113 results about "Absolute configuration" patented technology

The present invention relates to novel C-glycoside compounds of given absolute configuration, to a process for synthesising them and to compositions containing them. The invention also relates to the cosmetic use of these C-glycoside compounds as agents to stimulate the synthesis of glycosaminoglycans containing a D-glucosamine and/or N-acetyl-D-glucosamine residue, advantageously hyaluronic acid, and/or of proteoglycans, advantageously proteoglycans containing hyaluronic acid, by fibroblasts and/or keratinocytes. The invention also relates to a cosmetic process for treating keratin materials using a composition containing at least one C-glycoside compound according to the invention.

This invention belongs to pharmacy field, it relates optical pure mei pu ta fen and its preparation method and application. Racemation mei pu ta fen is splited by optical pure tartaric acid evolving object to get optical pure monomer, enantiomeric excess testing is done through capillary electrophoresis method, their e.e.valude are both excess 99 percent. Laevorotation and dextrorotation mei put a fen absolute configuration is decided by single crystal X-diffraction method as S and R. the R(+)mei pu ta fen has srong activity in analgesia activity testing, but S(-)mei pu ta fen has more stronger activity in acetylcholine esterase restrain activity testing, analgesic medicine and senile dementia medicine can be further prepared.

A process for efficiently producing compound (XIV) being useful as a drug intermediate on an industrial scale at low cost without the need to use ozonization and highly toxic agents; and an intermediate for use in the process. In particular, a process for producing a compound having the absolute configuration of the formula (XV) or an enantiometric isomer thereof without the need to use means such as optical resolution; and an intermediate for use in the process. (1) Compound (XIV) is produced by deriving compound (I) from compound (XIII) as a starting material and sequentially performing introduction of a protective group, reduction and cyclization. Particularly, compound (XIV) is produced by deriving compound (I) through compound (XX) from compound (XIII) as a starting material. Compound having the absolute configuration of the formula (XV) or the like is produced in high stereoselectivity from optically active compound (XIII) as a starting material. (2) Compound (XXVI) is produced by deriving compound (XXII) from compound (XXI) as a starting material through stereoselective reduction thereof and sequentially performing introduction of a protective group, reduction and cyclization. Compound (XV) is produced by inverting hydroxyl of the compound (XXVI). (1) (2) wherein symbols are as defined in the description.

The present invention provides a method for producing compound (XIV) useful as an intermediate for pharmaceutical agents efficiently and economically on an industrial scale without using ozone oxidation and highly toxic reagent, and an intermediate used for this method. Particularly, the present invention provides a method for producing a compound having an absolute configuration represented by the formula (XV) and an enantiomer thereof without using a technique such as optical resolution and the like, and an intermediate used for this method.

(1) Compound (XIII) as a starting material is led to compound (I), and after introducing a protecting group, subjected to reduction and cyclization to give compound (XIV). Particularly, compound (XIII) as a material is led to compound (I) via compound (XX) to produce compound (XIV). Using an optically active compound (XIII) as a starting material, a compound having an absolute configuration represented by the formula (XV) and the like are produced highly stereoselectively. (2) Compound (XXI) as a starting material is stereoselectively reduced to give compound (XXII), and by introduction of a protecting group, reduction and cyclization, compound (XXVI) is obtained, and by inverting hydroxyl group, compound (XV) is produced.

wherein each symbol is as defined in the specification.

The invention provides an inula wissmannian extract and preparation thereof and application in preparation of an antitumor drug. The extract is gemma alkane type sesquiterpene lactone inula wissmannian lactone methyl, ethyl, propyl, butyl and amyl or sheepear inula herb lactone. The extract has the following chemical structural formula and absolute configuration that: due to the toxicity killing function experiment of inula wissmannian lactone methyl, ethyl, propyl, butyl and amyl or sheepear inula herb lactone on human hepatoma cells HepG2, human prostatic cancer cells PC-3, human gastric carcinoma cells MGC-803, human leukemia cells K562, human nasopharynx cancer cells KB and normal human hepatocytes LO2, the result shows that the gemma alkane type sesquiterpene lactone has strong tumor cell killing function, and proliferation of tumor cells can be inhibited, so that the tumor cells are killed. The animal in-vivo experiment proves that the inula wissmannian plant extract and monomeric compounds have the anti-tumor effect and can serve as active ingredients for preparing the antitumor drug. A novel cancer treatment medicine is provided clinically, and high clinical application values and social benefits are generated.

