170 results about "Tosylphenylalanyl Chloromethyl Ketone" patented technology

The invention relates to a method for preparing (S)-(4-chlorphenyl)-(pyridine-2-yl)-methanol by utilizing microbial catalysis, and belongs to the technical field of biological catalysis. According to the method, 4-chlorphenyl-(pyridine-2-yl)-ketone is subjected to asymmetrical reduction by utilizing kluyveromycessp (CCTCCM 2011385) whole cells to synthesize the (S)-(4-chlorphenyl)-(pyridine-2-yl)-methanol. The method comprises the following steps of: sieving a microbe which has high-stereoselectivity carbonyl reductase activity on a prochiral ketone substrate, determining a series of conditions of asymmetrical reduction reaction, such as reaction temperature, pH, the concentration of cells, the concentration of the substrate and reaction time and additives (including various secondary solvents, polyethyleneglycol (PEG), phosphates and the like), wherein the enantiomer excess value and yield of the (S)-(4-chlorphenyl)-(pyridine-2-yl)-methanol serving as a product can reach 86.7 percent e.e and 92.1. The product is separated and extracted initially by silicagel column chromatography, so that the purity of the separated product is 99.2 percent, and the extraction yield is 56.7 percent.

A ultraviolet curing coating and its production are disclosed. The coating consists of filming substance, diluent and light initiating agent or assistants. The diluent is a organic solvent which comprises one of several from toluene, acetic ether, acetate butyrin, isobutyl acetate, propyl acetate, alcohol, n-butyl alcohol, ethylene ketone, dimethyl benzene, methyl isobutyl ketone, acetone, methyl ethyl ketone, ethanediol butyl ester and propylene butyl ester. It costs low, has better abrasive-resistance, hardness and adhesion.

The invention relates to a novel process for preparation of N-[2-n-butyl-3-[4-[3-(di-n-butylamino)-propoxy]-benzoyl]-benzofuran-5-yl]methanesulfonamide (I) and pharmaceutical acceptable salts thereof, where a salt of (5-amino-2-butyl-1-benzofuran-3-yl) {4-[3-(di-n-butylamino)propoxy]phenyl}methanone of formula (II)—where A is a mono- or dibasic acid forming an acid addition salt with the compound of formula (II), n is 1 if A is dibasic acid and n is 1 or 2 if A is a monobasic acid—is reacted with a mesylating reagent in a heterogen reaction, if desired, in the presence of a phase transfer catalyst. The invention also relates to the novel salts of compound of formula (II), for the preparation thereof and their use in the preparation of dronedarone.

The invention discloses a fingerprint resisting ultraviolet curing paint which mainly comprises the following components according to the mass percent: 25-28 of stain resisting low polymer, 4-6 of multifunctional-group aliphatic urethane acrylate, 5-6 of urethane acrylate, 22-25 of polymer modified acrylate, 25-30 of tri(propylene glycol) diacrylate, 15-18 trimethylolpropane methylacrylate, 4-5 of 1-hydroxycyclohexy phenyl ketone, 0.4-0.5 of stain resisting photo-curing assistant, 0.1-0.3 of flatting agent and 120-130 of diluting agent. The invention develops the fingerprint ultraviolet curing paint which has fingerprint resisting effect, easy cleaning of permanent pen marks and better oil stain resistance and is used for a PC board by adopting stain resisting low polymer as main resin and adding the stain resisting photo-curing assistant in the formulation, and solves the problems that common ultraviolet curing paint is easily stained by fingerprints, the permanent pen marks are not easy to remove and the stain resistance is poor.

