46 results about "Methoxystemofoline" patented technology

The invention belongs to the field of compound preparation, and specifically discloses a preparation method of an anti-tumor medicine chlorambucil. The preparation method comprises the steps of performing a Vilsmeier reaction on a raw material N,N-dihydroxyethylaniline and phosphorus oxychloride and DMF so as to prepare 4-[bi(2-chloroethyl)amino]benzaldehyde, then performing a witting reaction on4-[bi(2-chloroethyl)amino]benzaldehyde and methoxymethyl triphenylphosphonium chloride so as to prepare 4-[bi(2-chloroethyl)amino]-BETA-methoxystyrene, reacting under an acid condition so as to obtain4-[bi(2-chloroethyl)amino]phenylacetaldehyde, and finally, reacting with Meldrum's acid in triethylamine and formic acid systems so as to prepare a target product. The raw material N,N-dihydroxyethylaniline is cheap, has a wide source and is easy to obtain; the whole reaction process has high yield, production conditions are mild, the steps are short, and post treatment and purification are easyto operate, so that the preparation method is applicable to commercial large scale production, and meets the rapidly growing market demands.

The invention relates to a synthetic technology of p-methoxystyrene, which comprises: using p-methoxyhypnone as a raw material, reducing to p-methoxy-alpha-methylbenzylalcohol by a reducing agent, adding a small quantity of weakly acidic catalyst to the p-methoxy-alpha-methylbenzylalcohol, agitating and reacting for a period of time, taking liquid, and flowing the liquid through a tubular reactor under negative pressure to generate the p-methoxystyrene, wherein the tubular reactor is used for replacing the reactor units such as traditional reaction kettles and the like, continuous production can be conveniently carried out and production cost is greatly decreased.

A process for synthesizing 4-methoxy styrene includes reductive reaction of 4-methoxy acetophenone to obtain 4-(4'-methoxyphenyl) ethanol, esterifying reaction to obtain 1-(4'-methoxyphenyl) ethyl sulfonate, abate reaction to obtain 4-methoxy styrene, and vacuum rectifying.

The invention relates to a method for preparing 4-methoxystyrene. The method comprises the following steps: (1) dissolving 4-methoxyacetophenone into an ethanol solvent, adding a reducer and performing reduction reaction to obtain an intermediate 1-(4-methoxyphenyl) ethanol; and (2) performing dehydration reaction on the intermediate obtained in step (1) under the catalysis of a dehydrating agent, and distilling at the same time to obtain a rough 4-methoxystyrene product. The method for preparing the 4-methoxystyrene is readily available in raw materials, simple in process, high in reaction yield and high in product purity, and a polymerization inhibitor is not needed, so that the problems that the requirement for raw materials is strict, the post treatment is difficult, polymerization is easily caused in the reaction, the production is discontinuous, the requirement for production equipment is strict and the like in the existing synthetic method are solved, and the method can be effectively applied to production practice.

The invention provides a synthesis method of resveratrol, and belongs to the technical field of natural product synthesis. The synthesis method comprises the following steps: with 3,5-dimethoxy benzoic acid as a raw material, generating 3,5-dimethoxy benzoyl chloride (12) through an acylating chlorination reaction; generating 3,5-dimethoxy benzamide (13) through an amidation reaction of the (12);generating 3,5-dimethoxyaniline (14) through a Hofmann degradation reaction of the (13); generating 3,5-dimethoxy iodobenzene (15) through a Sandmeyer reaction on the (14); generating 3,5,4'-trimethoxy diphenylethene (31) through a reaction between the (15) and p-methoxystyrene (23), and performing demethylation of the (31) to finally obtain resveratrol (1), wherein total yield is 23.3%. Accordingto the method, the adopted reagent is cheap and easily available, aftertreatment is simple, and two expensive intermediates for Heck reaction are synthesized by adopting cheap raw materials. A new synthesis method is provided for synthesizing resveratrol.

The invention discloses a synthesis process of an apremilast intermediate. The synthesis process comprises the following steps: (a) carrying out reaction on 3-ethoxyl-4-methoxystyrene and methanesulfonyl chloride under the action of a ruthenium catalyst to generate 4-[(1-chloro-2-methylsulfonyl)-ethyl]-2-ethoxyl-1-methoxybenzene; and (b) carrying out reaction on 4-[(1-chloro-2-methylsulfonyl)-ethyl]-2-ethoxyl-1-methoxybenzene and an alcohol liquid of ammonia, so as to obtain 1-(3-ethoxyl-4-methoxyl)phenyl-2-methylsulfonylethylamine. The synthesis process is simple and convenient to operate, and special reaction conditions are not needed, so that the synthesis process is more suitable for industrial production.