The invention provides a preparation for inula wissmannian extracts and an application of the extracts in preparation of an anti-inflammatory medicine. The extracts are germacrane sesquiterpene lactone inula wissmannian lactones A, B, C, D and E and inula cappa lactone with the following chemical structural formulas and absolute configurations shown in the specification, wherein the inula wissmannian lactones A, B, C, D and E and the inula cappa lactone generate an inhibition effect on the NO of the RAW264.7 macrophage induced by LPS (lipopolysaccharide); and in an xylene-induced ear swelling mouse model and a Freund complete adjuvant arthritis rat model, the inula wissmannian lactones A, B, C, D and E and the inula cappa lactone are found to be able to obviously inhibit the ear swelling and foot swelling of experimental animals, and the result indicates that the inula wissmannian lactones A, B, C, D and E and the inula cappa lactone are good in anti-inflammatory activity, capable of being used for preparing an anti-inflammatory medicine, and great in application value. The invention provides an extraction and separation method for the inula wissmannian lactones A, B, C, D and E and the inula cappa lactone.

The invention relates to a puerarin monocrystal and a preparation method thereof. The puerarin monocrystal is named crystal form A, the CCDC number is 708830, the crystal structure is asymmetrical, each crystal cell contains two asymmetrical molecules, i.e. molecule a and molecule b, each of which carries a molecular crystal water, and moreover, the binding sites of the crystal waters are different. The crystal water of the molecule a and a hydroxyl group on a benzene ring carry out hydrogen bonding, the crystal water of the molecule b and a carbonyl group on a flavone mother nucleus carry out hydrogen bonding, the hydroxymethyl group of the glucose of the molecule a is at the position of an equatorial bond and perpendicular to a ring plane, the oxygen atom of the hydroxymethyl group is in a saccharide ring plane, the hydroxymethyl group of the glucose of the molecule b is at the position of an axial bond and perpendicular to a ring plane, the hydrogen on the rest pyranose carboatomic ring is an axial bond, the hydroxyl group is positioned at an equatorial bond, and the molecular formulas of the molecule a and the molecule b are the same, i.e. C21H20O9.H2O. The absolute configuration of the puerarin monocrystal is an asymmetrical isomer. The melting point of the puerarin monocrystal is increased, and the heat stability is remarkably enhanced compared with powder. The average purity of the puerarin crystal form A reaches 99.8 percent, higher than 99.1 percent of average purity of bulk pharmaceutical chemicals, and the quality is remarkably increased.

The present invention is a synthesis method of the shikonin dimethyl ester derivative in the pharmaceutical and chemical technological field. The synthesis method of the second-level side-chain isomer and the sixth-level side-chain isomer of the shikonin dimethyl ester of the present invention uses the shikonin as the raw material; the shikonin is first cyclized; then the cyclized shikomin is in the tetramethyl and ring-opening reaction; in the process, the absolute configuration of the shikonin is maintained; then the esterification or etherification is done; at last, the methyls are selectively doffed to get the target compound. The reagent in each step of the reaction is easy to get; the conditions are mild; the collection rates of the reaction all surpass 65 percent; the total collection rate is 33.2 percent (calculated by the shikonin). The reaction process has no racemic reaction.

The present invention provides a method for producing optically active flurbiprofen. The method of the present invention includes mixing racemic flurbiprofen and (S)- or (R)-3-methyl-2-phenylbutylamine in an organic solvent to produce a diastereomeric salt; and treating the diastereomeric salt with an acid in a second solvent. In the method of the present invention, flurbiprofen having a desired absolute configuration can be obtained very efficiently without repeating the procedure for optical resolution a plurality of times.

The invention belongs to the field of medical chemical engineering and relates to a chromone dipolymer derivative as well as a preparation method and application thereof. Specifically, the invention relates to a compound with formula I, wherein S and R respectively represent absolute configurations of corresponding marking carbon atoms; R1-R3 independently represent various substituent groups, respectively; R3 and H connected by a wavey line can orientate alpha or beta. The invention further relates to penicillium purpurogenum of the compound with the formula I. Experiments prove that the compound with the formula I has good anti-tumor activity, can be used for preparing biological reagents such as a tumor cell killing agent, a tumor cell proliferation inhibitor and an anti-tumor agent, and further can be used for preparing anti-tumor and anti-cancer drugs. The formula I is as shown in the specification.

The present invention is directed to analytical methods for determining the concentration, and/or stereoisomeric excess, and/or absolute configuration of chiral analytes in a sample.

