103 results about "PHENYLBUTYRIC ACID" patented technology

Controlled-release formulations and dosage forms containing 4-phenylbutyric acid sodium salt, or other pharmaceutically acceptable salts, esters or prodrugs, and a controlled release material for use in the treatment of diseases and disorders including neoplastic disorders and neurodegenerative diseases The formulations provide extended release and extended half-life.

Crystals of (E)-4-[4-(5-methyl-2-phenyl-4-oxazolylmethoxy)benzyloxyimino]-4-phenylbutyric acid (provided that crystals having a melting point of 126° C. to 127° C. are excluded), which have an excellent anti-diabetic action.

The invention discloses a method for kinetically separating 2-phenylbutyric acid enantiomer by using lipase. The (S)-phenylbutyric acid is prepared by high-efficiency selective lipase catalytic hydrolysis of racemic 2-phenylbutyrate. Cyclodextrin is added to a reaction system, so the substrate conversion rate is greatly improved, and the ee value is equal to or more than 96%. Compared with other separation techniques, the method has the advantages of mild reaction conditions, simplicity in operation, small environmental pollution, and obtaining of (S)-2-phenylbutyric acid with a high optical purity. The (S)-2-phenylbutyric acid is a key intermediate for synthesizing indobufen, and provides a feasible method for the preparation of the indobufen.

The invention discloses melamine hapten and antigen as well as a preparation method and application thereof. The method for preparing the compound shown in the formula I comprises the following steps:mixing 2-chloro-4,6-diamino-1,3,5-triazine and p-aminophenylbutyric acid to undergo reflux reaction for 24-30h at a temperature of 70-80 DEG C in the alkaline environment without water and obtainingthe compound shown in the formula I. The molar ratio of the 2-chloro-4,6-diamino-1,3,5-triazine to the p-aminophenylbutyric acid is 1: (1-3), preferably 1:1. The experimental results show that the titer of antiserum obtained by utilizing the antigen of the invention to immunize animals can reach 1:8*10<4>, the lowest limit of detection is 49ng / mL, the hemi-inhibitory concentration is 257ng / mL andthe generated antibody has high specificity, high sensitivity and high accuracy. Therefore, the antigen, antibody and detection method of the invention have extensive application prospects.

A process for preparing a stable aqueous dosage form of sodium 4-phenylbutyrate, including such dosage forms in a highly concentrated solution, as well as methods for making 4-phenylbutyrate and 4-phenylbutyric acid, and for using 4-phenylbutyrate. The stable aqueous dosage forms do not freeze at 0° C.

The invention relates to medicine preparation methods, particularly a preparation method of trimebutine, which comprises the following steps: esterifying and amino-methylating 2-amino-2-phenylbutyric acid which is used as the raw material, and reducing into 2-(dimethylamino)-2-phenylbutyl alcohol; and synthesizing trimebutine from the 2-(dimethylamino)-2-phenylbutyl alcohol and 3,4,5-trimethoxybenzoic acid in an organic solvent by using protonic acid as a catalyst. The invention is characterized in that the esterification and amino-methylation of the 2-amino-2-phenylbutyric acid are carried out at the same time to obtain the 2-(dimethylamino)-2-phenylmethyl butyrate, and sodium borohydride is used for reduction to obtain the 2-(dimethylamino)-2-phenylbutyl alcohol. In the invention, the 2-amino-2-phenylbutyric acid is subjected to esterification and amino-methylation at the same time, and reduced into alcohol, thereby simplifying the operation, greatly reducing the production risk, enhancing the reaction yield (up to higher than 80%) and greatly lowering the raw material cost. In the last preparation step, the protonic acid is added, thereby reducing the feed amount of the 3,4,5-trimethoxybenzoic acid and lowering the reaction cost.

