77 results about "Tetralones" patented technology

The invention provides a method for preparing cobalt-doped mesoporous alumina by taking a rubber latex as a biological template, and a method for catalytically oxidizing tetralin into tetralone under liquid phase. The invention relates to the method for preparing the cobalt-doped mesoporous alumina by taking the rubber latex as the template, and the method for synthesizing tetralone. The invention aims to develop a method which is used for preparing the cobalt-doped mesoporous alumina by taking the rubber latex as the biological template and a high-conversion and high-selectivity method which is used for catalytically oxidizing tetralin into tetralone under the liquid phase, and comprises the following steps: a mesoporous material is taken as a heterogeneous catalyst, and tetralin is catalytically oxidized into tetralone under the low temperature liquid phase. The experimental results show that the conversion rate of the tetralin reaches 80.3 percent and the selectivity of tetralone reaches 74.5 percent.

The invention relates to novel tetralone based amines and their use in the treatment of central nervous system (CNS) disorders, such as depression, attention deficit hyperactivity disorder (ADHD) and Parkinson's disease. The invention further relates to pharmaceutical compositions containing the compounds and compositions of the invention as well as methods of inhibiting reuptake of one or more monoamine, such as such as dopamine and norepinephrine, from the synaptic cleft, and methods of modulating one or more monoamine transporter.

A new family of indanone and tetralone tubulin-binding compounds (TBs) is disclosed. Unlike classical TBs, which inhibit mitosis among affected dividing cells, the TBs of the invention possess two unique properties: (1) they induce apoptosis among stationary phase (non-dividing) malignant cells, yet do not impair the viability of normal nonproliferating cells; and, (2) they affect cells which have acquired MDR more powerfully than they affect cells without MDR. Thus, the TBs of the invention provide means to target malignant cells for chemotherapy, even after previous therapies have failed, without affecting normal cells and tissues in the host.

The invention relates to a method of preparing Alpha-tetralone by catalysis and oxidation of tetralin, comprising following steps: quinonyl compounds and N-hydroxyphthalimade are combined to be double-component non-metallic catalysis system; air or oxygen is used as oxygen source to prepare Alpha-tetralone through catalysis and oxidation of tetralin with high efficiency under a certain condition; the applied quinonyl compounds comprise organic compounds, such as benzoquinones, naphthoquinones and anthraquinones and substituted derivatives of the organic compounds. The invention has the advantages of mild preparation conditions for the method of preparing the Alpha-tetralone, high efficiency and environmental friendliness.

The invention relates to a method for synthesizing alpha-tetralone by gas solid phase reaction. Benzene and gamma-butyrolactone are taken as raw materials; a molecular sieve is taken as a catalyst; the alpha-tetralone is continuously synthesized in a fixed bed reactor by the gas solid phase reaction; the reaction temperature is 210-300 DEG C; the reaction is carried out under the condition that the liquid space velocity is 1-6.0 h<-1>; the average conversion rate of gamma-butyrolactone is 25-79%; and the average mole yield of alpha-tetralone is 5-40%. The catalyst which is devitalized can be reproduced through oxygenation ignition to recover the catalyst performance. The method for synthesizing alpha-tetralone has the characteristics of avoiding the problems of not reusing the catalyst and discharging a great amount of acidic waste water. A serialization synthetic process is beneficial to automation production and production efficiency and enhances the production efficiency.

The invention discloses a method for extracting, separating and purifying chemical components of walnut green seedcases and application of the chemical components. According to the method, 13 compounds are separated from the walnut green seedcases and respectively identified as 3,5-dimethoxy-4-hydroxy-benzoic acid-7-O-beta-D-glucoside (1), myricananin F (2), beta-sitosterol (3), oleanolic acid (4), walnut ketone (5), asiatic acid (6), hederagenin (7), beta-carotene (8), (4R)-4,8-dihydroxy-alpha-tetralone-4-O-beta-D-glucopyranoside (9), 3beta,23-dihydroxy-12-olefin-28-ursolic acid (10), ursolicacid (11), syringic acid (12) and Juglanoside B (13). After screening of anti-tumor activity in vitro, it is found that some compounds have certain growth inhibitory activity against cancer cells andcan be further used for preparing anticancer drugs.

The invention relates to a method for preparing a lasofoxifene intermediate (namely, a compound IV) or an inorganic acid salt thereof. The method comprises the following steps: after a compound I is converted into a Grignard reagent, reacting the Grignard reagent with 6-methoxy tetralone so as to obtain a compound II or an inorganic acid salt thereof; carrying out bromination reaction on the obtained compound II or the inorganic acid salt thereof so as to obtain a compound III or an inorganic acid salt thereof; and then, carrying out coupling reaction on the obtained compound III or the inorganic acid salt thereof so as to obtain the lasofoxifene intermediate (namely, the compound IV) or the inorganic acid salt thereof. The compound IV or inorganic acid salt thereof is a key intermediate for preparing a medicament lasofoxifene for treating osteoporosis. The method provided by the invention is low in production cost, good for environmental protection, and suitable for industrial production.