The invention discloses 3-methyl-2-(methoxy styrene keto)-quinoxaline-1,4-dioxide and a preparation method thereof. Mequindox and methoxy benzaldehyde are subjected to aldol condensation to generate 3-methyl-2-(methoxy styrene keto)-quinoxaline-1,4-dioxide by adopting a one-step method. Active experiments indicate that 3-methyl-2-(methoxy styrene keto)-quinoxaline-1,4-dioxide has good bacteriostasis activity against escherichia coli, staphylococcus aureus, pseudomonas aeruginosa, bacillus subtilis and the like. Through studies on growth promotion and drug residues, 3-methyl-2-(methoxy styrene keto)-quinoxaline-1,4-dioxide (a) has relatively good effect of promoting growth, and is safe to use. The prepared 3-methyl-2-(methoxy styrene keto)-quinoxaline-1,4-dioxide (a) can be used as a livestock and poultry antibacterial growth-promoting veterinary drug feed additive and can be widely applied.

The invention relates to a preparation method of Ramage linker and mainly solves problems of long processes, complex post-treatment, much waste water, waste gas and solid waste, and high cost in a conventional synthetic method. The preparation method includes following steps: (A) carrying out a reaction to 2-carboxybenzaldehyde and m-methoxyphenylacetic acid to obtain an intermediate 2-(3-methoxylstyryl)benzoic acid, dissolving the intermediate with a solvent, performing hydrogenation reduction, and performing post-treatment crystallization to obtain a compound R-1; (B) carrying out a reaction to the R-1 with SOCl2 or POCl3 to obtain 2-methoxyl-10,11-dihydro-5H-dibenzo[a,d]cycloheptene-5-one, performing negative-pressure evaporation to remove the SOCl2 or the POCl3, dissolving the 2-methoxyl-10,11-dihydro-5H-dibenzo[a,d]cycloheptene-5-one in benzene, methylbenzene or 1,2-dichloroethane, performing a catalytic reaction with anhydrous AlCl3 and performing post-treatment crystallization to obtain a compound R-2; (C) carrying out a reaction to the R-2 with benzyl bromoacetate in DMF or an acetone / K2CO3 solution to obtain a compound R-3; (D) performing hydrogenation reduction to the R-3 to obtain a compound R-4; and (E) adding a catalyic amount of PTS to the R-4 in DMF and carrying out a reaction to the R-4 with Fmoc-NH2 to obtain the Ramage linker, which is an effective C-terminal linker in solid-phase synthesis.

An object of the present invention is to provide a skin temperature elevating agent that can further effectively raise a skin temperature. Another object is to provide a cosmetic composition, a food and a sundry article having a skin temperature elevating effect. A skin temperature elevating agent of the present invention is selected from one or more selected from a group consisting of: an extract of Japanese peppermint; an extract of clary sage; dihydro-β-ionol; and geraniol, and thus it can raise a skin temperature of a cheek. The skin temperature elevating agent according to the present invention is also selected from one or more selected from a group consisting of: an extract of Japanese peppermint; an extract of juniper berry; and 4-methoxystyrene, and thus it can raise a skin temperature of a hand fingertip. Hence, the skin temperature elevating agent according to the present invention can further effectively raise a skin temperature. A composition, a food, and a sundry article according to the present invention contain the skin temperature elevating agent, and thus have the skin temperature elevating effect.

The invention aims to provide a preparation method of Sarpogrelate intermediate 2-((3-methoxy) phenethyl) phenol (I), which comprises the following steps of: 1) carrying out perkin reaction on 3-methoxyphenylacetic acid (II), salicylic aldehyde (III), organic base and acetic anhydride; 2) further obtaining 2-(3-methoxyphenyl)-3-(2-acetoxy-phenyl) acrylic acid (IV); 3) decarboxylating a compound IV under the existence of quinoline and metal copper to obtain 3-methoxy-2'-acetoxy stilbene (V); 4) hydrolyzing the compound IV to obtain 2-((3-methoxy) styryl) phenol (VI); and 5) carrying out catalytic hydrogenation on the compound IV to obtain a compound I. The technical scheme disclosed by the invention has the characteristics of simplicity in operation, mild reaction condition, no hydroxyl protection or deprotection required, easiness for product purification, short synthetic route, easiness for material obtaining, high yield, low cost and the like and has a wide industrial application prospect.