The invention relates to optical activity di(heteto)aryl methanol and an asymmetric synthesis method thereof. The method comprises the following steps: taking mono-sulfonyl chiral diamine and a complex of metals ruthenium, rhodium and iridium as catalysts, taking sodium formate or formic acid/triethylamine or isopropanol as a hydrogen source, carrying out an asymmetric transfer hydrogenation reaction of di(heteto)aryl ketone first, thereby obtaining the optical activity di(heteto)aryl methanol. The method is mild in reaction conditions, easy and convenient to operate, readily available in raw materials, wide in substrate application range and high in enantioselectivity and has important application prospects in the aspects of synthesis of antihistamine chiral drugs such as diphenhydramine, methyldiphenhydramine, carbinoxamine and bepotastine.

The invention relates to an asymmetric synthesis method of an ophthalmologic drug pylistramine besylate. The method concretely comprises the following steps: oxidizing (4-chlorophenyl)(2-pyridyl)methanone to obtain (4-chlorophenyl)(2-pyridyl)ketone-N-oxide; carrying out asymmetric transfer hydrogenation reduction on the (4-chlorophenyl)(2-pyridyl)ketone-N-oxide through using a complex of monosulfonyl chiral diamine and metallic ruthenium, rhodium and iridium as a catalyst and a sodium formate or formic acid and triethylamine mixture or isopropanol as a hydrogen source in order to prepare (S)-(4-chlorophenyl)(2-pyridyl)methanol-N-oxide; reducing the (S)-(4-chlorophenyl)(2-pyridyl)methanol-N-oxide to prepare (S)-(4-chlorophenyl)(2-pyridyl)methanol; and condensing the (S)-(4-chlorophenyl)(2-pyridyl)methanol and ethyl 4-(4-bromopiperidine-1-yl)butyrate to obtain the ophthalmologic drug pylistramine besylate. The total yield is 61.6%.

The invention discloses fingerprint resisting UV light oil which mainly comprises the following components according to the weight portion: 30-35 of stain resisting low polymer, 5-6 of urethane acrylate, 15-18 of polymer modified acrylate, 15-18 of tri(propylene glycol) diacrylate, 25-30 trimethylolpropane methylacrylate, 4-5 of 1-hydroxycyclohexy phenyl ketone, 0.4-0.5 of stain resisting photo-curing assistant, 0.1-0.3 of flatting agent and 120-140 of diluting agent. The invention develops the fingerprint UV light oil which has fingerprint resisting effect, easy cleaning of permanent pen marks and better oil stain resistance and is used for an ABS+PC plastic piece by adopting stain resisting low polymer as main resin and adding the stain resisting photo-curing assistant in the formulation, and solves the problems that common UV light oil is easily stained by fingerprints, the permanent pen marks are not easy to remove and the stain resistance is poor.

The invention discloses a method for synthesizing a chiral bisaryl alcohol compound. The method provided by the present invention specifically uses a mutant of a carbonyl reductase SSCR derived from Sporobolomyces Salmonicolor and a mutant of alcohol dehydrogenase TbSADH derived from Thermoanaerobacter brockii to catalyze asymmetric reduction of (4-chlorophenyl)pyridine-2-ketone to form (S)-(4-chlorophenyl) pyridine-2-methanol. The experiment proves that the method provided by the invention has high yield and high ee value, can reduce the addition amount of coenzyme, and does not need to add enzyme such as glucose alcohol dehydrogenase for cofactor circulation, the reaction condition is mild, and the operation is simple.

The invention relates to a recoatable UV radiation cured coating for plastic as well as a production method and an application method of the coating. The recoatable UV radiation cured coating for the plastic comprises the following components in percentage by weight: 20-30% of tetrafunctional aliphatic polyurethane acrylate resin, 20-30% of bifunctional polyurethane acrylate resin, 8-15% of trimethylolpropane trimethacrylate, 15-25% of 1,6-hexanediol diacrylate, 2-5% of 1-hydroxy-cyclohexyl-phenyl ketone, 0.5-2% of diphenyl(2,4,6-trimethylbenzoyl)phosphine oxide, 7-17% of a solvent, and 0.5-1% of reactive polysiloxane acrylate, wherein the solvent is a mixed solvent composed of at least two of ethyl acetate, butanone, butyl acetate, n-butyl alcohol and isopropanol. The UV radiation cured coating for the recoatable plastic disclosed by the invention can be directly repaired without integrally grinding and prespraying a layer of bottom water while being used normally.