The present invention provides a method for preparing an ubenimex intermediate (2S,3R)-3-acetamido-2-hydroxyl-4-phenylbutyric acid by using an organic alkali as a resolving agent, wherein the organic alkali is selected from S-1-naphthalene ethylamine, (S)-1-(2-naphthyl)ethylamine, L-phenylglycinol, and L-phenylalaninol. According to the present invention, the preparation method has advantages of good ubenimex intermediate purity, high yield, simple operation and good reproducibility, and is suitable for industrial production.

The invention provides a preparation method of ubenimex. The preparation method comprises that L-leucine benzyl ester p-toluenesulfonate and HOBt undergo a condensation reaction to produce an activated ester solution, (2S, 3R)-3-benzyloxyformamido-2-hydroxy-4- phenylbutyric acid and a weak acid strong alkali inorganic salt are mixed, the activated ester solution is added into the mixture drop by drop and undergoes a reaction to produce N-[(2S, 3R)-3-benzoylformamido-2-hydroxy-4-phenylbutyryl]-L-leucine, and N-[(2S, 3R)-3-benzoylformamido-2-hydroxy-4-phenylbutyryl]-L-leucine is reduced into ubenimex through hydrogen gas. The preparation method utilizes ethyl acetate as an organic solvent, saves tetrahydrofuran-caused potential safety hazard, utilizes the weak acid strong alkali inorganic salt as a base catalyst, saves a cost, is free of an organic solvent and is easy to operate.

The invention discloses a chlorambucil derivative with a structure as shown in a formula I, II or III and pharmaceutically acceptable salts thereof, wherein the formula is described in the specification. The invention also relates to a preparation method for the chlorambucil derivative, a preparation of the chlorambucil derivative and application of the chlorambucil derivative.

The invention discloses a method for preparing phenyl piracetam, and belongs to the field of compound preparing. The method includes the following steps that alkali, cinnamic acid alkyl ester and nitromethane are subjected to an addition reaction to obtain 4-nitryl-3-phenylbutyric acid alkyl ester; after nitryl of the 4-nitryl-3-phenylbutyric acid alkyl ester is reduced with a reducing agent, the reduced nitryl and carbonyl are cyclized, and 4-phenyl-2-pyrrolidone is obtained; alkali, haloacetic acid alkyl ester and the 4-phenyl-2-pyrrolidone are subjected to an alkylation reaction to obtain 4-phenyl-2-pyrrolidone-1-acetic acid alkyl ester; the 4-phenyl-2-pyrrolidone-1-acetic acid alkyl ester and ammonia gas are reacted to obtain the phenyl piracetam. The method has the advantages of being short in reaction step, high in atom utilization, more environmentally friendly, safe in operation, high in reaction yield and purity, beneficial for achieving industrialization an the like.

The invention belongs to the field of medicine preparation and provides a completely novel method for synthesizing Ubenimex. The method comprises the steps of firstly, protecting amino of a starting raw material, i.e., (2S,3R)-3-amino-2-hydroxyl-4-phenylbutyric acid (AHPA for short) by using di-tert-butyl dicarbonate so as to form a Boc protective product, then, carrying out condensation with L-leucine tert-butyl ester, and finally, removing the protective group in an organic solution of hydrogen chloride, thereby obtaining Ubenimex. According to the method, reagents used by the adopted synthesis route are all commonly-used reagents, produced industrially and low in cost; reaction solvents are all ordinary solvents, are low in toxicity and little in environmental pollution; and each reaction step is mild in conditions and simple and convenient in operation and does not need special equipment, so that the method is suitable for carrying out industrial production. The purity of the prepared product reaches 99.5% or more.

Conjugates of transferrin, albumin and polyethylence glycol consisting of native or thiolated transferrin or albumin or of polyethylene glycol (MW between approximately 5,000 and 20,0000) with at least one HS-, HO- or H2N group and cytostatic compounds derived through maleinimide or N-hydroxysuccinimide ester compounds, such as doxorubicin, daunorubicin, epirubicin, idarubicin, mitoxandrone, chloroambucil, melphalan, 5-fluorouracyl, 5'-desoxy-5-fluorouridine, thioguanine, methotrexate, paclitaxel, docetaxel, topotecan, 9-aminocamptothecin, etoposide, teniposide, mitopodoside, vinblastine, vincristine, vindesine, vinorelbine or a compound of general formula A, B, C or D, where n=0-6, X=-NH2, -OH, -COOH, -O-CO-R-COR*, -NH-CO-R-COR*, where R is an aliphatic carbon chain with 1-6 carbon atoms or a substituted or unsubstituted phenylene group and R*H, phenyl, alkyl with 1-6 carbon atoms.

