- CRYSTAL FORMS OF THIOPHENE DERIVATIVES
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Disclosed is crystal form I of compound (S)—N-[5-[1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl]-4,6-dioxo-5,6-dihydro-4H-thieno[3,4-c]pyrrole-1-yl]acetamide.
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Paragraph 0266
(2021/05/14)
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- Method for synthesizing isovanillin
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The invention provides a method for synthesizing isovanillin, and belongs to the technical field of chemical engineering. The method for synthesizing isovanillin comprises the steps of (1) conducting a methylation reaction, specifically, adding ethyl vanillin, dimethyl sulfoxide, Pd (OAc) 2 and a sodium hydroxide solution into a reaction kettle, carrying out oxygen replacement, controlling the oxygen pressure at 0.2 MPa, reacting at the temperature of 100 DEG C for 6 hours, ending the reaction, and filtering and separating the reaction liquid to obtain an oil-phase intermediate; (2) conducting a hydrolysis reaction, specifically, adding the oil-phase intermediate, a SO4/ZrOTiO2 catalyst and water into the reaction kettle, reacting at the temperature of 65 DEG C, and ending the reaction; carrying out suction filtration on the reaction liquid, dissolving a filter cake with 2000g of ethanol, carrying out heat preservation stirring at the temperature of 60 DEG C for 2-6 hours, and carrying out suction filtration; cooling the filtrate to 0 DEG C, preserving heat and stirring for 2-6 hours, and performing suction filtration to obtain a wet product; and drying the obtained solid in vacuum until the weight is constant to obtain the isovanillin.
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Paragraph 0019; 0022-0030; 0040; 0042-0044
(2021/07/31)
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- AMINO ACID DERIVATIVES FOR THE TREATMENT OF INFLAMMATORY DISEASES
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The present disclosure provides certain amino acid derivatives that inhibit NF-kB activation and are therefore useful for the treatment of inflammatory diseases. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
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Page/Page column 47
(2020/08/13)
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- Synthesis method of 3-ethyoxyl-4-methoxybenzaldehyde
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The invention discloses a synthesis method of 3-ethyoxyl-4-methoxybenzaldehyde. The synthesis method of the 3-ethyoxyl-4-methoxybenzaldehyde is characterized by comprising the following steps: by taking isovanillin and halogenated ethane as raw materials, stirring the isovanillin and the halogenated ethane for reaction in a solvent under the action of alkali and a catalyst, and carrying out filtering, so as to obtain the 3-ethyoxyl-4-methoxybenzaldehyde. The method disclosed by the invention is simple, convenient and safe in reaction operation, and an obtained product is easy to separate; treatments on waste gas, wastewater and solid wastes are easy and feasible; in the reaction process, used equipment is simple, and operation can be carried out without special equipment and conditions ofhigh pressure and high vacuum; the synthesis method is an environmentally-friendly green synthesis process.
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Paragraph 0034-0041
(2018/05/16)
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- New synthesis process for 3-methoxyl-4-ethoxybenzonitrile
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The invention discloses a new synthesis process for 3-methoxyl-4-ethoxybenzonitrile, and relates to the technical field of organic synthesis. The new synthesis process for the 3-methoxyl-4-ethoxybenzonitrile comprises the following steps: taking ethyl vanillin as a raw material, taking N,N-dimethylformamide as a solvent, reacting the raw material and the solvent with potassium carbonate at first to form potassium salt, and reacting the obtained potassium salt with methyl iodide to obtain 3-methoxyl-4-ethoxy-benzaldehyde as an intermediate; adding hydroxylamine hydrochloride in a formic acid solution of the 3-methoxyl-4-ethoxy-benzaldehyde as the intermediate, heating and dehydrating, and carrying out desolventizing and recrystallization to obtain the high-purity 3-methoxyl-4-ethoxybenzonitrile finished product. The ethyl vanillin which is low in cost and is easily obtained as the raw material, aftertreatment operation is simple, and after being recycled, the N,N-dimethylformamide as the solvent can be directly used for other items; the 3-methoxyl-4-ethoxy-benzaldehyde as the intermediate are used for next reaction when not purified, so that purification cost is saved, and yield loss is avoided; and moreover, solid wastes are not produced in the whole process, and the total yield reaches 93.8%.
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Paragraph 0024; 0028; 0031; 0034
(2017/09/01)
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- Synthetic method of 6-Bromoisovanillin
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The invention discloses a synthetic method of 6-Bromoisovanillin. The method comprises the steps of taking ethyl vanillin as a starting material, and preparing the 6-Bromoisovanillin through a methylation reaction, a bromination reaction and an acid decomposition reaction in sequence. After the bromination reaction is finished, first a reacted material is neutralized by using alkali liquor, and then excessive bromine is removed by using sodium thiosulfate. The acid decomposition reaction is first performed at a relatively low temperature, and then is performed at a relatively high temperature. The method provided by the invention takes the ethyl vanillin as the starting material, so the production cost is greatly reduced relative to that of expensive isovanillin. The yield of two steps of the methylation reaction and the bromination reaction can reach more than 95 percent, and more important, the reaction yield of removing ethyl by acid decomposition can reach about 75 percent, so that the total reaction yield can reach 70 percent or more than 70 percent.
