73 results about "Phenylpropanoic acid" patented technology

The presently described technology provides phenylethanoic acid, phenylpropanoic acid, phenylpropenoic acid, a salt thereof, a derivative thereof or a combination thereof chemically conjugated to hydrocodone (morphinan-6-one, 4,5-alpha-epoxy-3-methoxy-17-methyl) to form novel prodrugs or compositions of hydrocodone which have a decreased potential for abuse of hydrocodone. The present technology also provides methods of treating patients, pharmaceutical kits and methods of synthesizing conjugates of the present technology.

The invention mainly relates to a synthesis method of alvimopan. A preparation method of the related alvimopan comprises the following steps of: condensing phenylpropionic acid and substituted oxazolidone; undergoing reaction with chloromethyl benzyl ether under the action of a catalyst to obtain a single configuration; hydrolyzing, and recycling oxazolidone to obtain carboxylic acid; condensing with glycinate; performing deprotection and undergoing reaction with a leaving group donor; butting with (+)-(3R,4R)-4-(3-hydroxy phenyl)-3,4-dimethyl piperidine to obtain alvimopan ester; and hydrolyzing to obtain the alvimopan. The invention also relates to a novel intermediate of the alvimopan and preparation methods of the alvimopan and the novel intermediate of the alvimopan. The technical scheme of the invention has the advantages of simple process, low cost and high product purity, and is suitable for industrial production.

The invention belongs to the field of microbial fermentation, and especially relates to a fermentation metabolite having an effect of protecting skins, and a preparation method and applications thereof. The product is prepared by taking lactobacillus plantarum, lactobacillus casei, lactobacillus lactentis, bifidobacterium animalis and lactobacillus rhamnosus as fermentation strains and taking sucrose, seaweed meal, soybean meal and milk powder as fermentation raw materials through mixing and fermentation. The product contains specific fermentation metabolites, such as malonylgenistin, genistein, hyaluronic acid, irone, Preaustinoid A and daidzein, which are helpful for the enhancement of a skin protection effect; and tartaric acid, malic acid, succinic acid, salicylic acid, vanillic acid, phenylpropionic acid and other organic acid generated by fermentation can control pathogenic bacteria and spoilage microbial flora, so that skin flora balance can be maintained, and a natural antiseptic effect can be achieved. Efficacy tests show that the product has the efficacy of removing wrinkles, increasing skin elasticity, resisting inflammation and repairing skin barriers, and is significant in effect.

The invention provides novel substituted phenylpropionic acid derivatives that bind to the receptor as ligands of human peroxisome proliferator-activated receptor α (PPARα) to activate and exhibit potent lipid-decreasing action, and processes for preparing them.It relates to substituted phenylpropionic acid derivatives represented by a general formula (1)[wherein R1 denotes a lower alkyl group with carbon atoms of 1 to 4, lower alkoxy group with carbon atoms of 1 to 3, trifluoromethyl group, trifluoromethoxy group, phenyl group which is unsubstituted or may have substituents, phenoxy group which is unsubstituted or may have substituents or benzyloxy group which is unsubstituted or may have substituents, R2 denotes a hydrogen atom, lower alkyl group with carbon atoms of 1 to 4 or lower alkoxy group with carbon atoms of 1 to 3, R3 denotes a lower alkoxy group with carbon atoms of 1 to 3, and the binding mode of A portion denotes —CH2CONH—, —NHCOCH2—, —CH2CH2CO—, —CH2CH2CH2—, —CH2CH2O—, —CONHCH2—, —CH2NHCH2—, —COCH2O—, —OCH2CO—, —COCH2NH— or —CHCH2CO—], their pharmaceutically acceptable salts and their hydrates, and processes for preparing them.

The invention belongs to the field of synthesis of drug intermediates, and particularly relates to a preparation method of p-bromomethyl isophenylpropionic acid, which comprises the following steps: A, synthesis of alpha-methyl benzyl chloride: carrying out addition reaction on styrene serving as a raw material and hydrogen chloride gas in an organic solvent to generate alpha-methyl benzyl chloride, B, synthesis of 2-phenylpropionic acid: preparing alpha-methyl benzyl chloride into a Grignard solution through a Grignard reaction, the Grignard solution and carbon dioxide gas are subjected to acarboxylation reaction to generate a carboxylation solution, and the carboxylation solution is hydrolyzed to obtain 2-phenylpropionic acid, and C, synthesis of p-bromomethyl isophenylpropionic acid: carrying out bromomethylation reaction of 2-phenylpropionic acid, hydrobromic acid and polyformaldehyde so that p-bromomethyl isophenylpropionic acid is generated. The preparation method of p-bromomethyl isophenylpropionic acid provided by the invention has the advantages of cheap and accessible raw materials and simple technique, and is suitable for industrial production.