The invention relates to substituted benzylidene tetralone derivatives and a preparation method and application. The chemical structural formula of the substituted benzylidene tetralone derivatives is shown in the formula (1) in the specification, and in the formula (1), X represents CHOH or C=O, and R represents any one of H, OH, F, Cl, CN, CONH2, NO2, CH3, OCH3 and NH2. In the synthetic route, any substitution group can be introduced into two benzene rings, thus eliminating the limit on organic synthesis for finding out compounds with better activity. After water-soluble groups such as amino and the like are introduced, the water solubility can be greatly improved compared with a pilot compound CA-4, and the research of druggability is facilitated. In addition, after amino, hydroxyl and the like are introduced, not only can the bioactivity be improved, but also a prodrug can be prepared on the basis of the group, and the in-vivo activity study can be favorably conducted. The derivatives have the effects of treating ovarian cancer, colon cancer, thyroid cancer and leukemia.

The invention relates to a method for catalytically oxidizing tetrahydronaphthalene to tetralone in liquid phase. The invention relates to the synthesis method of ketone compounds, particularly the synthesis method of tetralone. The invention aims to develop a method for catalytically oxidizing tetrahydronaphthalene to tetralone in liquid phase at high conversion rate and high selectivity. The method selects a mesoporous material as a heterogeneous catalyst to catalytically oxidize tetrahydronaphthalene to tetralone under the condition of low temperature and liquid phase. The test result shows that the conversion rate of tetrahydronaphthalene is 97.6%, and the selectivity of tetralone is 75.5%.

The invention discloses technology for preparing 5-methoxyl-2-tetralone, which belongs to a method for preparing tetralone compounds and is technology for preparing the 5-methoxyl-2-tetralone by using sodium metals to reduce 1,6-dimethoxy benzene in an alcohol medium and an ammonia medium at a temperature of between 15 and 35 DEG C, wherein the weight ratio of anhydrous alcohol to the 1,6-dimethoxy benzene during reduction is 6.0-9.0:1; the weight ratio of an ammonia liquid to the 1,6-dimethoxy benzene is 0.05-0.4:1; the weight ratio of the sodium metals to the 1,6-dimethoxy benzene is 0.7-1.2:1; and the reduction temperature is between 15 and 35 DEG C, and the reduction time is between 35 and 48 hours. The technology for preparing the 5-methoxyl-2-tetralone has the advantages of easily obtained reaction raw materials, simple conditions, easy industrialization and high selectivity of the 5-methoxyl-2-tetralone. The 5-methoxyl-2-tetralone is important medical intermediate, and is mainly used for synthesizing medicines for treating Parkinson's disease.

The invention discloses an alpha, beta-unsaturated carbonyl tetralone derivative and application thereof. The alpha, beta-unsaturated carbonyl tetralone derivative has the following structural formula, wherein R1 represents methylene or -HC-CH3; R2 represents hydrogen atoms or methoxyl; R3 represents hydrogen atoms, chlorine atoms, methoxyl, bromine atoms, fluorine atoms or nitryl; R4 represents hydrogen atoms or methoxyl; R5 represents hydrogen atoms, hydroxyl or methoxyl; R'3 and R'4 respectively represent hydrogen atoms or methoxyl; R'6 represents chlorine atoms or bromine atoms. The synthetic compound has pharmacological activities associated with anti-Alzheimer's disease, and is suitable for serving as a drug that can prevent, treat and diagnose Alzheimer's disease, and has a good potential application prospect. (Please see the formula in the description).

A process for preparing indanylamine and aminotetralin derivatives from indanone or tetralone oximes by acylating the oximes with an organic anhydride, followed by catalytic hydrogenation in the presence of an organic anhydride with subsequent hydrolysis is described. The process is commercially feasible providing indanylamine and aminotetralin derivatives in high yield that are useful as intermediates in the production of therapeutically active compounds. Also described are novel intermediates, 1-indanone O-acetyl oximes and 1-tetralone O-acetyl oximes.

