98 results about "Raceme" patented technology

The invention relates to a method for separating a raceme based on a biological enzyme, in particular to an enzymatic separation method for racemizing 1-phenylethanol compound. The technical proposal adopted in the invention is that: the enzymatic separation method for racemizing the 1-phenyl ethanol compound comprises the following steps that: the vinyl acetate used as a raw material is reacted in organic solvent under the action of the biological enzyme to prepare an R-(+)-1-phenyl ethanol compound and an S-(-)-1-phenyl ethanol compound, and the reaction formula is shown as a top right formula, wherein R is one of or the combination of two or three of hydrogen, p-halogen, o-halogen, m-halogen, p-CN, o-CN, m-CN, p-C1 to C5 alkyl groups, o-C1 to C5 alkyl groups, m-C1 to C5 alkyl groups, p-nitro group, o-nitro group, m-nitro group, p-CF3,o-CF3 and m-CF3.

The present invention provides amine derivatives represented by formula I, its isomers, racemes or optical isomers, pharmaceutical salts thereof, its amides or esters, pharmaceutical compositions containing said compounds and the preparation methods thereof. The invention also relates to the use of the above mentioned compounds in the preparation of drugs for the prophylaxis or treatment of cardiovascular diseases, diabetes, bronchial and urinary smooth muscle spasm as well as ischemic and anoxic nerve injury. The above compounds can be used to treat hypertension, angina diaphragmatic, myocardial infarction, congestive heart failure, arrhythmia, diabetes, spasmodic bronchial diseases, spasmodic bladder or ureter diseases, and depression.

The invention relates to the chemical and medicinal technology field, and provides compounds with a structural characteristic in formula I and applications of the compounds and pharmaceutically acceptable salts, isomers, racemes, prodrug cocrystallization compounds, hydrates and solvates in preparation of medicines treating or preventing relative diseases with ROR regulation and control. Importantly, the compounds can be used for reducing generation of immunological factors relative to immunological diseases and alleviating immunologic derangement symptoms.

The invention provides a method for preparing a dipeptidyl peptidase-IV inhibitor, and in particular relates to a method for preparing 7-[3-amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl]-5,6,7,8-tetrahydro-3-trifluoromethyl-1,2,4-triazol[4,3-a]pyrazine raceme or an optically pure (R) or (S) compound thereof. The method comprises the following steps of: (1) performing hydrogenation reduction to obtain racemate; (2) reacting the racemate with camphorsulfonic acid or tartaric acid; and (3) converting a salt obtained in the step 2 into a corresponding alkali. The method has low cost and can be applied to industrial production.

The invention discloses a route and method for preparing 3-aminomethyl-5-methylhexanoic acid, namely pregabalin raceme hydrochloride. The method comprises the following steps of: performing condensation on 4-methyl-2-pentanone to obtain a compound in a formula (1), and performing reduction to obtain a compound in a formula (2); performing halogenation or esterification to obtain a compound in a formula (3a), and performing substitution to obtain a compound in a formula (4), or performing elimination on the compound in the formula (3a) to obtain a compound in a formula (3b) and performing addition to obtain a compound in the formula (4); and performing reduction and acidolysis on the compound in the formula (4) to obtain a pregabalin hydrochloride compound in a formula (6). The method is easy to operate, mild in reaction conditions, and low in cost, and is suitable for large-scale industrial production.

The invention provides a preparation method and novel use of amine compounds. Specifically, the invention provides compounds shown in the formula A or their optical isomers, racemes, solvates or pharmaceutically acceptable salts and a medical use thereof. The above compounds can be used for preparation of a pharmaceutical composition or a preparation. The pharmaceutical composition or preparationis used for (a) inhibiting a transient receptor potential channel protein TRPA1 and (b) treating diseases associated with the transient receptor potential channel protein, wherein each group is defined in the specification.

