171results about "Steroids preparation" patented technology

The invention relates to the field of ginsenoside extraction, in particular to a device and method for removing a plasticizer in a ginsenoside extract, and the device comprises a roll-over stand, a removal cabin and the like. According to the equipment and the method for removing the plasticizer in the ginsenoside extract, the filtering assembly and the adsorption resin blocks are distributed in the removal cabin in the vertical direction, so that fine filtering treatment and adsorption removal treatment of a ginsenoside extract solution are completed in sequence; and in addition, the filter assembly and the plurality of adsorption resin blocks can be subjected to backwashing treatment in a mutually separated state, so that the overall treatment process steps of the backwashing treatment work are reduced on the basis of ensuring that efficient backwashing treatment is synchronously performed on the filter assembly and all the adsorption resin blocks. The defects that multiple treatment devices need to be used in multiple filtering treatment and ion adsorption treatment processes of the ginsenoside extract solution, the plasticizer removal treatment efficiency is affected, and the plasticizer removal treatment period is delayed are overcome.

The invention discloses a preparation method and application of a novel bird nest alkane diterpenoid compound, and relates to the technical field of medicinal chemistry. The invention aims to solve the problems that chemical synthesis needs harsh conditions and the cost is difficult to control when diterpenoid compounds are obtained in the prior art, and a large amount of resources are wasted and new molecules are difficult to obtain under conventional fermentation conditions. The prepared bird nest alkane type diterpene has dual functions of promoting neurite growth and nourishing neurons, is expected to be developed into a neuroprotective agent, and is used for treating neurodegenerative diseases and peripheral nerve injury diseases; meanwhile, the problems that in the prior art, when the compounds are obtained, conditions needed by chemical synthesis are harsh, the cost is difficult to control, a large number of resources are wasted under conventional fermentation conditions, but new molecules are difficult to obtain, and production and smooth follow-up biological activity research are not facilitated are effectively solved. The invention provides the preparation method and the application of the novel bird nest alkane diterpenoid compound.

The invention discloses a method for extracting bilirubin, cholic acid and chenodeoxycholic acid from chicken bile. The method comprises the steps of pretreatment, chicken bile treatment, hydrolysis reduction, chromatographic separation and the like. The method comprises the following steps: slicing frozen chicken gallbladder, heating, unfreezing and melting to denature protein into solid, then cooling, performing three-phase centrifugal degreasing and deproteinization, and adding three enzymes including biliverdin reductase, coenzyme I and glucose dehydrogenase to reduce free biliverdin and combined biliverdin, so as to obtain the biliverdin-free biliverdin-glucose dehydrogenase-free biliverdin-glucose dehydrogenase-free biliverdin-glucose dehydrogenase. The method comprises the following steps: adding cholic acid and chenodeoxycholic acid into a container, adding gluconic acid hydrolase and bile salt hydrolase to hydrolyze biliverdin and bile acid, adding trypsin to hydrolyze impure protein, performing chromatography by using macroporous silica gel, and separating bilirubin, cholic acid and chenodeoxycholic acid by using different molecular space structures to obtain high-purity bilirubin, cholic acid and chenodeoxycholic acid. The method has the advantages of simple process, few types of used solvents, low toxicity, and facilitation of environmental protection and industrial production.

The invention belongs to the technical field of medicines, and particularly relates to a triterpenoid extracted from edible and medicinal fungus ganoderma lucidum, a preparation method of the triterpenoid and application of the triterpenoid in the aspect of resisting Alzheimer's disease. The triterpenoid compound is shown as a structural formula I. The triterpenoid compound provided by the invention has remarkable acetylcholin esterase inhibitory activity, is an ideal candidate compound of an acetylcholin esterase inhibitor which is novel in structure and efficient in activity, and has a good application prospect in the aspect of treatment of Alzheimer's disease. # imgabs0 #

The present invention relates to a process for preparing B-[(7α,17β)-17-hydroxy-7-[9-[(4,4,5,5,5-pentafluoropentyl)sulfinyl]nonyl]estra-1,3,5(10)-trien-3-yl]-boronic acid, also known as Fulvestrant-3-boronic acid or ZB716, whose structure is reported below.

