788 results about "Phenylacetic acid" patented technology

The invention discloses a method for preparing trifluoro-phenylacetic acid. The method comprises the following steps: (1) in the presence of an evocating agent, trifluoro-benzyl halides and magnesium in an organic solvent react to obtain a Grignard reagent; (2) carbon dioxide gas is introduced into the Grignard reagent for reaction; and (3) a product obtained in the step (2) is hydrolyzed to obtain the trifluoro-phenylacetic acid. The invention also discloses a method for preparing sitagliptin. The method has the characteristics of high yield, good purity, low cost, simple process, mild condition, few three wastes and good safety, and is suitable for industrialized production.

The present invention provides a process for the preparation 6-[3-(hetero)aryloxy-2-fluoro-benzyl]-2H-pyridazin-3-one compounds 1 where R2 is an optionally substituted aryl or an optionally substituted heteroaryl, R⁶ is NO₂, NH₂, alkyl, halogen, or a function group readily derived therefrom and R^4c is hydrogen or alkyl. There also is provided a process for the

preparation of phenylacetic acid compounds 2, wherein R² and R⁶ are as defined previously and R^5a is hydrogen or alkyl, which are useful for the preparation of pyridazinone compounds.

The present invention provides a method for producing an enantiomerically enriched α-(phenoxy)phenylacetic acid compound of the formula:

from its enantiomeric mixture, where R¹ is alkyl or haloalkyl and X is halide.

An aqueous liquid preparation of the present invention containing 2-amino-3-(4-bromobenzoyl)phenylacetic acid or its pharmacologically acceptable salt or a hydrate thereof, an alkyl aryl polyether alcohol type polymer such as tyloxapol, or a polyethylene glycol fatty acid ester such as polyethylene glycol monostearate is stable. Since even in the case where a preservative is incorporated into said aqueous liquid preparation, the preservative exhibits a sufficient preservative effect for a long time, said aqueous liquid preparation in the form of an eye drop is useful for the treatment of blepharitis, conjunctivitis, scleritis, and postoperative inflammation. Also, the aqueous liquid preparation of the present invention in the form of a nasal drop is useful for the treatment of allergic rhinitis and inflammatory rhinitis (e.g. chronic rhinitis, hypertrophic rhinitis, nasal polyp, etc.).

The invention belongs to the technical field of medicament synthesis, and in particular relates to a chemical synthetic method of hydroxytyrosol. The chemical synthetic method comprises the steps of (1) protecting two phenolic hydroxyl groups of catechol by using dichloromethane, and enabling catechol to react with dichloromethane to prepare 1,2-methylenedioxybenzene; (2) enabling 1,2-methylenedioxybenzene to react with various monoesters of oxalyl chloride to prepare 3,4-methylenedioxy phenylglyoxylic acid ester; (3) preparing 3,4-methylenedioxy phenylacetic acid by using 3,4-methylenedioxy phenylglyoxylic acid ester through a Wollff-kishner-Huang Minglong reduction reaction; and (4) reducing the 3,4-methylenedioxy phenylacetic acid by using lithium aluminum hydride, lithium borohydride or sodium borohydride to prepare 3,4-methylenedioxy phenethyl alcohol, and then removing methylene protection of the 3,4-methylenedioxy phenethyl alcohol by using boron tribromide or palladium on activated carbon to prepare hydroxytyrosol. A reactive reagent used in the synthetic method disclosed by the invention is easy to obtain and low in price, the reaction condition is mild, and the final yield of the whole reaction is 23%.

The invention relates to a preparation method of an azoxystrobin intermediate. The method comprises the following steps of: (1) synthesizing benzofuranone from o-hydroxyphenylacetic acid serving as a raw material; and (2) making benzofuranone react with trimethyl orthoformate to generate the azoxystrobin intermediate, wherein no solvent is used in the reaction in the step (1); and the reaction isperformed by the following steps of: putting o-hydroxyphenylacetic acid and 0-3 percent of catalyst into a reaction kettle; preserving heat in vacuum at the temperature 125-180 DEG C to react for 2-3hours; and evaporating water generated by the reaction in vacuum, wherein the residue in the reaction kettle is benzofuranone. The method has the advantages of simple process, high yield of the azoxystrobin intermediate and low production cost.