The invention belongs to the technical filed of polymer membrane separation and discloses a beta-cyclodextrin grafted polymer chiral separation membrane and a preparation method thereof. The method comprises the following steps: (1) with beta-cyclodextrin as the raw materials, preparing aldehyde cyclodextrin by reacting the beta-cyclodextrin with toluene sulfochloride and triethylamine in sequence; (2) performing aldolization with the aldehyde cyclodextrin and a polymer containing hydroxyl or Schiff base reaction with the aldehyde cyclodextrin and a polymer containing amidogen, so as to obtain a beta-cyclodextrin grafted polymer; and (3) dissolving the beta-cyclodextrin grafted polymer in a solvent to prepare a casting membrane liquid and preparing the beta-cyclodextrin grafted polymer chiral separation membrane by adopting a phase conversion method. The prepared beta-cyclodextrin grafted polymer chiral separation membrane can be applied for separating raceme, so as to realize green and efficient separation of chiral medicines.

The invention provides a novel synthetic method for the main intermediate compound-(2R)-3-methy-2-(4 -methoxy-3-(3-methoxy-C) benzyl)-1-butyl alcohol of hypertension drug Aliskiren. The invention adopts the method with the steps that firstly the raw material of 3-hydroxy-4-methoxy benzaldehyde is etherified by 3-methoxy bromopropane (mol ratio of 1:1 to 1.2), and then is condensed with isopentyl aldehyde (in mol ratio of 1:1 to 1.3); catalytic hydrogenation is performed to the condensation product; then the main intermediate compound of the hypertension drug Aliskiren is obtained through resolution. The method has the advantages that the raw material and the reagent are easy to be obtained, the cost is low, the synthetic process is short, and only three steps are required to prepare the raceme of the main intermediate compound of the Aliskiren; when the enzyme method is utilized to perform the resolution of the raceme, the main intermediate compound-(2R)-3-methy-2-(4-methoxy-3-(3-methoxy-C) benzyl)-1-butyl alcohol of the hypertension drug Aliskiren can be obtained.

The invention provides a compound with an effect of preventing and treating PD-L1 (programmed death-ligand 1)-related diseases as well as a preparation method and an application of the compound. Specifically, the invention provides the compound shown as the formula I in the description, as well as a stereoisomer, a raceme or a pharmaceutically acceptable salt of the compound, and provides the application of the compound to preparation of drugs for preventing and treating the PD-L1-related diseases.

The invention relates to a preparation method of artificially synthesized raceme nicotine, in particular to a preparation method of obtaining the raceme nicotine through two-step reaction of 4- methylamino-1-(3-pyridine)-butanone hydrochloride. The preparation method comprises the following specific synthesis steps: (1) dissolving 4-methylamino-1-(3-pyridine)-butanone hydrochloride by using an appropriate solvent in an appropriate reaction vessel, reacting under the conditions of an alkaline solution with appropriate concentration and an appropriate temperature, concentrating after ending reaction, and then purifying by using an appropriate solvent to obtain 1-methyl-2-(3-pyridine)-2-pyrrolidinol; and (2) reacting 1-methyl-2-(3-pyridine)-2-pyrrolidinol in an appropriate solvent in the reaction vessel under the conditions of an appropriate amount of reducing agent and an appropriate temperature, concentrating after ending reaction, and then purifying by using an appropriate solvent to obtain the raceme nicotine with high content and high purity. The preparation method of the artificially synthesized raceme nicotine is simple in process, low in cost, easy to operate, mild in reaction conditions, environmentally-friendly and suitable for industrialized production.