The invention provides a UV curing high wear-resistant low luster coating and a preparation method thereof. The coating comprises the following components in percentage by weight: primer and a curingagent, wherein, the primer comprises 55-60 of hydroxyl acrylic resins, 10-13 of solution containing 20% of cellulose acetate butyrate resins, 4-6 of methyl isobutyl ketone, 0.1-0.2 of flow agent, 5-7of aluminum paste and 17-19 of ethyl acetate; the curing agent comprises 55-60 of hexamethylene diisocyanate, 10-15 of unsaturated aliphatic polyurethane acrylate and 26-32 of butyl acetate. The invention has the advantages as follows: the invention has low VOC discharge when being used for construction under common coating conditions; the invention can achieve the effects of high wear resistanceand difficult surface shining by using the common plastics coating method; the invention features simplicity and commonality of construction and has very good adhesion on the plastics and aluminum; the invention features thin film thickness and has cost lower than that of the common UV coatings.

The invention discloses a F-18 tagged P2X7 receptor imaging agent which is a compound 18F-{(2-chloro-3-trifluorophenyl)(1-(pyrimidin-2-yl)-6,7-dihydro-1H-[1,2,3]triazolo[4,5-c]pyridin-5(4H)-yl)methanone shown as formula I. The P2X7 receptor imaging agent is suitable for identifying and diagnosing pulmonary inflammation and tumors.

The invention relates to a chiral catalytic synthesis method of thiamphenicol which is a chloramphenicol broad-spectrum antibiotic. Thioanisole serves as an initating raw material, acylation and bromo are achieved, nitrogen iridine containing substituent groups is synthetized, and a qualified product which meets the requirement of drug administration is synthetized through chiral catalytic reduction, oxidizing reaction, acidification loop opening, deprotection and acylation reaction. The chiral catalytic reduction includes that under the action of a catalyst trans-RuC12[(R)-xylbinap][(S)-DPEN], [1-substituent group nitrogen iridine-2-group] [4-(methylthio group) phenyl group] ketone is subjected to hydrogenation reduction to obtain [1-substituent group nitrogen iridine-2-group] [4-(methylthio group) phenyl group] ketone with a high ee value and a high de value. D-methylsulfonylphenyl serine ethyl ester used in industrial production serves as a raw material to synthetize the thiamphenicol, the D-methylsulfonylphenyl serine ethyl ester is obtained through chemical chiral resolution by using a racemic compound, and the other half of the raw material is wasted. According to the unsymmetrical chiral catalytic dynamic reduction method, waste of the other half of the raw material is avoided, the utilization rate of a material is improved, and the production cost is reduced.

The invention discloses a method for catalyzing cellulose hydrolysis by a sulfonic acid functionalized ionic liquid composite system. The method comprises: taking methyl isobutyl ketone-water as the solvent, adding a transition metal salt water solution and a sulfonic acid functionalized ionic liquid into cellulose to carry out reaction under a temperature of 120DEGC-180DEG C and a pressure of 2atm-3atm for 3-8h; wherein, the transition metal salt is a manganese salt, an iron salt, a ferrous salt, a cobalt salt or a zinc salt; the sulfonic acid functionalized ionic liquid is 1-(4-sulfobutyl)-3-methylimidazolium hydrogen sulfate, and the structural formula is shown as the specification. The sulfonic acid functionalized ionic liquid provided by the invention shows good catalytic activity in catalyzing cellulose hydrolysis, and when a catalytic amount of the transition metal salt (Mn<2+>, Fe<3+>, Fe<2+>, CO<2+>, Zn<2+>) is added into the system, the product selectivity and the cellulose hydrolysis efficiency are improved.