The invention discloses a formula of tobacco flavoring essence with sweet essence. According to the formula, the tobacco flavoring essence consists of the following components in percentage by mass: 1.0 to 4.0 percent of ethyl maltol, 2.0 to 3.0 percent of plum extractum, 1.0 to 2.0 percent of phenethyl ethanol, 0.01 to 0.1 percent of damascenone, 0.1 to 0.5 percent of phenylacetic acid ethylester, 0.5 to 1.0 percent of methyl cyclopentenotone, 2.0 to 5.0 percent of red date extractum, 0.01 to 0.03 percent of linalool, 0.02 to 0.08 percent of 5-methylfurfural, 0.1 to 0.5 percent of benzoic acid, 0.05 to 0.15 percent of beta-irisone, 0.02 to 0.08 percent of 4-guaethol, 15 to 25 percent of glycerol, 45 to 55 percent of propylene glycol and 3 to 15 percent of purified water. By the formula, tobacco produces sweet fragrance, tobacco fragrance can be increased and taste of the tobacco can be adjusted, so that the taste of the tobacco is improved, the natural sweet fragrance of the tobacco is enhanced and dry, astringent and bitter mouthfeel of customers is improved and requirements of the customers are met.

The invention relates to epoxy resin polymer mortar and a production process thereof. The mortar is prepared from the following components in parts by weight: 15-20 parts of epoxy resin slurry, 2-4 parts of an active diluent, 6-8 parts of a curing mixture and 70-80 parts of a base material which are mixed, stirred and mixed, wherein the epoxy resin slurry is prepared from bisphenol A epoxy resin E51, modified epoxy resin, organic bentonite and dioctyl phthalate; the active diluent is prepared from epoxy chloropropane, fatty alcohol and trichloropropane; the curing mixture is prepared from 85 parts of modified phenolic aldehyde amine, hydroxy-terminated liquid nitrile rubber, 2-(3, 4-expoy cyclohexyl) ethyl triethoxyl silane, lauryl phenylacetate and resorcinol; the base material is prepared from ordinary portland cement, quartz sands, hydrophobic expanded perlite, refined graphite powder and sericite powder. The epoxy resin polymer mortar provided by the invention not only has excellent mechanical property and wear resistance, but also has a good adhesive performance, and can be integrally formed with substrate concrete.

The invention discloses a preparation method of sitagliptin, comprising the following steps: reacting 2, 4, 5-trifluoro-phenylacetic acid with malonic cyclo (sub) isopropyl ester; reacting 3-oxo-4-(2, 4, 5-trifluorophenyl) methyl butyrate with ammonium acetate; reacting 3-amino-4-(2, 4, 5-trifluorophenyl) methyl crotonate with hydrogen; performing hydrolysis reaction to (R)-3-amino-4-(2, 4, 5-trifluorophenyl) methyl butyrate; and reacting (R)-3-amino-4-(2, 4, 5-trifluorophenyl) butyric acid with 3-(trifluoromethyl)-5, 6, 7, 8-tetrahydro-[1, 2, 4] triazol [4, 3-a] pyrazine hydrochloride to obtain sitagliptin. According to the invention, EE value greater than 90% is obtained through high-efficiency catalytic hydrogenation; sitagliptin is prepared by only five steps; yield is higher; technical conditions are mild; operations are simple; cost is low; and yield and purity of products are high.

The invention discloses rhodococcus ruber FQ-2 and an application thereof in degradation of acetone and other common industrial organic pollutants. The application method comprises the steps: an inorganic salt culture medium containing acetone and other common industrial pollutants is inoculated with the rhodococcus ruber FQ-2, a degradation reaction is carried out under the conditions of the temperature of 30 DEG C and the rotating speed of 160 r/min, and thus the organic pollutants are degraded; the common organic pollutants comprise acetone, n-hexane, carbon disulfide, chlorobenzene, butylacetate, ethyl acetate or alpha-pinene. The rhodococcus ruber FQ-2 is taken from activated sludge of an aeration tank of a pharmaceutical factory in Zhejiang province, has good degradation effect on VOCs organic pollutants, especially acetone, and can completely convert acetone into harmless substances such as CO2, H2O, cell biomass and the like; at the same time, the bacterial strain also can degrade common industrial pollutants such as carbon disulfide and chlorobenzene in different extent, so the bacterial strain has broad application prospects in biological purification of industrial wastegas and wastewater.

