142 results about "Phenethylamine" patented technology

Chemical syntheses and medical uses of novel inhibitors of the uptake of monoamine neurotransmitters and pharmaceutically acceptable salts and prodrugs thereof, for the treatment and / or management of psychotropic disorders, anxiety disorder, generalized anxiety disorder, depression, post-traumatic stress disorder, obsessive-compulsive disorder, panic disorder, hot flashes, senile dementia, migraine, hepatopulmonary syndrome, chronic pain, nociceptive pain, neuropathic pain, painful diabetic retinopathy, bipolar depression, obstructive sleep apnea, psychiatric disorders, premenstrual dysphoric disorder, social phobia, social anxiety disorder, urinary incontinence, anorexia, bulimia nervosa, obesity, ischemia, head injury, calcium overload in brain cells, drug dependence, and / or premature ejaculation are described.

Phenylethylamine analogs useful for treating glaucoma are disclosed.

The invention discloses Omega-transaminase from bacillus pumilus and application in biological amination, and belongs to the technical field of bioengineering. In the invention, an Omega-transaminasegene is separated and identified from bacillus pumilus for the first time, and by adopting an escherichia coli recombination expression system to produce codon optimized Omega-transaminase, the yieldcan be remarkably increased, and the requirements of industrial application are met more easily. The invention discovers that the most proper action pH of the Omega-transaminase is 7.0 and the most proper action temperature is 45 DEG C when (R)-Alpha-phenethylamine serves as a substrate; meanwhile, the R-Omega-transaminase has excellent pH stability and temperature stability, and the catalytic activity on the experimental group (taking (R)-Alpha-phenethylamine as a substrate) is higher than that on the control group (taking (S)-Alpha-phenethylamine as a substrate), indicating that the recombinant Omega-transaminase has a function of synthesizing R-chiral amine with perfect selectivity and has relatively great application potential.

The invention provides a 1-phenyl-1, 2, 3, 4-tetrahydroisoquinoline preparation method. The 1-phenyl-1, 2, 3, 4-tetrahydroisoquinoline preparation method comprises the following steps of: mixing benzoyl chloride or benzoic acid, phenethylamine and alkali metal hydroxide with water, and reacting to obtain N-(2-phenethyl) benzamide; then mixing the N-(2-phenethyl) benzamide with phosphorus pentoxide, chloride phosphorus and a benzene solvent, heating and reacting to obtain 1-phenyl-3, 4-dihydro-isoquinoline; and further mixing the 1-phenyl-3, 4-dihydro-isoquinoline with a first alcohol solvent and hydroboron, and reacting to obtain the product. Compared with the prior art, the 1-phenyl-1, 2, 3, 4-tetrahydroisoquinoline preparation method has the advantages that firstly, no organic solvents are added, the product N-(2-phenethyl) benzamide is insoluble in an aqueous solution, and therefore, the steps of skimming and the like are avoided in the after-treatment process, and the after-treatment operation is simplified; secondarily, as the organic solvents are not added, the cost is reduced, and the pollution to environments is avoided; and thirdly, as the phosphorus pentoxide and the chloride phosphorus are subjected to oxidization cyclization reaction, polyphosphoric acids are prevented from being heated and decomposed to generate hypertoxic phosphorus oxide exhaust gas.

A producing method for a R-5-(2-aminopropyl)-2-methoxybenzsulfamide is provided, which is including: catalyzed by Pd / C, doing an ammoniation hydrogenation reaction in the organic solvent making use of the chiral phenethylamine and 2-methoxy-5-(2-oxopropyl)benzsulfamide to get a product and acidifying to a hydrochlorate; removing the eshyl phenyl in a condition of hydrogen to get a R-5-(2-aminopropyl)-2-methoxybenzsulfamide hydrochlorate; further reacting with alkali to produce R-5-(2-aminopropyl)-2-methoxybenzsulfamide. The producing method is simple with a good yield and can obtain the product with a high optical purity and can be an industrial production method as the intermediate of the tamsulosin medicine.

The invention discloses application of trans-cucurbit(7)uril in recognition of biogenic amines. Trans-cucurbit(7)uril can be used for recognizing tryptamine by the following steps: (a) adding trans-cucurbit(7)uril into a nuclear magnetism tube, adding D2O, and vibrating to dissolve, so as to obtain a product A; (b) storing tryptamine into a frozen storage pipe, adding D2O to dissolve, so as to obtain a product B; and (c) successively adding the product B into the product A so as to obtain a corresponding nuclear magnetism spectrogram in each dropwise adding process until a series of nuclear magnetism spectrograms of a host-guest complex, making comparison on the nuclear magnetism spectrograms and a nuclear magnetism spectrogram of tryptamine, and determining biogenic amines as tryptamine when two groups of signal peaks Hg and Hf appear in the spectrograms, Hgs move towards a low field, Hfs move to a high field, peak forms of signal peaks of other Ha-He protons are widened and signal peaks move towards the high yield. Trans-cucurbit(7)uril can be used for recognizing six biogenic amines including tryptamine, spermine, spermidine, tyramine and phenylethylamine and is of a great significance to reveal of biological phenomena and processes.

The invention discloses a method for enzymatic resolution of phenethylamines by using a novel acyl donor, which comprises following steps: (1) adding parachlorophenol, organic acid, dicyclohexylcarbodiimide (DCC) and 4-dimethylaminopyridine (DMAP) with a molar ratio of 1:(1-2):(1-2):(0.03-0.05), reacting under stirring, filtering, concentrating and separating by column chromatography to obtain the acyl donor; alternatively adding acetophenone and sodium borohydride with a molar ratio of 1:1.2 into methanol, reacting under stirring, distilled under reduced pressure, water washing, carrying out extraction with dichloromethane, drying and concentrating to obtain phenethyl alcohol, adding phenethyl alcohol, acetyl chloride and triethylamine with a molar ratio of 1:(1-1.2):(1-1.3), reacting under stirring, washing with saturated sodium bicarbonate solution, drying, concentrating and separating by column chromatography to obtain the acyl donor; and (2) adding phenylethylamine and the acyl donor with a molar ratio 1:(0.6-1) into 2-4mL organic solvent, and reacting with 10-20 mg / mL lipase to obtain amide. The method of the invention has advantages of mild reaction conditions, fast reaction, high conversion rate and high optical purity of the product, and has great application value.

The invention discloses a method for splitting a gamma-dodecalactone chiral molecule. The method comprises the following steps of: under the alkaline condition, hydrolyzing gamma-dodecalactone into hydroxy acid; under the action of a catalyst, reacting a chiral splitting agent R-(+)-alpha-phenyl ethylamine with optical activity and the hydroxy acid to form a hydroxyl-acid salt complex; splitting and purifying the racemized hydroxyl-acid salt complex by using a recrystallization method; and under the action of the catalyst, acidifying and cyclizing the purified product to obtain chiral gamma-dodecalactone. According to the method disclosed by the invention, the problems of low half-quantity yield and high splitting cost in the splitting process of the gamma-dodecalactone chiral molecule inthe prior art are solved; and the method for splitting the gamma-dodecalactone chiral molecule with the advantages of high half-quantity yield, chromatogram content as high as over 99.9 percent and higher utilization value in scale production is provided.