Cinnamic and phenylpropiolic acid derivatives of Formula (I) having antitumour and chemosensitizing activity are described. Also described are pharmaceutical compositions containing the above-mentioned compounds, for the treatment of tumours.

The present invention provides a new strain-Saccharomyces cerevisiae CGMCC NO.3361 and application thereof in preparing (R)-(+)-beta-hydroxy-benzenepropanoic acid ethylester by microbial transformation. The Saccharomyces cerevisiae was collected in China General Microbiological Culture Collection Center (CGMCC). The collection date is October 23, 2009 and the collection number is CGMCC NO.3361. The beneficial effects of preparing (R)-(+)-beta-hydroxy-benzenepropanoic acid ethylester by the microbial transformation method in the invention are mainly as follows: (1) the biocatalyst is a microbial thallus, thus is lower in cost than the chemical catalysts; (2) the environment is friendly, the reaction conditions are mild and the transformation can be carried out smoothly under normal temperature and normal pressure; (3) the strain used in the production is safe and nontoxic; (4) the method is not influenced by seasons and is easy to realize large-scale industrial production; (5) the production operation is simple and convenient and the biotransformation rate is higher; and (6) coenzyme is unnecessary to be added in the whole reaction process.

The present invention relates to the compounds according to Formula (I), the racemates, enantiomers, diastereomers thereof or pharmaceutical acceptable salts thereof, or pharmaceutical compositions comprising these, for the treatment or prevention of metabolic disorders. The compounds according to Formula (I) are, as GPR40 agonists, available for oral administration with glucose-dependent insulin secretion mechanism, which exhibit excellent glucose lowering efficacy without the risk of hypoglycemia. Thus, the compounds and / or pharmaceutical compositions comprising the compounds as effective components are useful in treating and / or preventing symptoms of type 2 diabetes through adequate control of blood glucose.

The invention discloses a tenofovir bisphenylpropionate phosphoramidate compound and salt thereof, and also discloses a preparation method and a pharmaceutical composition containing the tenofovir bisphenylpropionate phosphoramidate compound. Tests prove that the compound has the activity of inhibiting HBV virus replication, and has the advantages of higher activity, higher development coefficientand the like than the existing drug tenofovir disoproxil fumarate (TAF) for treating AIDS. The tests also prove that the compound also has the activity of inhibiting HIV1 virus replication, and can be used for developing medicines for treating AIDS or medicines for treating hepatitis B.

The invention relates to a synthetic method of novel chemicals, in particular to a preparation method of 2-guanidino phenylpropionic acid. The preparation method comprises the main steps: step one, stirring and mixing phenylalanine with purified water, thus forming a mixed solution; step two, regulating the PH (Potential of Hydrogen) value of the mixed solution to be 8 to 10 by using liquid caustic soda; step three, starting to dropwise add hydrogen cyanamide while rising the temperature of the mixed solution obtained in the step two to 60 to 80 DEG C; step four, starting to cool to 20 DEG C or less after keeping warm for 2 hours; step five, regulating the PH value of the mixed solution to be 6 to 8 by using hydrochloric acid; step six, centrifuging, drying and packaging. The 2-guanidino phenylpropionic acid is a new compound, a small amount of information shows that the 2-guanidino phenylpropionic acid is a derivative of aromatic amino acid needed by a human body, and the 2-guanidinophenylpropionic acid has a very important function in the fields of medicinal intermediates, food and feed. According to the preparation method disclosed by the invention, the 2-guanidino phenylpropionic acid is produced by adopting the phenylalanine, the liquid caustic soda, the hydrochloric acid and the hydrogen cyanamide as main raw materials, and the preparation method has the advantages thatthe technology is simple, the reaction is mild, the yield is high, the product purity is high, greening and environment protection are realized, and the like.

The invention discloses a 6-bromotryptamine derivative as well as a preparation method and application thereof. The 6-bromotryptamine derivative is characterized by being expressed by a structural formula (I) and comprising 6-bromotryptamine chloro-phenylacetic acid and 6-bromotryptamine phenylpropionic acid. The preparation method comprises the following steps: weighing chloro-phenylacetic acid or phenylpropionic aci, dissolving with dichloromethane, further adding EDC.HCl till a white muddy liquid is generated, further adding HOBt, stirring for 30 minutes at normal temperature till a white muddy phenomenon is vanished, detecting the reaction process through thin-layer chromatography, when new points occur, dropping dichloromethane in which 6-bromotryptamine is dissolved into a reaction liquid, performing stirring reaction at room temperature, leaving to stand over night, performing thin-layer chromatography detection, terminating reaction if raw material points are eliminated, boiling off a solvent so as to obtain a crude product, finally separating a trace product by using semi-preparative type liquid chromatogram, and purifying, thereby obtaining the 6-bromotryptamine derivative. The 6-bromotryptamine derivative has the advantages that AchE can be remarkably inhibited, and the 6-bromotryptamine derivative has the potential of being developed into medicines for treating the Alzheimer's disease.