77 results about "Single isomer" patented technology

A process for synthesizing a single isomer of a naphthacene compound comprises the steps of: (a) reacting a symmetrically substituted 1,1-diarylpropargyl alcohol compound with a reagent capable of forming a leaving group to form a reaction mixture containing a intermediate; and then (b) heating the intermediate in the presence of a solvent and in the absence of any oxidizing agent to form a single naphthacene compound.

The invention discloses a method for preparing carotenoid microcapsules with controllable isomer proportion, which comprises the following steps of: adsorbing the single isomer of carotenoid with a stationary phase in a chromatographic column; taking the stationary phase out, adding the stationary phase into an autoclave according to required proportion and drying the stationary phase; introducing supercritical fluid to fully dissolve the isomer adsorbed by the stationary phase; after filtering, quickly releasing the solution above aqueous solution which contains an antioxidant and a protective colloid under reduced pressure in a spraying mode, and simultaneously controlling the emulsification temperature to be between 40 and 60 DEG C; and homogenizing and emulsifying for 5 to 30 minutes and then performing spray drying to obtain the finished product of the microcapsules. The method has the advantages that: 1) the particle size of the carotenoid reaches 0.04 to 0.6mu m and the bioavailability is high; 2) the proportion of the main isomer of any type of carotenoid can be controlled as required; 3) the product purity is high and solvent residue is avoided; and 4) the configuration of the isomer in the product can be effectively ensured. The method is particularly suitable for preparing carotenoid products as required, which have the controllable isomer proportion and can be applied to different fields, so that the physiological functions of the carotenoid are maximized.

The present invention is fermentation process of preparing conjugate linoleic acid with the seed of halophyte alfalfa as material. The process includes the following steps: 1. compounding culture medium, 2. pre-culturing the seed liquid via adding alfalfa seed oil and lactic acid bacteria to the culture medium, 3. fermenting to isomerizes and to obtain fermented liquid, and 4. extracting conjugate linoleic acid via dissolving the fermented liquid in isopropyl alcohol and extracting the fermented liquid with n-hexane. The preparation process of the present invention has low material cost, simple process, mild reaction condition and single isomer composition.

The invention discloses a novel method for preparing S-pantoprazole and salt, comprising the following steps: chiral separation reagents S-1,1,2-triphenyl-1,2-glycol and racemic pantoprazole react in an appropriate solvent, and the S-pantoprazole.S-1,1,2-triphenyl-1,2-glycol compound deposition is produced by filtering; the compound is dissociated by using alkali to remove S-1,1,2- triphenyl-1,2- glycol, then is neutralized by using acid, and neutral S-pantoprazole is obtained by filtering; and if S-pantoprazole salt is further required to be prepared, the S-pantoprazole prepared in the step (3) reacts with corresponding alkali in an appropriate solvent to obtain the S-pantoprazole salt. The method has high yield, high proportion of single isomer, simple technology, and convenient industrial production.

The invention discloses a ring opening method of aziridine compounds, particularly a ring opening method of aziridine compounds in different structures by using metal bromide, belonging to the technical field of organic synthesis. The aziridine compound is subjected to ring opening reaction by using tosyl-activated aziridine compounds as the initial raw material, dichloromethane as a solvent and bromine in the metal bromide as a nucleophilic reagent. The method has the advantages of simple reaction process, mild conditions and wide applicability, can obtain higher yield for aziridine compounds in different structures, has very high regioselectivity, and can form a single isomer from most aziridine compounds.

The invention discloses a preparation method for 3-aminopiperidine and an optical isomer thereof. The preparation method comprises the following steps of: reacting a compound shown in formula (I) with R2NH2 to obtain a compound shown in formula (II) or a compound shown in formula (III); removing an amino protecting group from the compound shown in formula (II) under the action of a metal catalyst to obtain the compound shown in formula (III) or a compound shown in formula (IV); and removing a primary amine protecting group from the compound shown in formula (III) to obtain the compound shown in formula (IV) or corresponding salts. According to the method, starting materials are low in the prices, simple and easily-available; reaction in each step is high in yield and few in by-products; reaction conditions are moderate, and racemized 3-aminopiperidine or 3-aminopiperidine with a single optical isomer can be obtained via the same method and only by changing the optical rotation of carbon atoms in the starting materials; moreover, the obtained optical isomer can achieve a high optical purity.