The invention discloses a method for increasing the content of diammonium glycyrrhizinate, and aims to solve the problems of low solubility, unstable crystallization and easy degradation in the existing purification process. The method comprises the following steps: adding a diammonium glycyrrhizinate crude product and hydroxypropyl-beta-cyclodextrin into purified water at normal temperature to prepare a homogeneous solution; adding stronger ammonia water to obtain ammoniated liquid; raising the temperature to 35-40 DEG C at the speed of 1-2 DEG C / min and Adding 90% ethanol and maltitol to prepare a stable crystallization solution; dropwise adding glacial acetic acid to adjust the pH value to 4-5, standing and crystallizing for 12-14 hours, filtering, leaching with purified water at 40-45 DEG C, and performing vacuum freeze drying to obtain a finished product. According to the method, the hydroxypropyl-beta-cyclodextrin is used for solubilization, the maltitol is used for stable crystallization, the process is mild and free of degradation, the purity of the finished product is high, no solvent is left, and the method is suitable for industrial production of pharmaceutical-grade diammonium glycyrrhizinate.

The invention belongs to the field of traditional Chinese medicine chemistry and natural product separation, and particularly relates to extraction and separation of a novel triterpenoid compound 25-Etherxy-dammar-20 (22) Z-ene-3beta, 6alpha, 12beta-triol and application of the novel triterpenoid compound 25-Etherxy-dammar-20 (22) Z-ene-3beta, 6alpha, 12beta-triol in myocardial protection drugs. The compound is named as 25-Etherxy-dammar-20 (22) Z-ene-3beta, 6alpha, 12beta-triol, and the structural formula of the compound is shown in the description. The invention provides an extraction and separation method of the compound. The extraction and separation method mainly comprises the following steps: sequentially carrying out solvent extraction, macroporous adsorption resin enrichment, silica gel column chromatography, ODS medium-pressure column chromatography, high performance liquid chromatography separation and purification and the like on ginseng and other traditional Chinese medicine processed products and hydrolysates. The structure of the compound is determined through comprehensive analysis of a high-resolution mass spectrum (HRMS), one-dimensional nuclear magnetic resonance (1H NMR, 13C NMR) and a two-dimensional nuclear magnetic resonance spectrum (such as HSQC, HMBC, ROESY and the like), and the compound is a newly discovered dammarane type triterpene compound. Experiments show that the compound and the composition thereof have a remarkable protection effect on myocardial cell hypoxia / reoxygenation reperfusion injury, and can be used for preparing drugs for preventing or treating myocardial ischemia reperfusion injury and other related diseases.

The invention relates to the technical field of cholesterol preparation, and discloses a preparation method of plant-derived cholesterol, which comprises the following steps: 1) heating and dissolving phytosterol with n-amyl alcohol, adding stigmasterol until saturation, cooling and crystallizing, and then carrying out solid-liquid separation to obtain a stigmasterol crude product; 2) heating and dissolving the stigmasterol crude product with absolute ethyl alcohol, adding pyridine, and continuously dropwise adding acetic anhydride for reaction; after the reaction is completed, adding deionized water for mixing, extracting with n-hexane for multiple times, separating an upper-layer oil phase, and concentrating and drying the oil phase to obtain a white solid; 3, the white solid is subjected to oxidation reduction, witting reaction and hydrogenation reaction, and cholesterol is obtained.The method has the advantages that compared with the prior art that the plant source cholesterol is directly prepared from the raw material phytosterol, the process is simplified, and meanwhile the product yield can be increased.

The present invention provides a process for Pd(II) -catalyzed site selective β- and γ-C(sp3)-H arylation of primary aldehydes controlled by transient directing groups.

The invention belongs to the technical field of biological medicines, and provides a method for synthesizing testosterone 17-O-beta-D-glucosyl-(1-> 4)-6 ''-O-acetyl-beta-D-glucoside through two-step enzymatic coupling. Mainly relates to an intermediate compound testosterone 17-O-beta-D-glucosyl-(1-> 4)-beta-D-glucoside for synthesizing the molecule, mutant amino acid and nucleotide sequences of glycosyl transferase OsSGT2 for synthesizing the intermediate, and synthesis application. In addition, the invention also provides an application of the testosterone 17-O-beta-D-glucosyl-(1-> 4)-6 ''-O-acetyl-beta-D-glucoside in liver protection.