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Paragraph 0019; 0026; 0027
(2016/10/17)
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- THIOPHENE DERIVATIVES
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Disclosed is a compound of formula (1), wherein R1, R2, R3, R4, R5, R6, R7 and R8 are as defined in the present application.
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Page/Page column 23
(2012/04/17)
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- METHODS OF TREATING PSYCHOLOGICAL CONDITIONS
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A method and composition for inducing in a subject a tolerance to a psychoactive substance or for treating an abnormal mental condition in a subject. The composition used in the method comprises in one embodiment a 5-HT2B receptor agonist disposed within a pharmaceutically-acceptable vehicle or carrier.
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Page/Page column 11
(2011/01/12)
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- Synthesis of aryl alkyl ethers by alkylation of phenols with quaternary ammonium salts
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Phenolic compounds can be efficiently O-methylated with tetramethylammonium chloride in diglyme or polyethyleneglycol (PEG) at temperatures of 150-160 °C and in the presence of either K2CO3 or NaOH. When applying benzyl-trimethylammonium chloride as a reagent, the benzylation and methylation of phenols occurs, with the benzylation product always predominating. With allyl-substituted phenols as substrates and using NaOH as a base it was possible to achieve both the alkylation and the double-bond isomerization of the allyl group to obtain (E/Z)-propenyl-substituted methyl and benzyl aryl ethers in a single preparative step.
- Maras, Nenad,Polanc, Slovenko,Kocevar, Marijan
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experimental part
p. 29 - 36
(2010/09/05)
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- Microwave-assisted methylation of phenols with tetramethylammonium chloride in the presence of K2CO3 or Cs2CO3
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We have evaluated the potential of using tetramethylammonium chloride (Me4NCl) as an alternative methylating agent for phenols under microwave-assisted conditions. Its chemical behavior was tested in a reaction with 2-naphthol in the presence of various bases and solvents. The method was then applied in 1,2-dimethoxyethane or toluene under heterogeneous conditions for the O-methylation of a series of phenolic compounds. We found that many simple phenols can be methylated in the presence of K2CO3, whereas some other less-reactive phenols require the presence of the more reactive Cs2CO3.
- Mara?, Nenad,Polanc, Slovenko,Ko?evar, Marijan
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experimental part
p. 11618 - 11624
(2009/04/05)
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- PYRIDAZINE DERIVATIVES
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Disclosed are pyridazine derivatives of formula (I), which act as phosphodiesterase IV inhibitors and can be used for treating osteoporosis, tumors, cachexia, atherosclerosis, rheumatoid arthritis, multiple sclerosis, diabetes mellitus, inflammatory processes, allergies, asthma, autoimmune diseases, myocardial diseases, and AIDS.
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- ARYLOXIMES
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The invention relates to aryloximes of formula (I), wherein R1, R2, R3, X and B have the meanings as cited in Claim No. 1. These aryloximes act as phosphodiesterase IV inhibitors and can be used for treating osteoporosis, tumors, cachexia, atherosclerosis, rheumatoid arthritis, multiple sclerosis, diabetes mellitus, inflammatory processes, allergies, asthma, autoimmune diseases, myocardial diseases and AIDS.
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- Compositions containing aromatic aldehydes and their use in treatments
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Disclosed are pharmaceutical and cosmetic compositions containing aromatic aldehyde compounds. Some of the disclosed compositions are useful as topical therapeutics for treating inflammatory dermatologic conditions. Some of the compositions are useful in transdermal and other systemic dose forms for treating other inflammatory conditions in mammals.
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- Process for the preparation of isovanillin
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The present invention relates to a novel process for the preparation of isovanillin. The process for the preparation of isovanillin according to the invention is characterized in that it consists in dealkylation being carried out using a strong acid, selectively in the 3-position, on a 3-alkoxy-4-methoxybenzaldehyde wherein said alkoxy group has at least two carbon atoms.
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- Process for preparing a methoxybenzaldehyde from the corresponding phenolic benzaldehyde
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Described is a genus of compounds defined according to the structure: STR1 (Z) represents one of the moieties STR2 as well as the substantially pure compound defined according to the structure: STR3 and the use thereof for augmenting or enhancing the aroma or taste of consumable materials including foodstuffs, chewing gums, medicinal products, toothpastes, chewing tobaccos, smoking tobaccos, smoking tobacco articles, perfumes, colognes and perfumed articles including solid or liquid anionic, cationic, nonionic or zwitterionic detergents, fabric softeners, fabric softener articles, perfumed articles, hair preparations and the like.
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- Novel compounds, processes and marking systems
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Mono and bis substituted (arylsulfonyl)alkanes useful as color formers, particularly in carbonless duplicating and thermal marking systems, are prepared by the interaction of the appropriate aldehyde or dialdehyde with the appropriate aryl or heterocyclic moiety and the appropriate phenylsulfinic acid in the presence of a catalyst.
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