A process for synthesizing 4-methoxy styrene includes reductive reaction of 4-methoxy acetophenone to obtain 4-(4'-methoxyphenyl) ethanol, esterifying reaction to obtain 1-(4'-methoxyphenyl) ethyl sulfonate, abate reaction to obtain 4-methoxy styrene, and vacuum rectifying.

The invention discloses 1,3-bis(2-bromo-5-methoxylstyryl)-2,4,6-trinitrobenzene and a preparation method thereof. The preparation method comprises the following steps: adding 1,3-bis(3-methoxylstyryl)-2,4,6-trinitrobenzene, liquid bromine, and a catalyst into a reactor, taking dichloromethane as the solvent, carrying out reactions at the room temperature, after reactions, filtering, neutralizing the filtrate by a saturated sodium carbonate solution, extracting the filtrate by dichloromethane, carrying out spinning evaporation, and finally drying to obtain 1,3-bis(2-bromo-5-methoxylstyryl)-2,4,6-trinitrobenzene. Each benzene ring on the periphery of 1,3-bis(2-bromo-5-methoxylstyryl)-2,4,6-trinitrobenzene contains a bromine atom, the symmetrical property is good, moreover, the central benzene ring is connected to two other benzene rings through two conjugated double bonds, and thus the stability of the compound is greatly improved. The provided compound can be used to produce functional materials used in the fields such as medicine, pesticide, heatproof materials, and the like.

The invention discloses a synthesis method of resveratrol. The synthesis method comprises the steps of a preparation technology of 3,5-dibromo-4-aminotoluene, a preparation technology of 3, 5-dibromotoluene, a preparation technology of (E)-1,3-dibromo-5-(4-methoxy-styrene)benzene, a preparation technology of (E)-1,3-dimethoxy-5-(4-methoxy-styrene)benzene and a preparation technology of resveratrol. The synthesis method has the advantages of being low in raw material price, less in step, high in yield and suitable for scale production.

The present invention relates to a p-methoxystyrene synthesis process, specifically to production of p-methoxystyrene through gas-solid phase catalysis dehydration of p-methoxyphenethyl alcohol. The synthesis process is a continuous production process, and specifically comprises that: p-methoxyphenethyl alcohol is sucked through a water circulation vacuum pump, the feeding amount is adjusted through an adjustment valve, vaporization is performed with a vaporization device, the obtained material enters a reactor, a catalysis dehydration reaction is performed at a temperature of 275 DEG C, the obtained reaction gas is condensed into a liquid, and the liquid enters a product receiver. According to the present invention, the process has characteristics of simple process, mild process conditions, safe operation, single raw material and product, high selectivity, high yield, no by-product emission, low environmental pollution, simple structure of the required equipment, application of ordinary carbon steel, and no special requirement.

The invention relates to an agrochemical composition used for controlling plant viral diseases. The composition comprises the following components: 30 parts of sodium carbonate, 18 parts of magnesium chloride, 6-18 parts of phenyl ring, 8 parts of polyethylene glycol, 12 parts of styrene, 5 parts of methyl styrene, 3 parts of ethyl styrene, and 1 part of methoxy styrene. The agrochemical composition used for controlling plant viral diseases has a significant synergistic effect, and helps in retarding disease drug resistance. With the composition, production cost and application cost are reduced. The agrochemical composition can be used for controlling resistant diseases. The agrochemical composition is mainly used for controlling viral diseases of various crops such as tobaccos, tomatoes, chilli peppers, melons, paddy rice, wheat, vegetables, fruits, legumes, and the like.

The invention discloses a compound dimethoxystyryl-amino-benzimidazolyl-triazine and salt thereof as well as a preparation method and application. The compound 2-[(E)-3',4'-dimethoxystyryl]-4-amino-[1, 2]-benzimidazolyl-[1, 3, 5]-triazine has a good anti-tumor activity against a plurality of tumor cell lines, and obviously influencesan obvious influence on the tumor cell microtubules, wherein theeffect on the cell microtubules is in positive correlation with the time and the concentration, and the compound has a broad application prospect in the anti-tumor field; meanwhile, the preparation method of the compound 2-[(E)-3',4'-dimethoxystyryl]-4-amino-[1, 2]-benzimidazolyl-[1, 3, 5]-triazine has the advantages of simple technology and low equipment requirements and promotes large-scale production.

