence and ratiometric ultraviolet absorption. The structure formula of the compound a is as shown in the specification.

A compound represented by the formula wherein R<1> and R<2> are the same or different and each is an optionally substituted hydrocarbon group or an optionally substituted hydroxy group; R<3> is an optionally substituted aromatic group; R<4> is an optionally substituted amino group; L is a divalent chain hydrocarbon group; Q is a bond or a divalent chain hydrocarbon group; and X is a hydrogen atom, a cyano group, a nitro group, an acyl group, a substituted hydroxy group, an optionally substituted thiol group, an optionally substituted amino group or an optionally substituted cyclic group; provided that when X is an ethoxycarbonyl group, then Q is a divalent chain hydrocarbon group. The compound has a peptidase inhibitory action, is useful as an agent for the prophylaxis or treatment of diabetes and the like, and is superior in efficacy, duration of action, specificity, lower toxicity and the like.

The invention belongs to the field of medical chemistry, and relates to a preparation method of Bilastine. The preparation method comprises following steps: adding compound 2-[1-(2-{4-[1-(4,4-dimethyl-4,5-dihydro-oxazole-2-yl)-1-methyl-ethyl]-phenyl}-ethyl)-piperidine-4-yl]-1-(2-ethoxy-ethyl)-1H-benzimidazole into water containing organic acid, then subjecting the mixture to a thermal-reflux reaction for 1 to 36 hours, and finally obtaining Bilastine after post-processing. The preparation method has the advantages of mild reaction conditions, simple operation and easy industrialization.

The invention relates to preparation of a medicine, and particularly relates to a crystal form of 2[4-(2-{4-[1-(2-ethoxyethyl)-1H-benzimidazole-2-yl]-piperidine-1-yl}-ethyl)-phenyl]-2-methyl propionic acid and a preparation method. The invention provides a stable bilastine crystal form and a preparation technology scheme thereof. The X-ray powder diffraction 2 theta (+ / -0.2) data of the stable bilastine crystal form are 11.30, 12.50, 17.18, 18.94, 19.80, 21.14, 22.68 and 24.92.