The invention belongs to the technical field of polymer membrane materials, and discloses a chiral-separation solid membrane grafted by a chiral identification body through dopamine pretreatment, and a making method and an application thereof. The method includes the following concrete steps: 1, immersing a solid membrane in a dopamine solution, stirring for reacting, and flushing with clear water; and 2, immersing the flushed solid membrane in a solution of the chiral identification body, heating for reacting, washing, and carrying out vacuum drying to obtain the chiral-separation solid membrane grafted by the chiral identification body through dopamine pretreatment. Firm and stable fctive function groups comprising -NH2, -OH and -C=O are introduced to the surface of the solid membrane through the above immersion technology; and chiral recognition sites are introduced to the surface of the solid membrane through the above immersion technology without influencing the structure or performances of the membrane, so the chiral-separation solid membrane grafted by the chiral identification body through dopamine pretreatment can be used for the effective separation of racemes The making method has the advantages of realization of the implementation of above reactions in an aqueous solution for a whole course, and mild and unharsh reaction conditions, development of the modification selectivity of the solid membrane, simple process, and easy realization of the industrialized batch production.

The three-zone supercritical fluid analog movable bed chromatographic equipment includes 3-36 stuffing columns connected successively with back pressure regulator, with the output of the last stuffing column being connected to the input of the first one with back pressure regulator. All the inlets of the stuffing columns are connected with the flow phase inlet pipeline and sample feeding port pipeline, all the outlets of the stuffing columns are connected with extracting port pipeline and residue port pipeline, and the outlets of the extracting port pipeline and the residue port pipeline have cyclonic separators connected separately. The flow phase is supercritical fluid, and the present invention may operate in either pressure gradient operation mode or modifier gradient operation mode. The present invention has supercritical CO2 fluid as the flow phase and chiral fixed phase as stuffing, and may be used in splitting chiral medicine raceme in large scale.

The invention discloses silica gel bonded with a single-chiral spiral polyether which has a frame structure of poly[3-(9-alkylfluoren-9-yl)-1,2-epoxy propane], a preparation method thereof, and application thereof used as a chiral immobile phase of a high-performance liquid chromatographic column. The invention has the following technical effects that: the silica gel bonded with a single-chiral spiral polyether which has the frame structure of poly[3-(9-alkylfluoren-9-yl)-1,2-epoxy propane] is used as the chiral immobile phase of the high-performance liquid chromatographic column, which can separate and analyze a plurality of racemes such as alcohols, ketones, esters, carboxylic acids and amines.

The invention relates to a 2-oxo-1,2-dihydrobenzo[cd] indole-6-sulfamide compound and a composition and application thereof. The invention provides a compound with the structural characteristics of the general formula I in the specification serving as a novel retinoic acid orphan nuclear receptor gamma subtype (RORgamma) inhibitor, as well as an application of the compounds and pharmaceutically acceptable salts, isomers, racemes, pro-drug co-crystallization compounds, hydrates and solvates thereof in medicines for treating or preventing RORgamma-regulated related diseases. More importantly, the compounds are possibly used for reducing generation of immune factors related to immunological diseases and alleviating symptoms of immunologic derangement and cancers.

The invention discloses a compound taking quinolizine ketone as a mother nucleus and for treating or preventing hepatitis B virus infection. The compound comprises optical isomer, raceme, cis-trans-isomer and any combination thereof or medicinal salt thereof. The invention further discloses a preparation method and application of the compound. The compound can remarkably lower in-vivo HBsAg leveland inhibit duplication of HBV, has good medicinal attribute and is low in toxicity, and pharmacokinetic and pharmacodynamic functions are improved; efficiency of combining with the HBV can be improved greatly, and clearance rate of in-vivo HBV can be further increased.

The invention provides compounds as shown in a general formula (I) which is described in the specification and cis-trans-isomers, enantiomers, diastereomers, racemes, solvates, hydrates, pharmaceutically acceptable salt and esters thereof. The invention further provides preparation method for the compounds, pharmaceutical compositions of the compounds and application of the compounds as modulators for an alpha5-GABAA receptor. T, Z, A and Y in the formula (I) are as defined in the specification.

The invention discloses a new method for resolution of a tetrahydroisoquinoline racemate, consisting of resolving the racemate by a resolving agent with an optical activity (formula II), precipitating diastereomers which S- takes most, getting diastereomer mother liquid which R- takes most, resolving with the resolving agent (formula III or IV) with another optical activity after dissociating the mother liquid, getting a single R-stereoisomer. The invention solves the problem of applying single resolving agent and gets the enantiomer with a high yield and a high optical purity and improves the efficiency and benefit, which can be widely used in the racemate resolution field.