The invention provides a manganese-base catalyst for synthesizing alpha-tetralone from tetrahydronaphthalene and a preparation method thereof, belonging to the technical field of catalyst preparation. The manganese-base catalyst provided by the invention uses active aluminum oxide as a supporter; and Mn oxide is used as the main active component of the catalyst, and oxide of Zr, Co, Fe, Cu or Ce is used as the auxiliary active component of the manganese-base catalyst. The preparation method comprises the following steps: impregnating the active aluminum oxide supporter in a mixed solution of Mn nitrate and nitrate of Zr, Co, Fe, Cu or Ce, drying, and roasting to obtain the catalyst. The manganese-base catalyst provided by the invention has the outstanding advantage of high low-temperature activity, has the characteristic of low cost, can completely substitute toxic chrome-containing catalyst, and has favorable industrial application prospects. For example, after the reaction is carried out at 90 DEG C for 8 hours by using oxygen as an oxidizer, the conversion rate of tetrahydronaphthalene is up to 51.67%; and after the reaction is circulated four times, the activity of the catalyst is basically unchanged, and the peroxide content in the product is very low.

The invention discloses a method for preparing benzothiazole quinazoline derivatives through catalysis and belongs to the technical field of ionic liquid catalysis. In the preparation reaction, the molar ratio of 2-aminobenzothiazole derivative to alpha-tetralone to aldehyde is 1:1:(1-1.1), the molar use amount of a double sulfonate radical acidic ionic liquid catalyst is 5 to 8 percent of the molar use amount of 2-aminobenzothiazole derivative, the volume amount of reaction solvent water based on milliliter is 5 to 7 times of the molar weight of the 2-aminobenzothiazole derivative based on millimole, the reaction temperature is 65 to 78 DEG C, and the reaction time is 24 to 57 minutes; after the reaction, cooling is conducted to room temperature, suction filtration is conducted, and the filter residue is washed with ethanol and vacuum-dried to obtain the benzothiazole quinazoline derivatives. Compared with the existing preparation method, the method for preparing the benzothiazole quinazoline derivatives through catalysis has the characteristics that the use amount of catalyst is small, the catalytic activity is stable, biodegradation is facilitated, the whole preparation process is simple and convenient to operate, and the greening degree is high; and industrialized large-scale production is realized easily.

The invention belongs to the field of chemical pharmacy and relates to a 7beta-methyl-tetralone derivative shown in a general formula (I) and a preparation method thereof. According to the compound shown in the general formula (I), with thebaine as a raw material, through related conversion methods such as N-demethylation, N-acylation, a Diels-Alder reaction and reduction, oxidation and Grignard reactions, the compound is synthesized. The compound shown in the general formula (I) belongs to an opioid receptor ligand, a radioactive receptor ligand combination experiment is adopted, the affinityand selectivity of the ligand to three subtypes of an opioid receptor are measured, and a [35S]GTPgammaS combination experiment is adopted for measuring the excitement inhibitory activity of the ligand; it is proved through a result that the compound has the functions of alleviating pain, resisting depression, withdrawing opioid addiction, relieving itching and the like and can be applied to preparation of an opioid receptor treatment medicine and applied to clinical analgesia or depression resistance or opioid addiction withdrawal treatment or itching relieving treatment.

The invention discloses a preparation method of 3-bromo-1,3,4,5-tetrahydro-2H-benzazepine-2-keto. The preparation method comprises the following stages: alpha-tetralone preparation stage, 2-bromo-3,4-dihydro-N-hydroxy-(2H)-naphthalimide preparation stage and 3-bromo-1,3,4,5-tetrahydro-2H-1-benzazepine-2-keto, wherein the alpha-tetralone preparation stage comprises the following steps: after mixing gamma-butyrolactone, benzene and aluminum chloride anhydrous, raising the temperature to be 60-90 DEG C, and preserving the temperature for reaction for 5-30 hours; after the reaction is finished, performing hydrolysis, layering and washing on 25 parts of 6% hydrochloric acid solution until neutral; and then distilling to remove excessive benzene, and performing high vacuum rectification to obtain alpha-tetralone. Then, the finished product is finally prepared through a bromination reaction, an oximation reaction and a beckmann rearrangement reaction, the purity of the finished product is high, and the yield is as high as more than 90%. Moreover, the production technology is simple, the production cost is low, and the pollution is little.

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 compound with tumor inhibition activity, and a preparation method and application thereof. The compound is diglucoside; one position is simultaneously connected with two molecules of saccharide; a concrete structural formula is 4(S)-4,5-dihydroxy-alpha-tetralone 5-O-beta-D-glucopyranose (1->6)-beta-D-glucopyranoside. Experiments show that the compound provided by the invention has a better inhibition effect on human cervical carcinoma cells and lung cancer cells.