A novel dentifrice composition is provided for prevention or treatment of carcinoma of the oral cavity, caries and periodontal diseases of the oral cavity. The dentifrice composition contains a silica abrasive and medicinal agents useful in the treatment of human neoplastic disease. The medicinal agent is selected from the group consisting of 3-N-phenylacetylamino-2,6-piperidinedione, phenylacetylglutamine, phenylacetylisoglutamine, phenylbutyrate, phenylacetate, combinations thereof and pharmaceutically acceptable salts thereof. The components of the dentifrice composition act advantageously to allow the composition to remove plaque, tartar, and oral disease-causing bacteria.

The invention provides a preparation method for 4-amino-3-phenylbutyric acid. The method comprises the following steps: step 1, benzaldehyde reacts with ethyl acetoacetate in a protonic solvent under the action of a condensation catalyst to generate 2,4-diacetyl-3- phenyl-pentanedionato diethyl ester (1); step 2, strongly alkaline solution is added in the 2,4-diacetyl-3-phenyl-pentanedionato diethyl ester (1) to obtain 3-phenylglutaric acid (2) after heating and decarbonylation; step 3, the 3-phenylglutaric acid (2) is subjected to ring-closing dehydration in a non-protonic solvent under the action of a dehydration catalyst to obtain 3-phenylglutaric anhydride step 4, the 3-(phenyl-glutaric anhydride) (3) is hydrolyzed with strong aqua ammonia to obtain 5-amino-5-oxo-3-phenyl-pentanoic acid (4); and step 5, the 5-amino-5-oxo-3-phenyl-pentanoic acid (4) and an oxidant are subjected to oxidation reaction under the alkaline condition to obtain 4-amino-3- phenyl butyric acid (5). The method has the advantages of easily-obtained inexpensive raw materials, normal reaction, simplicity and convenience in operation, moderate reaction conditions, security and high yield, and is suitable for industrial volume production.

The invention discloses an immune-electrochemistry sensor for detecting seven beta-adrenergic receptor agonists, and a manufacture method and application of the immune-electrochemistry sensor. The immune-electrochemistry sensor comprises a substrate glass electrode, and a film layer and a detection layer which sequentially coat the surface of the substrate glass electrode, wherein the material of the detection is a beta-agonist general hapten 4-(4-(2-terttert-butylamino) 1-ethoxy) phenylbutyric acid solution. The method comprises the following steps: firstly dispensing graphene / chitosan dispersion liquid on the surface of the clean substrate glass electrode, drying to form a film formation layer, dispensing the 4-(4-(2-terttert-butylamino) 1-ethoxy) phenylbutyric acid solution on the surface of the film layer, and then drying. The sensor is based on the cross immunoreactions of a beta-agonist broad specificity antibody on various beta-agonists, and can realize the detection of seven beta-agonists including clenbuterol, salbutamol, mabuterol, brombuterol, cimbuterol, tulobuterol and terbutaline.

Stable phenobarbital sodium solutions for injection that do not generate impurities during extended storage. These solutions include phenobarbital sodium in an amount of 15 to 200 mg / mL; a C1-C4 alcohol such as ethanol in an amount of 105 to 160 mg / mL; and a glycol such as propylene glycol in an amount of between 620 and 830 mg / mL and have a pH of between 9 and 12 which is adjusted to that range by adding acid or base, as required. No more than 50 mg / mL water is present including any water introduced by the acid or base. The solutions contain no more than 0.8% of phenyl ethyl acetyl urea impurity as well as no detectable amount of phenyl butyric acid after two years storage at room temperature.