The group of inventions relates to the field of medicine, pharmacology and the chemical and pharmaceutical industry and includes an improved method for producing (10S, 13S, 16R, 17R)-17-hydroxy-10,13,16-trimethyl-17-propanoyl-7,8,12,14,15,16-hexahydro-6H-cyclopenta[a]phenanthrene-3-one (compound of formula (I)) and the use thereof for industrial batch, semi-continuous and continuous chemical production. Also described is a method for producing an intermediate compound, Vamorolone Acetate. The method for producing the compound of formula (I) is carried out according to the schema depicted. The production method makes it possible to produce the compound of formula (I) with a purity suitable for the use thereof in a finished dosage form for subjects requiring treatment for Duchenne muscular dystrophy. Thus, the technical results of the present invention consist in an improved production method which results in: a high yield and chemical purity, including stereoisomeric purity, of the compound of formula (I) and intermediate products in the synthesis of the compound of formula (I), which are suitable for use in a finished dosage form for subjects requiring treatment for Duchenne muscular dystrophy; the adaptability of the synthesis of the compound of formula (I) to industrial production; environmentally-friendly production; and a decrease in the formation of undesirable by-products.

The invention discloses a marsdenia tenacissima extract as well as a preparation method and application thereof, and belongs to the technical field of medicines. The marsdenia tenacissima extract is Marsdenside A or Marsdenside C, and the structural formulas of the marsdenside A and the Marsdenside C are respectively shown as a formula I and a formula II. Marsdenside C can induce ferroptosis and inhibit liver cancer, and the liver cancer is liver cancer caused by HepG2 or Huh7 cells; the Marsdenside A induces pyroptosis to play a role in inhibiting the gastric cancer, and the gastric cancer is caused by HGC-27 or AGS cells, so that the Marsdenside C can be used for preparing the medicine for resisting the liver cancer, and the Marsdenside A can be used for preparing the medicine for resisting the gastric cancer.

The invention belongs to the technical field of medicines, and discloses an arbutin amino acid derivative as well as a preparation method and application thereof. According to the invention, a microbial conversion technology is utilized, the arbutin is taken as a substrate, pyroglutamic acid is introduced to the 28 site of the arbutin in a regioselective manner, and the arbutin-28beta-pyroglutamate with a novel structure is obtained. An in-vitro anti-tumor cell test proves that the compound has remarkable anti-tumor activity and can be used as an active component of an anti-tumor drug. A mouse in-vivo experiment proves that the compound has a remarkable anti-osteoporosis effect, can be used as an active ingredient of an anti-osteoporosis medicine, and has wide application.

The invention provides maslinic acid PROTACs as well as a preparation method and application thereof, and belongs to the technical field of drug development. According to the invention, maslinic acid is taken as a POI ligand, lenalidomide and fluoro-thalidomide are taken as E3 ligands, and linker selects a PEG chain or an aliphatic chain, so that the anti-cancer activity of the compound is superior to that of maslinic acid, and the compound has a good potential application prospect in the aspect of anti-tumor treatment.

The invention discloses a synthetic method of a high-grade intermediate of didrogesterone. The synthetic route of the invention is as shown in the specification, and more specifically, a compound 1 (9-hydroxyandrostenedione) is used as an initial raw material, a strategy of aromatization and dearomatization is adopted, and the synthetic route of bromination, A-ring aromatization, silicon-based protection of phenolic hydroxyl, carbonyl reduction, sulfonylation or halogenation of hydroxyl, deprotection of phenolic hydroxyl and dearomatization cyclization is adopted, so that the compound 1 (9-hydroxyandrostenedione) is obtained. According to the present invention, the non-natural steroid skeleton of the type of the didrogesterone can be obtained from the cheap 9-hydroxyandrostenedione, the high-grade intermediate (compound 8) of the didrogesterone can be efficiently and massively synthesized, and the sufficient raw material is provided for the further synthesis of the didrogesterone or the analogue thereof. # imgabs0 #

The present invention relates to the technical field of pharmaceutics, and in particular to a triptolide lignocerate, a liposome thereof and a preparation method therefor. The chemical structural formula of the triptolide lignocerate is represented by formula (I). The triptolide lignocerate provided by the present invention is obtained by esterification of triptolide C14-OH and lignoceric acid. The anti-tumor effectiveness, safety and the like of the triptolide lignocerate liposome are further improved with respect to the prior art, so that a foundation is laid for providing safer and more effective triptolide-related clinical preparations.