The invention provides a stone surface crystallization UV photocurable coating, a method for preparing the same and a construction process. The stone surface crystallization UV photocurable coating comprises the following components: aliphatic polyurethane acrylate, trifunctional aliphatic polyurethane acrylate, thermoplastic acrylic resin, trimethylolpropane triacrylate, dipentaerythritol pentaacrylate, 1-hydroxy-cyclohexyl phenyl ketone, a photoinitiator, ethyl acetate, a leveling agent, a defoaming agent, butyl acetate and toluene. When the coating is used for the surface crystallization protection treatment of stones, because the photocurable technique is adopted, the film forming efficiency is 20 to 23 seconds, so that the film can be quickly formed in high efficiency, and the surface of the stones, on which the film is formed, is high in hardness, glossiness and saturation; and the coating can also improve chemicals resistant, acid resistant, alkali resistant, pollution resistant, heat resistant, ironing resistant, smoke and fire resistant, aging resistant properties and the like of the surface of the stones.

The invention belongs to the technical field of medicines and relates to (1-aryl-1H-pyrazol-4-yl)(3,4,5-trimethoxyphenyl)ketone and ketoxime compounds and an application thereof and exactly relates to the compounds and an application thereof to antitumor medicines as tumor cell proliferation inhibitors. A structure of the compounds is shown in a general formula I in the specification: the definition of each substituent is shown in the claim and specification.

The invention belongs to the technical field of organic synthesis and specifically relates to a method for increasing the ketone-alcohol ratio in hydrogenation reaction of an anti-aging agent 4020 by modification-catalysis. The method is characterized by preparing raw materials, namely 4-aminodiphenylamine, methyl isobutyl ketone (MIBK) and an ionic liquid into a raw material solution, loading a copper-based catalyst into a fixed bed reactor, and putting the raw material solution into the fixed bed reactor in a continuous feeding and discharging way for preparing the anti-aging agent 4020 by catalytic hydrogenation, wherein the ketone-alcohol ratio after the hydrogenation reaction is significantly increased. The method provided by the invention is simple, convenient to operate, high in yield and good in selectivity, the MIBK becomes methyl isobutyl carbinol (MIBC) by hydrogenation, and side effects are obviously inhibited, so that the method is conductive to increasing the ketone-alcohol ratio after catalytic hydrogenation in industrial production, reducing the consumption of the MIBK and greatly reducing the production cost.

A novel hydroxyalkyl phenyl ketone: (1-hydroxycylohexyl)[4-(2- hydroxy ethoxy)phenyl] methanone, its preparing process and its application as the trigger for optical solidification are disclosed. Said trigger can effectively and optical trigger the polymerization between unsaturated compound and resin. Its special molecular structure can prevent migration, odoring and yellowing.

The invention belongs to the field of coating and relates to staining-resisting UV (Ultraviolet) coating as well as a preparation method and an application technology thereof. The staining-resisting UV coating is prepared from the following components in percentage by weight: 50 to 60 weight percent of fluorosilicon modified acrylate, 10 to 15 weight percent of dipentaerythritol hexaacrylate, 10 to 15 weight percent of propoxylated pentaerythitol tetraacrylate, 3 to 5 weight percent of 1-hydroxyl-cyclohexyl-phenyl ketone, 2 to 5 weight percent of (2,4,6-trimethylbenzoyl)diphenyl phosphine oxide, 0.2 to 1 weight percent of a de-foaming agent, 0.2 to 1 weight percent of a flatting agent and 5 to 15 weight percent of a diluting agent, wherein the diluting agent is a mixture of absolute ethylalcohol and dicarboxylate. Compared with the prior art, the staining-resisting UV coating provided by the invention has high reaction activity and a rapid curing speed and the coating has a low shrinkage rate; and a formed coating film has a strong attachment force and excellent flexibility and is continuous and stable.