The invention provides a method, which is characterized in that in a fixed bed device, solid acid is used as a catalyst, 4-phenylbutyric acid is used as a raw material and is dissolved into 1,2-dichlorobenzene according to a certain solid-to-liquid ratio, mixed liquid continuously flows through a catalyst layer after being gasified, the reaction is carried out on a catalyst, and the Alpha-tetralone can be continuously produced. The method solves the problem that in the existing intermittent liquid phase reaction system, the catalyst is easily inactivated and cannot be cyclically used. The gas-solid phase reaction has the advantages that the contact time between reactants and catalysts can be regulated so that the reaction condition is optimized, products generated in the reaction process are continuously separated in the reaction process, and the positive direction proceeding of the reaction is favorably realized. In addition, because the fixed bed catalytic mode is adopted, generated products leave the catalytic bed layer in time in the reaction process, the reaction can be continuously operated, the on-line regeneration can also be carried out when the catalyst is inactivated, and the production efficiency is greatly improved.

The invention discloses a preparation method of a levosimendan key intermediate 3-methyl-4-oxo-4-(p-amino)phenylbutyric acid, which comprises six reaction steps disclosed in the specification. The method has the advantages of novel technological design, accessible raw materials, environment-friendly reaction conditions, no need of virulent chemicals, high yield of each reaction step, high total yield and safe and simple operation, and is suitable for industrial production.

The invention discloses an application of 2-amino-3-phenylbutyric acid or a derivative thereof as a plant growth regulator. The invention discloses application of a compound shown in a formula (I) in preparation of a plant growth regulator. The compound shown in the formula (I) is 2-amino-3-phenylbutyric acid or 2-amino-3-(4-hydroxyphenyl) butyric acid. The plant growth regulator comprises the compound shown in the formula (I) in the claim 1 and a surfactant. The 2-amino-3-phenylbutyric acid and the 2-amino-3-(4-hydroxyphenyl) butyric acid are natural products, have simple structures, are easy for industrial production, can promote plant growth, and have the potential of being developed into natural plant growth regulators.

The present invention pertains to the enhanced activity of (+) epicatechin over (−) epicatechin. The present invention is related to novel analogs of (+) epicatechin of the formula (I), which enhances the pharmacokinetics and therefore the pharmacodynamics of (+) epicatechin. The present invention is related to analogs of (+) epicatechin of the formula (I). The general structure of the analogs of the present invention may be represented by Formula (I): Formula (I) wherein A and B are independently OR1 and C and D are independently OH; wherein R1 is independently C1 to C10 lower straight or branched chain acyclic or cyclic alkyl, or is selected from the group comprising, hydroxy butyric acid, dichloroacetic acid; phenyl butyric acid; valproic acid.

The invention discloses a sodium phenylbutyrate tablet and a preparation method thereof. Described sodium phenylbutyrate tablet is made up of sodium phenylbutyrate and diluent; Described diluent is filler, binding agent and lubricant; In described sodium phenylbutyrate tablet, described sodium phenylbutyrate and The mass ratio of the diluent is 1:0.2-1.5. The preparation method of the sodium phenylbutyrate tablet comprises the steps of: 1) mixing the sodium phenylbutyrate, the filler and the binding agent to obtain a mixture; 2) preparing the mixture granules and dried to obtain sodium phenylbutyrate granules; 3) mixing the sodium phenylbutyrate granules with the lubricant and then compressing into tablets to obtain the sodium phenylbutyrate tablets. Based on the strong hygroscopicity of the raw material of sodium phenylbutyrate itself and its large size (large proportion of the main drug), there are technical difficulties in the preparation. The present invention provides a product with stable quality, suitable hardness, simple and feasible process, and the dissolution level reaches the reference level. Preparations and sodium phenylbutyrate tablets with high bioavailability have filled the blank of sodium phenylbutyrate preparations in my country.