The invention discloses a method for separating chiral compound metalaxyl by adopting a simulated moving bed in a fourth region. The method is characterized by adopting a simulated moving bed chromatography system, taking cellulose-tris(3,5-dimethylphenylcarbamate) as a filler and methanol and water as mobile phases and separating high-purity R-metalaxyl and S-metalaxyl from racemes of metalaxyl. The simulated moving bed chromatography system has the advantages of continuous production, high degree of automation and high production efficiency.

The invention relates to the medical field, discloses applications of racemes of pinocembrin, racemes of pinocembrin salt, racemes of pinocembrin precursors or racemes of pinocembrin hydrate in preparation of medicals for preventing and treating cerebral apoplexy, and further discloses the application of racemes of pinocembrin in prevention and treatment of acute ischemic stroke.

The invention relates to a preparation method of propranolol hydrochloride single enantiomers, comprising the following steps of: (1) preparing a saturated solution from a raw material drug of propranolol hydrochloride raceme; (2) injecting the saturated solution to a high efficiency liquid chromatography system, and separating according to conditions that n-hexane-ethanol-isopropanol-diethylamine is used as a mobile phase and a chiral chromatographic column is used as a stationary phase to obtain propranolol enantiomer fraction A and fraction B within different peak value ranges of a chromatogram map; (3) concentrating and then evaporating the propranolol enantiomer fraction A and fraction B respectively to obtain propranolol hydrochloride single enantiomer crude products A and B; (4) adding n-butyl to the propranolol hydrochloride single enantiomer crude products A and B respectively, and dissolving by heating to form hot saturated solutions A and B; and (5) filtering, cooling and drying the hot saturated solutions A and B respectively to obtain propranolol hydrochloride single enantiomers A and B. The preparation method of the invention is simple in process and can simultaneously obtain two enantiomers with high optical rotation purity at a high yield.

The invention belongs to the field of analytical chemistry and the technical field of pesticide residue detection, particularly provides a method for separating and measuring enantiomers of chiral pesticides metalaxyl and dimethomorph with UPCC-MS / MS (ultraperformance convergence chromatography-tandem mass spectrometry) and relates to a separating and quantitating method for raceme of multiple chiral pesticides. According to the method, metalaxyl and dimethomorph in tobacco and dried fruits are extracted with a QuEChERS method, and the enantiomers of the two chiral pesticides metalaxyl and dimethomorph are synchronously detected through combination of chiral stationary phase of bonded phase chromatography and triple quadrupole MS. The convergence chromatography is adopted for the first time for rapid chiral separation of metalaxyl and dimethomorph, and sensitivity is high; supercritical CO2 is taken as a moving phase, so that a large quantity of organic solvents are saved, and the method is environmentally friendly.

The present invention provides a synthetic method and application of 1, 6-dihydro pyridazine and pyridazine compounds in inhibition of growth activity of five common pathogenic fungis, the compounds are a compound shown as the formula I, a pyridazine compound shown as the formula III, or enantiomers, diastereoisomers, racemes, pharmaceutically acceptable salts, crystalline hydrates or solvate, wherein R1 is an optionally substituted aryl, optionally substituted benzyl or optionally substituted alkyl; R2 is an optionally substituted aromatic group; and R3 is p-toluenesulfonyl. The compound can be used in the treatment of related diseases caused by fungis.

The invention relates to the field of drug synthesis and pharmacology and in particular relates to a preparation method of a quercetin-O-glucoside derivative and an application of the quercetin-O-glucoside derivative to treatment of lipid metabolism disorders. The derivative is a compound in a formula I in the specification and comprises salt, optical isomers and racemes of the compound in the formula I. The invention aims to design and synthesize the quercetin-O-glucoside derivative. Through in vitro and in vivo pharmacological activity study, the quercetin-O-glucoside derivative can play a role in reducing the lipid in the in vivo and in vitro experiments. Besides, the invention also provides a drug composition for treating lipid metabolism disorders.