The invention relates to an alpha-L-rhamnosidase gene, an application thereof and a method for utilizing a brewer yeast surface display system to express alpha-L-rhamnosidase and utilizing the enzyme to catalyze flavonoid hydrolysis. According to the invention, the alpha-L-rhamnosidase gene (rhA) derived from Aspergillus niger is subjected to codon optimization, a brand-new alpha-L-rhamnosidase gene (corhA) is acquired, an expression carrier containing corhA is established and a brewer yeast strain containing the expression carrier is acquired. According to the invention, the brewer yeast surface display system is utilized to display and express the alpha-L-rhamnosidase gene (coRHA) on the brewer yeast cell surface, the extracellular substrate is in full contact with the enzyme, the catalytic efficiency is increased, the single isomer with physiological activity can be acquired, the separating and purifying steps are avoided and the production cost is lowered.

A pharmaceutical composition comprising a drug substance consisting essentially of a pharmaceutically acceptable organic acid addition salt of an amine containing pharmaceutically active compound wherein the amine containing pharmaceutical active compound is selected from the group consisting of racemic or single isomer ritalinic acid or phenethylamine derivatives and the drug substance has a physical form selected from amorphous and polymorphic.

The present invention provides a new preparation method and an intermediate of a nucleoside phosphoramidate prodrug, specifically a first-step reaction product is subjected to isomer separation, and two-step chemical synthesis is performed to prepare the high-purity compound (Sp-1). According to the present invention, the method has characteristics of simple operation and low cost; the purity of the finally prepared single isomer (Sp-1) is high, and the HPLC purity is more than 97% and further more than 99%; and the method is suitable for industrial production and can meet the needs of clinical research. In addition, the present invention further provides a key intermediate phosphorus reagent for preparing the high-purity compound Sp-1, and a preparation method thereof.

The invention discloses a ring opening method of aziridine compounds, particularly a ring opening method of aziridine compounds in different structures by using metal chloride, belonging to the technical field of organic synthesis. The aziridine compound is subjected to ring opening reaction by using tosyl-activated aziridine compounds as the initial raw material, dichloromethane as a solvent and chlorine in the metal chloride as a nucleophilic reagent. The method has the advantages of simple reaction process, mild conditions and wide applicability, can obtain higher yield for aziridine compounds in different structures, has very high regioselectivity, and can form a single isomer from most aziridine compounds.

The invention relates to a preparation method of an electron-deficient group-containing multi-substituted pyrazole derivative. The preparation method comprises the following steps of: dissolving electron-deficient conjugated enyne, hydrazine and alkali in an organic solvent, and enabling the mixture to react in a range of room temperature to 40 DEG C, removing the solvent and obtaining a crude product; and obtaining the electron-deficient group-containing multi-substituted pyrazole derivative shown in a formula (I) or formula (II) by column chromatography. The preparation method has the advantages of simple and easy obtaining of raw materials, simplicity and safety in operation, high atom economy, high yield and high selectivity. The aldehyde ketone and other functional groups containing multi-substituted pyrazole derivative with a single isomer can be conveniently and effectively obtained by one step, various compound skeletons are provided, and the method has important significance on synthesis of the substituted pyrazole compound.

The invention discloses a fermentation method of conjugated linoleic acid and a strain used in method, and relates to a method in which linoleate isomerase is expressed by using a saccharomyces cerevisiae surface display system, and capable of catalytic synthesis of t10, c12-conjugated linoleic acid by using the linoleate isomerase. An expression vector containing a propionibacterium acnes derived linoleate isomerase gene (pai) is constructed and a saccharomyces cerevisiae strain containing the expression vector is obtained. After the induction culture, the linoleate isomerase is displayed and expressed in saccharomyces cerevisiae, and the linoleate isomerase is added into a buffer solution containing substrate linoleic acid for catalytic reaction to generate the t10, c12-conjugated linoleic acid. According to the method provided by the invention, the linoleate isomerase is linked to cytoderm of the saccharomyces cerevisiae by the microorganism surface display system, so that extracellular substrates and the linoleate isomerase can be fully contacted, the catalysis efficiency is improved, a single isomer with physiological activity can be obtained, separation and purification steps are simplified and the production cost is reduced.

The invention relates to a splitting method of 2-hydracrylic acid racemic mixture. The method comprises the following steps of: carrying out optical active alkali reaction on 2-hydracrylic acid racemic mixture and L-prolinamide, separating a single isomer L-prolinamide salt of 2-hydroxyl acrylic acid compound; and taking the single isomer of the 2-hydroxyl acrylic acid compound as important intermediate for synthetizing endothelin receptor antagonist for treating cardiovascular disease. Therefore, the single isomer with high optical purity is separated by the splitting method which is simple to operate and is provided by the invention; and the method is cheap in required material and reagent, and suitable for industrial production, and has good economic benefit.