The invention provides a synthetic method for 4-amino-3-phenylbutyric acid hydrochloride. The synthetic method for 4-amino-3-phenylbutyric acid hydrochloride prepares 4-amino-3-phenylbutyric acid hydrochloride by preparing a first intermediate, a second intermediate, a third intermediate, preparing 4-amino-3-phenylbutyric acid and forming a salt. The synthetic method is a complete technology for synthesizing 4-amino-3-phenylbutyric acid hydrochloride, is simple in technology, high in yield and relatively low in cost, and mainly solves the problems that initial raw materials employed in the prior art are high in price, operation steps are tedious and the production process has large pollution.

The invention provides a 4-phenylbutyric acid solution capable of reducing endoplasmic reticulum stress and a preparation method thereof, and belongs to the technical field of solvent preparation. Themethod comprises the following steps that 1), 4-phenylbutyric acid is mixed with a serum-free DMF / F-12 culturing medium, an obtained mixture eddies for 8-12 min in water bath at the temperature of 48-52 DEG C, and pretreatment liquid is obtained; 2), the pretreatment liquid in the step 1) is subjected to standing for 22-26 h, and the 4-phenylbutyric acid solution capable of reducing endoplasmic reticulum stress is obtained. The DMF / F-12 culturing medium containing the 4-phenylbutyric acid is placed in air to alkalify the solution, damage of acidic substances to cells is balanced, and therefore the prepared 4-phenylbutyric acid solution capable of reducing endoplasmic reticulum stress can reduce toxicity to the cells.

An effective dose of a pharmaceutically acceptable phenylbutyrate salt such as sodium phenylbutyrate applied to human ocular tissues or through injection or other means prevents ocular hypertension and treats glaucoma in humans, leading to a new medical therapy for lowering the intraocular pressure via a mechanism different from the existing glaucoma medications. This compound can be formulated in combination with topical or other forms of steroids in prevention and treatment of steroid induced ocular hypertension and glaucoma.

The invention relates to the technical field of landscaping and provides a garden plant planting method aiming at the problem of difficulty in nutrient absorption of tree seedlings. The garden plant planting method includes steps: S1 tree seedling pretreatment; S2, planting soil preparation; S3, planting pretreatment; S4, tree seedling planting. A soil additive is prepared from, by mass, 15-20 parts of urea, 1-2 parts of metalaxyl, 0.3-0.5 part of vermiculite, 0.5-1 part of eucalyptus leaf extract, 10-15 parts of metal salt, 50-55 parts of fertilizers, 1.5-2 parts of aminobenzoic acid, 0.1-0.5part of phenylbutyric acid and 0.5-1 part of potassium ortho-nitrophenolate. By adoption of rooting solution for pretreatment of tree seedling roots and adoption of planting soil for wrapping the tree seedling roots prior to tree seedling planting, rooting of the tree seedlings can be better promoted while the tree seedling growth speed is increased, subsequent maintenance of garden plants is avoided while the tree seedling survival rate is increased, simplicity and convenience in operation are achieved, and reduction of subsequent maintenance cost is benefited.

The invention discloses the application of the composition of benzenebutanoic acid and a triazole antifungal drug and an antifungal product. Static and dynamic combined antifungal activity, on drug-resisting candida albicans (CA), of the composition of the triazole antifungal drug and benzenebutanoic acid is researched. When PBA is combined with FLC, ITC and VRC, the antimicrobial activity of the triazole antifungal drug on drug-resisting CA can be improved, a synergic antifungal effect can be realized, the drug resistance of drug-resisting CA on the triazole antifungal drug can be reversed, and a research direction is provided for development of new drugs and new application of old drugs. For CA (MIC>=512 mug / ml) resistant to FLC, ITC and VRC, minimal inhibitory concentration can be reduced remarkably through drug combination, over 80% fungi can be killed through combination of PBA of 32 mug / ml and FLC of 1 mug / ml, combination of PBA of 32 mug / ml and ITC of 0.125 mug / ml, and combination of PBA of 16 mug / ml and VRC of 0.25 mug / ml, and the effect is better as concentration becomes higher.