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51 results about "Spirolactone" patented technology
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Spirolactones are a class of functional group in organic chemistry featuring a cyclic ester attached spiro to another ring system. The name is also used to refer to a class of synthetic steroids, called steroid-17α-spirolactones, 17α-spirolactosteroids, or simply 17α-spirolactones, which feature their spirolactone group at the C17α position. They are antimineralocorticoids, or antagonists of the mineralocorticoid receptor (which is activated predominantly by the mineralocorticoid steroid hormone aldosterone), and have been employed clinically as potassium-sparing diuretics. Some also possess progestogenic and/or antiandrogen properties, which have both contributed to side effects and been utilized for medical indications (e.g., spironolactone as an antiandrogen, and drospirenone as a progestin). The spirolactones were developed by G. D. Searle & Company in the 1950s and thereafter and were denoted as "SC" compounds (e.g., SC-9420 for spironolactone).
Application of thiospirolactone in intracellular hypochloric acid detection
InactiveCN101870864AHigh sensitivityImprove permeabilityOrganic chemistryFluorescence/phosphorescenceFluorescenceCytotoxicity
The invention relates to a fluorescence detection method and provides a fluorescent probe which has high sensitivity and high selectivity and is used for detecting intracellular hypochloric acid and an application of thiospirolactone in intracellular hypochloric acid detection. The structure of the fluorescent probe for detecting the intracellular hypochloric acid is a triphenylmethane fluorescent probe with a Xanthone ring parent structure; and the fluorescent probes of the thiospirolactone all adopt corresponding spirolactones as raw materials. The thiospirolactone has high-sensitivity fluorescent response characteristics on hypochloric acid, and when being used in the fluorescent probe for detecting the intracellular hypochloric acid, the selectivity is high. The probe has strong lightstability, no illumination self oxidation, rapid response to an aimed compound, good cell permeability and no strong cytotoxicity, and a product formed by combining the fluorescent probe and the aimed compound has strong photobleaching resistance. The thiospirolactone used for detecting the hypochloric acid of the aimed compound has high sensitivity and strong specificity and other active oxygen in cells has no interference on the detection.
Owner:XIAMEN UNIV
Preparation method of near-infrared emission xanthene fluorescent dye with large Stokes shift
The invention discloses a preparation method and application of near-infrared emission xanthene fluorescent dye with large Stokes shift. The preparation method has the advantages that xanthene fluorescent dye with maximum absorption wavelength exceeding 600 nm, maximum fluorescent emission wavelength exceeding 730 nm and Stokes shift exceeding 100 nm is designed and synthesized through a strategy of prolonging a xanthene conjugated system linearly, and the xanthene fluorescent dye is one of the fluorescent dyes with largest Stokes shift in the existing known rhodamine fluorescent dyes. According to a cell imaging experiment, the dye has good water solubility, biocompatibility, small biotoxicity and is used for positioning lysosome in a targeted mode. Besides, the dye structurally contains a spirolactone structure, and can be used as a near-infrared emission dye fluorescence reporter group to design various near-infrared emission fluorescence opening type biological fluorescent probes. In a word, the invention provides a design and synthesis method for the novel near-infrared emission xanthene fluorescent dye with large Stokes shift, and the novel near-infrared emission xanthene fluorescent dye is used for novel fluorescence probe design and development.
Owner:TIANJIN UNIVERSITY OF TECHNOLOGY
Pharmaceutical composition for treating polycystic ovary syndrome (PCOS)
InactiveCN102302668ADecreased androgen levelsIncrease ovulation rateHeavy metal active ingredientsOrganic active ingredientsIn vivoPolycystic ovary
The invention provides a pharmaceutical composition for treating polycystic ovary syndrome (PCOS). The pharmaceutical composition consists of a traditional Chinese medicine composition and chemical drugs, wherein the traditional Chinese medicine composition comprises the medicinal materials such as anemarrhena, fritillary bulb, tortoise plastron, fleece-flower root, lilyturf root, hippocampus andthe like; and the chemical drugs comprise one or more compound molecules of dexamethasone, spirolactone, ethinyloestradiol, estradiol valerate, conjugated estrogen and pharmaceutically acceptable salt. The pharmaceutical composition has the advantages of reducing the level of androgens and androgen receptors of patients suffering from PCOS, improving the level of sex hormone-binding globulin (SHBG), lowering the level of free testosterone (F-TESTO), further raising the level of in-vivo estrogens, improving growth and development of follicles and increasing ovulation rate and pregnancy rate ofthe patients.