The invention relates to a composition gathering compounds (Sp-1). The in-vitro tumor cell proliferative activity suppression effect of the composition is remarkably higher than that of NUC-1031 and a compound (Rp-1). The invention further relates to a preparation method of the compound. The preparation method specifically comprises the step that reaction products are subjected to isomer separation and then two steps of chemical synthesis, and the composition containing high-purity compound (Sp-1) is obtained. The method is easy and convenient to implement and low in cost, the purity of the single isomers (Sp-1) in the finally obtained composition is high, and the purity of HPLC reaches 97% or over and further reaches 99% or over. The method is suitable for industrialized production, and the prepared composition can meet clinical research requirements. In addition, the invention further relates to application of the composition and a pharmaceutical composition containing the composition and at least one pharmaceutically acceptable excipient.

The invention discloses a nitrophenol isomer detection array, which is a beta-cyclodextrin (beta-CD) modification-based dual-ligand functionalized fluorescent Au nanocluster (Au NC) sensor array. A fluorescence quenching mechanism comprises two steps: first, beta-CD adsorbs a nitrophenol isomer to the surfaces of Au NCs under the interaction of a host and a guest; and second, nitrophenol quenchesfluorescence of the Au NCs through an internal filtering effect. Experimental results based on the sensor array show that three isomers can be well distinguished under a concentration of lower than 10[mu]M, and any two mixed isomers can still be well distinguished by the same analysis method. Therefore, the sensor array has substantial application prospect of distinguishing a single isomer from an isomer mixture.

The invention discloses a method for resolving a barnidipine mother nucleus by using glucosamine as a resolving agent. The method comprises the following process routes shown in the description: resolving the barnidipine mother nucleus by using the glucosamine as the resolving agent, wherein the easily available low-cost barnidipine is used as a chiral resolving agent for resolving the racemized barnidipine mother nucleus and solvents used in the middle are easily available and low-cost alcohol and water; and obtaining a single isomer of the barnidipine mother nucleus with high yield and high optical purity (ee value is 99.0-99.6%) with. The method has the beneficial effects that the resolving agent is low-cost and easily available, the using of expensive resolving agents is avoided, the used solvents are harmfulless, the resolution recovery rate is high, and the product has high optical purity and strong atom economy; the experiment operation is simple, reaction conditions are mild and easy to control, and the technology repeatability is high; and the implementation of the industrial production is easy.

A pharmaceutical composition comprising a drug substance consisting essentially of a pharmaceutically acceptable organic acid addition salt of an amine containing pharmaceutically active compound wherein the amine containing pharmaceutical active compound is selected from the group consisting of racemic or single isomer ritalinic acid or phenethylamine derivatives and the drug substance has a physical form selected from amorphous and polymorphic.

The invention discloses water-soluble camptothecine derivatives with its general formula being (I), its mono-isomer, antimer and relevant mixer, medical-use salt and active metabolism. The definition of R1 and R2 is expressed in instruction manual. The derivatives are prepared through Sonogashira reaction with 7- chloro- camptothecine by using palladium catalyst with existance of organophosphorus ligand and alkali. Said water-soluble camptothecine derivatives can resist tumor and can be used to prepare anti-tumor medicine.

Chiral fungicides and compositions containing the same are provided. Also provided are methods for using the compositions of the present invention for inhibiting the growth of fungi, including phytotoxic fungi. The use of a single isomer in treating particular plant species and against particular fungi allows for selective inhibition of fungal growth with reduced fungicidal phytotoxic effects.

A process for synthesizing the simple optical isomer nitrendipine features that under existance of quinine-ammonium benzylbromide as chiral phase-transfer catalyst, 2-(3-nitrobenzilidene) ethyl acetylacetate and beta-methyl amino crotonate take part in stereoselective condensating reaction in absolute alcohol to obtain target product.

The invention relates to an improved method for separating and purifying zuclopenthixol. The method comprises the specific following steps of: dissolving a mixture of an alpha-isomer (i.e. zuclopenthixol) and a beta isomer of 2-chloro-9-[3'-(N'-2-ethoxy piperazine-N)-allyl]-thiaxanthene into an organic solvent, adding an active benzoic acid derivative, and esterifying with the mixture so as to remove the beta-isomer; subsequently carrying out alkali hydrolysis on the residual substances so as to obtain relatively pure zuclopenthixol; and further recrystallizing by using organic solvent so as to obtain zuclopenthixol which meets the United States pharmacopeia standards. In addition, the invention further relates to preparation of a carboxylic ester and pharmaceutically acceptable acid salt of zuclopenthixol. The method has the advantages that the content of zuclopenthixol is improved by optimizing the reaction of different steps when the raw material, namely, alpha / beta-chlorine thiaxanthene, is prepared, a novel and effective method for purifying a single isomer is provided, and high-yield and high-purity zuclopenthixol is obtained by using the method.