The invention pertains to the field of medical technology, which relates to a pair of new ginsengenins, the preparation method of the mixture thereof (raceme) and a novel anti-tumor preparation which contains the compounds as active ingredients. The names of the pair of compounds are 20(R)-25-methoxyl-dammarane-3 Beta, 12 Beta, 20-triol(known as 25Rmdt for short) and 20(S)-25-methoxy-dammarane-3 Beta, 12 Beta, 20-triol(known as 25Smdt for short). The compounds of the invention can be prepared by adopting acid hydrolysis method, alkaline hydrolysis method and synthesis method, and the preparation method is simple and feasible. The 25Rmdt, the 25Smdt, the mixture (raceme) and a pharmaceutically acceptable carrier can be made into the clinical feasible various formulations, studies prove that: the compounds and the preparations have significant anti-tumor effects, and can be made into any medicinal and health care formulation for the treatment of different cancers and be mainly applied in the prevention and the treatment of malignant tumors with the broad application prospect.

The invention belongs to the field of crop cultivation technologies, and particularly relates to a plant growth regulator and application thereof for regulating a phalaenopsis inflorescence type. Through applying the plant growth regulator in a process of inducing a bud of the phalaenopsis, the phalaenopsis with a raceme type is induced to be changed to the phalaenopsis with a compound raceme type. The plant growth regulator and the method can be used for different stages of low-temperature bud induction of the phalaenopsis, wider in using range, and have the better adaptability. Proved by a test, after the provided method and plant growth regulator are used, 2-3 dormant buds below a rachis flower of the phalaenopsis are totally germinated as a rachis, and the positive effect of improvingthe blooming quality of the phalaenopsis is achieved. The method is suitable for the industrial cultivation of the phalaenopsis, and the production cost is low. The obtained phalaenopsis is high in quality, good in consistency, has the advantages of low investment and high yield, and has the better popularization and application value.

The invention belongs to the technical field of polymer membrane materials, and discloses a hydrophilic chiral separation polysulfone membrane, and a making method and an application thereof. The method includes the following concrete steps: dissolving 1-10 parts by weight of a functional blend additive, 3-30 parts by weight of a pore forming agent and 10-100 parts by weight of polysulfone in 100-500 parts of an organic solvent to obtain a membrane casting liquid; dumping the membrane casting liquid onto a glass plate, and striking to uniformity; allowing the obtained glass plate to stand, immersing the glass plate in a solidification bath to form a membrane, putting the membrane in water for immersion, taking out, and carrying out vacuum drying to obtain a hydrophilic polysulfone membrane; immersing the hydrophilic polysulfone membrane in a phosphate buffer solution containing 1-ethyl-(3-dimethylaminopropyl)carbodiimide hydrochloride and N-hydroxysuccinimide, taking out the hydrophilic polysulfone membrane, and putting the hydrophilic polysulfone membrane in a phosphate buffer solution containing aminocyclodextrin to obtain the hydrophilic chiral separation polysulfone membrane which can be used for separating racemes.

The invention relates to Glycyrrhizin derivatives and preparation and use thereof, in particular to a compound in formula I: wherein, n is 0 or 1; R1 is C3-8 cycloalkyl; and R2 is H, as well as isomers, racemes, antimers, diastereomers, antimer concentrates, solvates, prodrugs and esters thereof. The invention further relates to a preparation method of the compound in the formula I, a pharmaceutical composition containing the compound in the formula I, and use of the compound in the formula I for preparing drugs for treating and / or preventing cerebral ischemic diseases, neurodegenerative diseases and inflammatory diseases. The compound in the formula I can be used for effectively treating and / or preventing the diseases described in the invention.