The invention aims to solve the technical problems of an existing alpha-hydroxycyclohexyl phenyl ketone synthesis method, provides a synthesis method of a photoinitiator 1-hydroxycyclohexyl phenyl ketone, and belongs to the technical field of chemical synthesis. The synthesis method comprises the following steps: (1) reacting a halogenated benzene with magnesium particles to prepare a Grignard reagent, dropwise adding cyclohexylcarbonitrile into the prepared Grignard reagent, and after the reaction is completed, hydrolyzing to generate cyclohexyl phenyl ketone; and (2) reacting cyclohexyl phenyl ketone with chlorine to obtain 1-chlorocyclohexyl phenyl ketone, and carrying out a hydrolysis reaction on the 1-chlorocyclohexyl phenyl ketone and a sodium hydroxide aqueous solution under the action of a catalyst to obtain 1-hydroxycyclohexyl phenyl ketone. The method is simple in synthesis process, high in yield and suitable for industrial production.

The invention provides a dicarbazole compound containing a tetraphenylethylene structure as well as a preparation and application thereof. The name of the compound is as follows: 9,9'-(5-(2,2-diphenyl-1-(4-benzyl))vinyl-1,3-phenylene)dicarbazole. A preparation method comprises the following steps: firstly, preparing 3,5-di(9-carbazolyl)phenyl-(4-methylphenyl)ketone; then enabling the 3,5-di(9-carbazolyl)phenyl-(4-methylphenyl)ketone to react with diphenylmethane to obtain the 9,9'-(5-(2,2-diphenyl-1-(4-benzyl))vinyl-1,3-phenylene)dicarbazole. The compound provided by the invention has good thermal stability, electrochemical stability, charge transferring property and luminescent property and can be used as a blue-green organic electroluminescent material.

The invention discloses an alcohol dehydrogenase mutant and application thereof in synthesis of chiral diaryl alcohol compounds. The alcohol dehydrogenase mutant disclosed by the invention is a protein, which is obtained through mutating amino acid residues located in a catalytic center pocket of alcohol dehydrogenase TbSADH, and particularly is the protein, which is obtained through mutating 39thand/or 42th and/or 84th and/or 85th and/or 86th and/or 104th and/or 110th and/or 294th amino acid residues of an amino acid sequence of the alcohol dehydrogenase TbSADH. According to the alcohol dehydrogenase mutant and the application thereof, the alcohol dehydrogenase TbSADH is subjected to enzyme reforming by applying an orthogenesis technology and method, a series of mutants, which have enzyme activity to diaryl ketones with represented by (4-chlorophenyl)pyrid-2-ketone, are obtained, and the mutants are applied to biocatalytic synthesis of optically-pure chiral diaryl alcohol compounds.

The invention belongs to the technical field of organic matter detection and analysis, and discloses a detection method of (6-aminopyridine-2-yl)(1-methylpiperidine-4-yl) ketone dihydrochloride. The detection method comprises the following steps: detecting (6-aminopyridine-2-yl) (1-methylpiperidine-4-yl) ketone dihydrochloride by adopting a liquid chromatography method, wherein the conditions of the liquid chromatography are as follows: the adopted mobile phase comprises a mobile phase A and a mobile phase B, wherein the mobile phase A is a phosphate buffer solution, the mobile phase B is acetonitrile, and the mobile phase is subjected to gradient elution according to certain conditions. The detection method can be used for accurately detecting the purity of the (6-aminopyridine-2-yl)(1-methylpiperidine-4-yl) ketone dihydrochloride in the test sample.

The invention discloses a method for preparing a dapagliflozin intermediate by a one-pot method, and the method comprises the following steps: reacting 5-bromo-2-chlorobenzoic acid with phenetole in the presence of an oxidant and a catalyst for a period of time, and performing purifying to obtain the dapagliflozin intermediate (5-bromo-2-chlorphenyl) (4-ethoxyphenyl) ketone. The method provided by the invention is high in yield, simplifies the process steps of the traditional synthesis method, makes the process simpler, reduces the reaction cost and impurity content, improves the purity and yield, and better conforms to the industrialization standard of benefit maximization.