The invention discloses a novel method for preparing alpha-tetralone by using tetrahydronaphthalene as a raw material. The method comprises the following two steps: a first step, under the condition without solvent and assistant, 1 to 20 atm (absolute pressure) of air or oxygen or mixed gas of oxygen and inert gases is introduced, the reaction temperature is between 60 and 150 DEG C, monometallic porphyrin of general formula (I) or (II) and mu-O-bimetallic porphyrin or solid carriers thereof are used as a catalyst, the concentration of the catalyst is 1 to 80 ppm, the reaction time is 1 to 12 hours, and oxidized mixed solution containing high alpha-tetrahydronaphthalene peroxide and alpha-tetralone can be selectively obtained; and a second step, the alpha-tetrahydronaphthalene peroxide in the oxidized mixed solution obtained in the first step is high selectively and directionally decomposed into the alpha-tetralone by using transition metal salt as a catalyst. In the step of catalytic decomposition, the molar ratio of transition metal irons to the alpha-tetrahydronaphthalene peroxide is 1:1-100, and the reaction temperature is between 0 and 100 DEG C. The method has the advantages of short reaction time, mild reaction conditions, little using amount of the catalyst, high conversion rate and good selectivity of a target product; and the used catalyst is environment-friendly and has no corrosion to equipment.

The invention discloses a synthesis method of 2-chloro-4-phenylbenzoquinazoline, and belongs to the field of organic chemical synthesis. In the synthesis method, 1-tetralone, benzaldehyde and urea areused as raw materials, and thereby the 2-chloro-4-phenylbenzoquinazoline is obtained through three steps of reaction of bigeminy reaction ring closing, oxidation and chlorination. The method has theadvantages of low requirements on equipment and reaction conditions, accessible raw materials, low cost and short process period, and can greatly enhance the synthesis efficiency and economic benefit.

The invention discloses a method for preparing agomelatine represented by structural formula 1. The method includes that 7-methoxy-tetralone represented by structural formula 5 is reacted with dimethyl cyanomethylphosphonate in an aprotic polar solvent under the sodium hydride catalytic action to generate (7-methoxyl-3,4-dihydro-2H-naphthalene-1-subunit) acetonitrile represented by structural formula 4, under the presence of an aromatization reagent, the (7-methoxyl-3,4-dihydro-2H-naphthalene-1-subunit) acetonitrile represented by the structural formula 4 is reacted with an organic acid to generate 1-cyano-7-methoxyl-1-naphthyl alcohol ester represented by structural formula 3, hydrogenation reduction is performed in an ammonia containing alcohol solvent under the catalysis of raney nickel to generate 2-(7- methoxyl-1-naphthyl) ethylamine represented by structural formula 2, finally the 2-(7- methoxyl-1-naphthyl) ethylamine represented by the structural formula 2 is reacted with acetic anhydride to generate the agomelatine represented by structural formula 1, and the agomelatine is separated out in a solid form. The method for preparing the agomelatine represented by the structural formula 1 has the advantages that the synthetic route is short, the reaction conditions are simple and mild, the raw materials are cheap and easy to obtain, the method is environment-friendly, the product yield and purity are high and the like, and the method is suitable for mass industrial production.

The invention discloses application of a bonded 3,5-dimethylcarbaniloylated beta-cyclodextrin chiral stationary phase in chiral analysis and/or separation of a sertraline hydrochloride intermediate (+/-)-Tetralone. The invention also discloses application of the bonded 3,5-dimethylcarbaniloylated beta-cyclodextrin chiral stationary phase in chiral separation of a sertraline hydrochloride intermediate (+/-)-Tetralone by simulated moving bed chromatography. The cyclodextrin chiral stationary phase can have better separating effects than the existing chiral stationary phases under identical conditions. The separation method, which adopts a four-region simulated moving bed system and uses a bonded 3,5-dimethylcarbaniloylated beta-cyclodextrin chiral stationary phase as a chiral column filler and an n-hexane-fatty alcohol mixed solution as a mobile phase, has the advantages of continuous sampling, high automation degree, high product purity and low mobile phase consumption, is suitable for industrialized chromatographic separation on (+/-)-Tetralone to obtain the optically Tetralone isomer product, and widens the application range of the cyclodextrin chiral stationary phase in the preparative chromatography system.

The present invention discloses a montelukast sodium preparation technology and intermediates; 7-chloro-2-methylquinine and 3-bromobenzaldehyde are used as raw materials for condensation reaction to obtain a compound A2; by carbon-carbon coupling of the compound A2 and 1-tetralone in the presence of a catalyst, an intermediate compound A3 is obtained; an important intermediate compound A4 is obtained by bio-enzyme catalyzed asymmetric Baeyer-villiger reaction, a chiral center is highly selectively constructed, an important intermediate compound A5 is prepared from the compound A4 by grignard reaction by use of methylmagnesium chloride, finally montelukast sodium (A6) is obtained; according to the technology, the highly chiral important intermediate compound A4 is obtained by bio-enzyme catalyzed asymmetric reaction, the catalyst can be effectively repeatedly used, and the kind of used solvents is less, and the montelukast sodium preparation technology has the characteristics of safety and environmental protection, greatly saves the production cycle, is low in production cost, high in total yield, and simple in operation of production units, and is suitable for industrialized production.