The invention discloses a fluorinated quinolylamide foldamer, a preparation method, a chirality recognition method of the fluorinated quinolylamide foldamer and an application of the fluorinated quinolylamide foldamer. The fluorinated quinolylamide foldamer has a structural formula represented by a formula (1) shown in the description, wherein R1 and R4 represent alkoxy of any length and may be the same or different, X is an O or N atom, R2 is an electron withdrawing group, for example nitro or cyano, R3 is alkyl of any length, and n is a random positive integer. The fluorinated quinolylamidefoldamer disclosed by the invention can be applied to the recognition and ee value determination of absolute configurations such as chiral amines, chiral diamines, chiral amine alcohols and chiral amino-acid esters. According to the fluorinated quinolylamide foldamer, the preparation method, the chirality recognition method and the application, a chiral group is linked to the quinolylamide foldamer in a covalent bond mode in a manner that amino attacks the fluorinated quinolylamide foldamer under alkaline conditions, so that chirality is transferred to the quinolylamide foldamer, and absoluteconfigurations and ee values of chiral guest molecules are detected according to CD signals of corresponding quinolylamide foldamers.

A clean oil environmental protection equipment, its box is fixed with an upper partition and a sealing plate in the horizontal direction to divide the box into a filter room, a clean oil room and an oil storage room; The swallowing hole of the plate is fixed with an oil suction pipe closely connected with the telescopic pipe, a filter residue box is installed in the filter chamber, a clean oil float floats on the oil surface in the clean oil chamber, a filter screen is fixed at the oil suction hole, and the oil suction pipe passes through There is a drain switch at the bottom of the oil cleaning room, an oil pump for delivering edible oil is installed in the oil storage room, and an observation window is arranged on the box body. The structure of the clean oil environmental protection equipment is simple and applicable. It adopts the method of combining filtration and sedimentation treatment to realize the separation of oil and residue and oil and water at the same time in one piece of equipment, and the effect of clean oil is good. It does not produce pollution and does not use energy. The use cost is low; the edible oil purified by the clean oil environmental protection equipment is clean and hygienic, has good market prospects for industrialization, high commercial value, and is very convenient to manufacture and use.

The invention provides a pyrethroid compound which is a stereoisomer of 2,3,5,6-tetrafluoro-4-methoxybenzyl-3-(3,3,3-trifluoro-1-propenyl)-2,2-dimethylcyclopropane carboxylate. The compound is characterized in that the structure of the compound is shown in formula (A), wherein the carbon-carbon double bond in the carboxylic acid part of the formula (A) is Z configuration, the absolute configuration of the 1-site of cyclopropane is R configuration; the compound is 2,3,5,6-tetrafluoro-4-methoxybenzyl-1R-(Z)-3-(3,3,3-trifluoro-1-propenyl)-2,2-dimethylcyclopropane carboxylate. The pyrethroid compound has high activity and significant effect for controlling the pestiferous pests. The invention also provides a preparation method and an application of the pyrethroid compound.

The invention discloses a group of platinum (II) coordinated complex having effective anticancer activity, which is represented by the structural formula (1) disclosed in the specification, wherein R groups are the same, which are hydrogen atoms or C1-5 alkyl, the cyclohexane diamine is 1,2-trans-cyclohexane diamine, R3 and R4 in formula (3) can be identical or different, which are hydrogen atom or C1-5 alkyl, or can connect with a carbon atom to form a cycloalkyl.

The invention provides a method for obtaining a pair of optical isomers by resolving racemic 1-cyclohexyl-2-(5H-imidazole[5,1-a]isobenzazole)ethyl-1-ketone (rac-1) shown in a formula rac-1. The methodcomprises the following steps: by taking L-di-p-methyl benzoyl tartrate or a hydrate thereof as a resolving agent, resolving in a mixed solvent system, thus obtaining a compound of (S)-1 and L-di-p-methyl benzoyl tartrate; enabling the compound to be free in water or alcoholic solution to obtain (S)-1, and classifying absolute configuration of a sample by comparing theoretic electronic circular dichroism with the practical electronic circular dichroism; and by virtue of the same steps, taking D-di-p-methyl benzoyl tartrate or a hydrate thereof as the resolving agent, and obtaining (R)-1. Themethod provided by the invention is simple to operate and high in resolution efficiency, the resolving agent is easy to recycle, and environmental pollution is low, so that the method is applicable tolarge-scale preparation and industrial production. (The formula rac-1 is described in the specification).