Pharmaceutical compositions of (E)-2,4,6-trimethoxystyryl-3-[(carboxymethyl)amino]-4-methoxybenzylsulphone and pharmaceutically acceptable salts thereof are described as well as methods of their use, and a dose regimen of (E)-2,4,6-trimethoxystyryl-3-[(carboxymethyl)amino]-4-methoxybenzylsulphone, sodium salt to reduce the incidence of urothelial toxicity.

The invention relates to a synthesis process of (R,S)-2-[[5-(9- fluorenylmethyloxycarbonylamino)dibenzo[A,D]cycloheptane-2-yl]oxyl]acetic acid. The synthesis process comprises the following steps of firstly, reacting o-phthalalde-hydic acid and m-methoxyphenylacetic acid under the catalysis of anhydrous sodium acetate to obtain 2-(3-methoxyphenylethenyl)benzoic acid, and carrying out a reduction reaction through introducing hydrogen under the catalysis of Pd-C; secondly, reacting the product and SOCl2 to obtain 2-methoxy-10,11-dehydro-5H-dibenzo[a,d]cycloheptene-5-ketone, and carrying out reflux reaction under the catalysis of anhydrous AlCl3; thirdly, reacting an intermediate product obtained through the reflux reaction and bromo-acetic acid phenylmethyl ester; and fourthly, carrying out reduction reaction through introducing hydrogen, then, reacting the product and Fmoc-NH2 to obtain (R,S)-2-[[5-(9- fluorenylmethyloxycarbonylamino)dibenzo[A,D]cycloheptane-2-yl]oxyl]acetic acid. According to the synthesis process, a catalyst is optimized, so that the total yield is remarkably increased, and the cost is reduced effectively; and the synthesis process is suitable for large-scale industrial synthesis application.

The invention discloses a fluorescent probe molecule for pH (potential of hydrogen) detection, which is 2-(4-methoxystyrene) quinoline-6-phenol. The invention further discloses a preparation method ofthe fluorescent probe molecule. The invention further discloses a fluorescent thin-film sensor of the fluorescent probe molecule for pH detection and a preparation method of the fluorescent thin-filmsensor. A glass matrix of the sensor is coated with the fluorescent probe molecule. The preparation method comprises the steps of putting the fluorescent probe molecule in a Nafion solution for uniform mixing to form a film casting liquid, spin-coating the film casting liquid onto the glass matrix, putting the glass matrix in a solvent evaporation chamber, heating to 100-120 DEG C under a high vacuum condition, holding the temperature for 0.5-12h, removing a solvent and obtaining the fluorescent thin-film sensor. The invention further discloses the application of the fluorescent probe molecule and the fluorescent thin-film sensor in detecting the pH value of a solution. A ratio-type fluorescent probe has two fluorescent emission peaks, and can be calibrated by two signal peaks of the fluorescent probe, and the detection accuracy is improved.

The invention discloses a fluorescent probe molecule for pH (potential of hydrogen) detection, which is 2-(4-methoxystyrene) quinoline-6-phenol. The invention further discloses a preparation method ofthe fluorescent probe molecule. The invention further discloses a fluorescent thin-film sensor of the fluorescent probe molecule for pH detection and a preparation method of the fluorescent thin-filmsensor. A glass matrix of the sensor is coated with the fluorescent probe molecule. The preparation method comprises the steps of putting the fluorescent probe molecule in a Nafion solution for uniform mixing to form a film casting liquid, spin-coating the film casting liquid onto the glass matrix, putting the glass matrix in a solvent evaporation chamber, heating to 100-120 DEG C under a high vacuum condition, holding the temperature for 0.5-12h, removing a solvent and obtaining the fluorescent thin-film sensor. The invention further discloses the application of the fluorescent probe molecule and the fluorescent thin-film sensor in detecting the pH value of a solution. A ratio-type fluorescent probe has two fluorescent emission peaks, and can be calibrated by two signal peaks of the fluorescent probe, and the detection accuracy is improved.