The invention provides a method for catalytically synthesizing 7-amino-3-oxabicyclo [3.3. 1] nonyl-6-ene-1-ol by using rare earth, which comprises the following steps of: adding a catalyst and a catalyst, according to the preparation method, rare earth trifluoromethanesulfonate is taken as a catalyst, 6-alkoxy-2, 6-dihydropyran-3-ketone and enamine compounds are taken as raw materials, and the 7-amino-3-oxabicyclo [3.3. 1] nonyl-6-ene-1-ol is prepared by catalyzing (3 + 3) cyclization reaction. The synthesis method provided by the invention is simple in reaction raw material synthesis, low in rare earth salt price, easy in experimental operation and suitable for large-scale preparation. The obtained compound can be applied to the fields of organic synthesis, drug synthesis, organic materials and the like.

The invention relates to a synthetic method of didrogesterone. According to the method, progesterone is subjected to ketalation, halogenation, elimination, illumination isomerization, deprotection and final isomerization, and the didrogesterone is obtained. The method has the advantages of high yield, cheap and easily available raw materials, green and safe whole process route, high bulk drug quality and purity of 99.8% or more, and is suitable for industrial production.

The present invention provides a process for Pd(II)-catalyzed site selective β- and γC(sp3)-II arylation of primary aldehydes controlled by transient directing groups.

The application relates to the technical field of organic synthesis, and particularly discloses a synthesis process of high-purity pregnenolone, which comprises the following steps: S1, esterification reaction of progesterone and an acylation reagent to obtain product 1; S2, ketalization reaction of the product 1, diol and a dehydrating agent in the presence of a catalyst to obtain product 2; S3, reduction reaction of the product 2 and a reducing agent to obtain product 3; and hydrolysis reaction of the product 3 and an acidic compound to obtain pregnenolone. The synthesized pregnenolone has high purity and yield.

The invention discloses a synthesis method of 8, 9-dehydroestrone. The invention discloses a preparation method of 8, 9-dehydroestrone, which comprises the following steps: (1) in the presence of an acid catalyst, in an aprotic solvent, carrying out a deprotecting group-isomerization reaction on a compound 5 to obtain a compound 6; and (2) in the presence of a catalyst, in an aprotic solvent, carrying out an addition reaction on the compound 6 and a hydrogen source reagent to obtain the 8, 9-dehydroestrone. The method has one or more advantages as follows: raw materials are cheap, reaction steps are simple, the reaction yield of each step is high, post-treatment is simple and convenient, conditions are mild, operation is controllable, and the method is suitable for amplification.

The invention provides a method for catalytically synthesizing 7-oxa-2-azabicyclo [3.3. 1] nonyl-3-ene-1-ol by using rare earth, which comprises the following steps of: adding a catalyst and a catalyst, according to the preparation method of the 7-oxa-2-azabicyclo [3.3. 1] nonyl-3-ene-1-ol, rare earth trifluoromethanesulfonate is taken as a catalyst, 6-alkoxy-2, 6-dihydropyran-3-ketone and enamine compounds are taken as raw materials, and the preparation of the 7-oxa-2-azabicyclo [3.3. 1] nonyl-3-ene-1-ol is realized. The method is simple in reaction raw material synthesis, simple in experimental operation and suitable for large-scale preparation. The obtained compound can be applied to the fields of organic synthesis, drug synthesis and the like.

The invention discloses a pentacyclic triterpene acylhydrazone compound as well as a preparation method and application thereof. A series of oleanolic acid derivatives are synthesized by carrying out structural modification on carboxyl at C28 site of oleanolic acid, structural confirmation is carried out by using 1H NMR, 13C NMR, HRMS and X-ray single crystal diffraction, and the inhibition effect of the pentacyclic triterpenoid acylhydrazone compound on the activity of tumor cells A549, AGS and K562 is evaluated by taking cis-platinum as positive control and adopting a CCK-8 method. Results show that the inhibition effect of the derivatives 5, 6, 9, 10, 16, 21, 27 and 28 on tumor cells is superior to that of cis-platinum. Reference is provided for research of oleanolic acid derivatives and discovery of anti-tumor seedling compounds.