The invention relates to a method for preparing a 3-arylbenzofuran ketone compounds. The method comprises that: phenolic compounds and phenylacetic-acid structure compounds are subjected to alkylationin a mol ratio of 1:1-2 at a temperature between 60 and 270 DEG C; an alkylation catalyst is an acidized crosslinked montmorillonite catalyst prepared by acidizing, loading, crosslinking and activating montmorillonite; the weight ratio of phenolic compounds serving as reaction raw material to the montmorillonite alkylation catalyst is 1:0.01-0.2; an esterification catalyst is added; the mol ratioof the phenolic compounds serving as the reaction raw material to the esterification catalyst is 1:0.001-0.02; esterification is performed at a temperature between 60 and 170 DEG C; supported metal ions of the acidized crosslinked montmorillonite catalyst are 1 to 10 mmol/g of montmorillonite; and the mol ratio of silicon to aluminum is 2-10:1. The 3-arylbenzofuran ketone compound prepared is suitable for serving as organic polymer sensitive to oxidation and heat/light-induced degradation, particularly a polyolefin stabilizer.

The invention discloses a preparation method 2,4,5-trifluorophenylacetic acid. The method is characterized by consisting of four reaction steps of: A, reaction of 2,4,5-trifluoronitrobenzene (I) and diethyl malonate which are condensed to prepare 2,5-difloro-4-nitrobenzophenone diethyl malonate; B, hydrolysis, acidification and decarboxylic reaction of dibasic ester; C, reduction reaction of nitryl; and D, diazotization fluoridation of amino. The four reaction steps can be sequentially carried out according to A, B, C and D, or A, C, B and D, or A, C, D and B. According to the preparation method provided by the invention, condensation of 2,4,5-trifluoronitrobenzene (I) and diethyl malonate is easy to realize by means of high substituting activity of nitryl p-fluorine, and the raw material 2,4,5-trifluoronitrobenzene (I) is low in cost and easy to obtain and can be easily prepared by nitration and fluorination of 2,4-dichlor fluorbenzene. Compared with the prior art, the preparation method provided by the invention has the characteristics of low-cost and easily obtained raw materials, mild reaction condition, high total yield, low production cost and the like, and is comparatively suitable for industrialized production.

The invention provides a synthesis method of sulbenicillin sodium and sulbenicillin sodium used for injection, which comprises the concrete steps of: using 6-APA and BSA to synthesize an organic salt, and dissolving the organic salt into dichloromethane; using a sulphur phenylacetic acid triethylamine salt and pivaloyl chloride to make mixed anhydride; carrying out anhydrous condensation on the sulphur phenylacetic acid triethylamine salt and the pivaloyl chloride in the dichloromethane; and then forming a sodium salt, free-drying and obtaining a finished product. The new technical process is stable and feasible, better and stable in product quality and strong in operability of production, and reduces the environmental pollution.

Disclosed herein are tablets and methods of treatment comprising the administration of such tablets. The tablets are immediate release tablets that comprise about 400 mg of 5-methyl-2-(2′-chloro-6′-fluoroanilino)phenylacetic acid or a pharmaceutically acceptable salt thereof, where the 5-methyl-2-(2′-chloro-6′-fluoroanilino)phenylacetic acid or a pharmaceutically acceptable salt thereof comprises between 60 and 70% by weight of the tablet. The methods involve the administration of the tablets of the invention to individuals in need of administration of such tablets.

The invention discloses a strapping band for fruit tree grafting, and the strapping band is used for strapping grafting scions onto rootstocks. The strapping band comprises a strip-shaped band body made of gauze. The band body is subjected to infiltration processing. The components of infiltrating liquid include, by weight, 1000-2000 parts of distilled water, 0.8-2 parts of vitamin C, 0-3 parts of tannic acid, 2-5 parts of phenylacetic acid, 0.03-0.05 part of potassium chloride, 0.2-0.5 part of ammonium nitrate and 0.01-0.02 part of chloramphenicol. The PH value of the infiltrating liquid is 5.2-7.2. By the strapping band for fruit tree grafting, coalescence of joints can be accelerated after grafting and survival rate of fruit grafting is increased.