639 results about "Ethoxidine" patented technology

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.

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.

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.

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.

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 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 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 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 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.

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 discused. 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.

The invention relates to a binary compound flooding compound and a preparation method thereof, mainly solving the problems that the oil displacement agent containing surface active agents has poor oil displacement efficiency and high using concentration under the high-temperature and high-salt conditions, and corrosion and scale deposition to a stratum and an oil well, caused by alkali in the ternary compound flooding, happen in the prior art. The binary compound flooding compound comprises the following components in percentage by weight: (1) 0.01-5.0 percent of N,N-bi fatty acyl group diamine neopentanoic acid di-polyoxyethylene ether bisulphonate; (2) 0.01-3.0 percent of polymer; (3) 92.0-99.98 percent of formation water, wherein in the general molecular formula of the component (1), R1 is C9-C17 alkyl group, R2 is C2-C6 alkyl group, n is adding composite number of ethoxy groups (EO) and is one integer from 2-7; M is one metal ion of K, Na or Li; the polymer is selected from one ofpolyacrylamide with superhigh molecular weight (viscosityaverage molecular weight is 25,000,000), temperature-resisting and salt-resisting polymer or xanthogen gum, and water is selected from the formation water of the oil field. By the technical scheme, the problems are better solved, and the binary compound flooding compound is suitable for tertiary oil recovery production in the oil field.

Disclosed is an alkoxy ethoxy propyl isothiazolinone, whose molecule formula is C8H10Cl2NO3SR, the preparation comprises reacting Na2Sx with acrylic methyl ester to obtain dithiodipropionic dimethyl ester, then reacting with alkoxy ethoxy alanine to obtain N, N'-dialkoxy ethoxy propyl dithioamides, and the latter further reacting with sulfuryl chloride. The invention can realize an antifouling agent for rapid degradation in the environment, very small influence to the biological availability for sea creatures can be achieved.

The invention aims at providing a method for more effectively synthesizing dapagliflozin with shorter steps. The method comprises the steps: catalyzing 5-bromo-2-chloro-4'-ethoxybenzophenone serving as a starting material by using a strong acid to finish ketal protection, treating the obtained diaryl ketal compound by using magnesium, then, reacting the treated diaryl ketal compound with trimethylsilyl-protected glucolactone, and reducing a hemiketal compound obtained after dilute acid quenching to finish the preparation of dapagliflozin.