The invention discloses an organic silicon graphene industrial coating and a preparation method thereof. The organic silicon graphene industrial coating comprises 40-60% of modified organic silicon resin; the modified organic silicon resin is formed by polymerizing an organic silicon polymer, diisocyanate, graphene oxide, 4-methoxystyrene, butadiene and a free radical initiator according to the weight ratio of 1: (0.01 to 0.03): (0.2 to 0.3): (0.1 to 0.3): (0.1 to 0.3): (0.001 to 0.003). The graphene oxide is introduced into organic silicon polymer molecules, so that the scratch resistance and the mechanical strength of the organic silicon resin are enhanced, and the bending property and the impact resistance of the organic silicon resin are improved; a flexible chain segment cis-1, 4-polybutadiene is introduced, so that the internal stress of the organic silicon resin is reduced, and cracks are reduced; a rigid chain segment poly (4-methoxystyrene) is introduced, so that the bending property and the impact resistance of the organic silicon resin are improved.

This present invention relates to (Z)-3,4,5-Trimethoxystyrylbenzenesulfonamides of general formula A. The invention also provides the synthesis of (Z)-3,4,5-trimethoxystyrylbenzenesulfonamides useful as potential antitumor agents against human cancer cell lines and a process for the preparation thereof.

The invention relates to a preparation method of Ramage linker and mainly solves problems of long processes, complex post-treatment, much waste water, waste gas and solid waste, and high cost in a conventional synthetic method. The preparation method includes following steps: (A) carrying out a reaction to 2-carboxybenzaldehyde and m-methoxyphenylacetic acid to obtain an intermediate 2-(3-methoxylstyryl)benzoic acid, dissolving the intermediate with a solvent, performing hydrogenation reduction, and performing post-treatment crystallization to obtain a compound R-1; (B) carrying out a reaction to the R-1 with SOCl2 or POCl3 to obtain 2-methoxyl-10,11-dihydro-5H-dibenzo[a,d]cycloheptene-5-one, performing negative-pressure evaporation to remove the SOCl2 or the POCl3, dissolving the 2-methoxyl-10,11-dihydro-5H-dibenzo[a,d]cycloheptene-5-one in benzene, methylbenzene or 1,2-dichloroethane, performing a catalytic reaction with anhydrous AlCl3 and performing post-treatment crystallization to obtain a compound R-2; (C) carrying out a reaction to the R-2 with benzyl bromoacetate in DMF or an acetone / K2CO3 solution to obtain a compound R-3; (D) performing hydrogenation reduction to the R-3 to obtain a compound R-4; and (E) adding a catalyic amount of PTS to the R-4 in DMF and carrying out a reaction to the R-4 with Fmoc-NH2 to obtain the Ramage linker, which is an effective C-terminal linker in solid-phase synthesis.

Pharmaceutical compositions of (E)-2,4,6-trimethoxystyryl-3-[(carboxymethyl)amino]-4-methoxybenzylsulphone and pharmaceutically acceptable salts thereof are described as well as methods of their use, and a dose regimen of (E)-2,4,6-trimethoxystyryl-3-[(carboxymethyl)amino]-4-methoxybenzylsulphone, sodium salt to reduce the incidence of urothelial toxicity.

The invention relates to benzocyclophosphamide phenate derivatives or pharmaceutically acceptable salts (I) thereof. The benzocyclophosphamide phenate derivatives or pharmaceutically acceptable salts thereof comprise stereoisomerides or tautomers. In the formula (I), R is 4-hydroxyphenyl, 4-methoxyphenyl, 4-acetoxy-phenyl, 3, 4-dihydroxyphenyl, 3, 4, 5-trihydroxyphenyl, 3, 4-dimethoxyphenyl, 3, 4, 5-trimethoxyphenyl, 3, 4-dihydroxy styryl, 3-methoxy-4-hydroxy styryl, 3, 4-dimethoxy styryl, 3, 4-diacetoxy styryl and 3-methoxy-4-acetoxy styryl. The benzocyclophosphamide phenate derivatives disclosed by the invention have significant anti-cancer effect, can effectively prolong the survival time of mice loaded with HL60, have better effects than the cyclophosphamide and have the obvious inhibitory action against the angiogenesis of a chorioallantoic membrane (CAM). Thus, the benzocyclophosphamide phenate derivatives disclosed by the invention can be applied to preparation of anti-tumor medicaments. The invention discloses the preparation method of the benzocyclophosphamide phenate derivatives.