The invention relates to the technical field of pharmaceutical chemicals, in particular to a refining method of an eplerenone intermediate. The method comprises the following steps: S1, dissolving: sequentially adding an eplerenone methyl ester crude product, an organic solvent and water into a reaction bottle, and stirring and heating to completely dissolve the eplerenone methyl ester crude product, the organic solvent and the water; s2, reaction: adding inorganic alkali into a dissolved reaction system, and stirring for full reaction at controlled temperature; s3, elutriation: cooling the system to room temperature, and slowly dropwise adding water to precipitate a solid product; s4, devitrification: cooling, devitrifying and fully stirring; s5, filtering and drying: filtering the system for solid-liquid separation, and drying to obtain an eplerenone methyl ester fine product. The eplerenone methyl ester refining method provided by the invention is high in product yield and low in cost, the adopted organic solvent is a common solvent and is low in toxicity, and the eplerenone methyl ester refining method has good industrial application value and is very suitable for large-scale industrial application.

The invention discloses an extraction method of 5 alpha-carp cholesteryl sulfate, and belongs to the technical field of extraction and purification of bile acid active substances. The extraction method of 5 alpha-carp cholesteryl sulfate comprises the following steps: (1) carrying out freeze drying or rotary evaporation concentration on fresh fish bile to obtain a crude product; (2) mixing and dissolving the crude product obtained in the step (1) with hot methanol at 50-80 DEG C according to a mass ratio of the crude product to the methanol of 1: (5-10), carrying out suction filtration while the crude product is hot, and collecting filtrate; and (3) ethyl acetate is added into the filtrate obtained in the step (2), the mass ratio of the methyl alcohol to the ethyl acetate is 1: (1-2), standing is conducted, a solid is separated out, and the obtained solid is the 5 alpha-carp cholesteryl sulfate. The extraction method disclosed by the invention is simple and convenient, high in yield, high in product quality and low in cost.

The invention relates to a bufalin derivative as well as a preparation method and application thereof, and belongs to the technical field of medicines. According to the invention, TEMPO oxidation reaction is adopted to selectively oxidize 19-site primary alcohol in 19-OH bufalin into aldehyde, so that 19-CHO bufalin is successfully synthesized, namely the bufalin derivative is obtained. The bufalin derivative has a remarkable killing effect on pancreatic cancer BxPC-3 cells, liver cancer HepG2 cells and brain glioma U-87MG cells, the IC50 of the bufalin derivative to the BxPC-3 cells is 40.63 nM, the IC50 of the bufalin derivative to the HepG2 cells is 36.74 nM, the IC50 of the bufalin derivative to the U-87MG cells is 28.73 nM, and the IC50 of the bufalin derivative to CHO-K1 cells is larger than 30 [mu] M, so that the bufalin derivative is relatively weak in toxicity to the heart, and the bufalin derivative has a remarkable killing effect on the liver cancer BxPC-3 cells, the liver cancer HepG2 cells and the brain glioma U-87MG cells. The compound can be applied to medicines for resisting pancreatic cancer, liver cancer and brain glioma.

The present invention relates to a compound for the prevention and / or treatment of neurodegenerative diseases. On one hand, the compound provided by the invention can effectively promote the proliferation of neuronal cells, and on the other hand, the compound has a protection effect on neuronal cell toxicity induced by neurotransmitters such as glutamic acid caused by excessive accumulation of Abeta amyloid protein, so that the effect of treating neurodegenerative diseases is comprehensively exerted; meanwhile, the compound disclosed by the invention has no obvious cytotoxicity. Therefore, the compound has a good application prospect in medicines for preventing or treating neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease, Huntington's disease and the like. Besides, a parent structure with a key active function on the neurodegenerative disease and an important influencing group in the cynanchum otophyllum extract are defined, the basic structure-function relationship between the compound and the treatment of the neurodegenerative disease is defined, and a sufficient scientific basis is provided for research and development of subsequent related drugs.

The invention relates to the technical field of haptens, in particular to a steroid derivative and a preparation method thereof, and a complete antigen derivative and a preparation method thereof. The steroid derivative comprises a steroid substance, a coupling group capable of carrying out a coupling reaction, a zwitterionic group and a linking group, the steroid substance and the zwitterionic group are bonded to the two sides of the linking group respectively, and the zwitterionic group is linked with the coupling group. According to the steroid derivative, isomeric impurities are reduced, so that the antigen homogeneity is better, the performance is more stable, meanwhile, the steroid derivative is good in hydrophilicity, precipitates are not prone to being generated in the subsequent coupling process, and the detection sensitivity and accuracy are improved.