The invention relates to a method for preparing a novel androgen receptor antagonist. The method mainly comprising the following step: performing a cyclization reaction on a compound of formula V as shown in the description, thereby obtaining a compound of formula VI as shown in the description. The method has the characteristics of being easy in raw material obtaining, high in atom utilization rate, mild in reaction condition and simple and convenient in aftertreatment; in addition, by controlling stereo-chemical configuration of initial raw materials, ODM-201 and single isomer thereof can bedirectionally synthesized, and the method is simple and controllable in process and applicable to industrial production.

The present invention relates in a first aspect to a process for hydrogenation of ketones having at least a carbon-carbon double bond in the y,8-position to the keto group by hydrogen in the presence of at least one chiral iridium complex of formula (I), where R1 represents a group of formula (II) or (III) or (IV). It has been shown that this process leads to a strong increase in preferential formation of a single isomer. The process is particularly suitable for the hydrogenation of y,8-unsaturated ketones which can be used as flavors and fragrances or for the preparation of vitamin E and its derivatives or of flavors and fragrances.

The invention provides a new method for separating and purifying a single stereoisomer (namely, a compound II) of Argatroban from Argatroban.

An improved method is described for making single isomers of synthetic benzoprostacyclin analogue compounds, in particular the pharmacologically active 314-d isomer of beraprost. In contrast to the prior art, the method is stereoselective and requires fewer steps than the known methods for making these compounds.

The invention relates to a preparation method and an application of an NUC-1031 single isomer. The method comprises specific steps as follows: a reaction product in the first step is subjected to isomer separation and then subjected to two-step chemical synthesis, and composition containing a high-purity compound (Sp-1) is prepared. The method is simple to operate and low in cost, the purity of the single isomer (Sp-1) contained in the finally prepared composition is high, and HPLC purity is 97% or higher and further reaches 99% or higher; the method is suitable for industrial production, and the prepared composition can meet clinical research demands. Besides, the invention further relates to an application of the composition and pharmaceutical composition containing the composition and at least one pharmaceutically acceptable excipient.

The invention relates to a method for expressing a linoleic acid isomerase by using a Saccharomyces cerevisiae surface display system and synthesizing t10, c12-conjugated linoleic acid through the catalytic action of the enzyme. The invention performs codon optimization on a linoleic acid isomerase gene (pai) derived from Propionibacterium acnes to obtain a brand new linoleic acid isomerase gene (copai), construct an expression vector containing the copai and obtain a Saccharomyces cerevisiae strain containing the expression vector. According to the invention, a microbial surface display system is used to express the linoleic acid isomerase (coPAI) on the surface of a Saccharomyces cerevisiae cell, so that an extracellular substrate can be in full contact with the enzyme, thereby improving the catalytic efficiency; and the single isomer having physiological activity can be obtained, the separation and purification step can be omitted, and the production cost can be lowered.

The invention pertains to photodynamic treatment field, in particular to photosencitizer of photodynamic treatment. The invention provides a reversed-phase purification method for separating a 3 (or 8)-(1-methoxyethyl)-8 (or 3)-(1-ethoxyl) deuteroporphyrin IX positional isomer. The method can be used for preparing an 8-(1- methoxyethyl)-3-(1-ethoxyl) deuteroporphyrin IX or 3-(1-methoxyethyl)-8-(1-ethoxyl) deuteroporphyrin IX single isomer. The two isomers, through an animal experiment, are proved to be applicable to blocking new-born veins effectively as the photosencitizer. The single isomer of the invention can be used for preparing medicine with single molecule structure and steadier properties.

The invention relates to a phosphoric acid / phosphonic acid derivative shown in a formula Ia and non-toxic pharmaceutically-acceptable salt thereof. The content of diastereoisomers shown in formula Ibis smaller than 2%; in the structural formulas Ia and Ib, Ar denotes a substituted or unsubstituted benzene ring or naphthalene ring, R1 denotes H or alkyl with the carbon atom number being 1-6; R2 denotes alkyl with the carbon atom number being 1-6 or naphthenic base; D denotes a residue of a pharmacological active molecule containing phosphoric acid / phosphonic acid groups, and that is, the groupshown in the specification denotes a pharmacological active molecule containing phosphoric acid / phosphonic acid groups.