Owner:上海泰坤堂中医医院有限公司
Rhodol derivative dye and application thereof
ActiveCN110423487AFine tuning of protonation constantExcellent photophysical propertiesStyryl dyesMethine/polymethine dyesQuantum yieldExtinction
The invention relates to a Rhodol derivative dye and a photoacoustic imaging PA (polyamide) probe and in particular to preparation and application of the Rhodol derivative dye and the photoacoustic imaging PA probe. A novel Rhodol derivative dye Rhodol-NIR is designed and synthesized, has novel Rhodol-NIR chromophore which has a large mole extinction coefficient, excellent photostability and an ideal quantum yield, and has excellent optical physical properties when a high-contrast activated PA probe. Tests prove that the Rhodol-PA probe designed and synthesized by the invention has high sensitivity and high selective detection on hNQO1 in in-vitro PA absorption and fluorescent measurement. By adopting the Rhodol derivative dye, the high-contrast activated PA probe is developed through a spirolactone open-loop conversion policy in China for a first time. The related policy of the invention is a generally applicable design, and a new platform can be provided for developing the high-contrast activated PA probe.
Owner:HUNAN UNIV
Spirolactone composition freeze-dried tablets and preparation method thereof
InactiveCN104490750AReduce typesReduce dosageOrganic active ingredientsPharmaceutical delivery mechanismSucroseMedicine
The invention provides spirolactone composition freeze-dried tablets and a preparation method thereof, and relates to the technical field of medicine and medicine production. The spirolactone composition freeze-dried tablets comprise spirolactone, starch and sucrose; the starch and sucrose are used as accessories, common corn starch is processed by a heating process, the bonding and disintegration effects of the starch in the tablets can be improved, the formability of the tablets is increased, and only two accessories, namely starch and sucrose, are needed in the spirolactone composition freeze-dried tablets. A freeze-drying process of two-time reduction and two-time increase is adopted for the spirolactone composition freeze-dried tablets, the formability of the tablets is better through two-time reduction and two-time increase of temperature, and the dissolubility of the tablets is improved so as to improve the bioavailability of the tablets; the tablets overcome the shortcomings of common spirolactone tablets, and the types and amount of accessories in the spirolactone tablets are reduced; and moreover, the dissolubility and bioavailability of the tablets are high, and the curative effect and safety of clinical medication are guaranteed.
Owner:HAINAN WEI KANG PHARMA QIANSHAN
Para-quinol derivatives and methods of stereo selectively synthesizing and using same
This application relates to para-quinol derivatives, such as analogues of manumycins, aranorosins and gymnastatins. This application also relates to methods of synthesizing and using the para-quinol derivatives. In one embodiment of the invention a compound having the chemical structure (I) is provided wherein X1 and X2 are carbon atoms either joined by double bond or joined by a single bond and comprising constituents of an epoxide ring or a hydroxyethylene moiety; X3 and X4 are carbon atoms either joined by double bond or joined by a single bond and comprising constituents of an epoxide ring; R1 is selected from the group consisting of branched alkyl chains, unbranched alkyl chains, cycloalkyl groups, aromatic groups, alcohols, ethers, amines, and substituted or unsubstituted ureas, esters, aldehydes and carboxylic acids; and R2 is selected from the group consisting of H, OH and NHR3 wherein R3 is a nitrogen protecting group. In a particular embodiment of the invention R1 is a polyunsaturated carbon chain as found in biologically active manumycins. The applicant's synthetic method may involve diasteroselective formation of a spirolactone in an oxidative spiroannulation process using tyrosine or a tyrosine derivative having a chiral centre as a starting material.
Owner:UNIVERSITY OF NORTHERN BRITISH COLUMBIA
Diabetes treating compound medicine for reducing side effect of rosiglitazone and preparation method thereof
The invention discloses a diabetes treating compound medicine for reducing side effect of rosiglitazone and a preparation method thereof, and belongs to the field of medicine preparation. The compound medicine consists of rosiglitazone and a diuretic medicine, wherein the ratio of rosiglitazone to the diuretic medicine by weight is 1:(0.04-1). The diabetes treating compound medicine is compounded and matched with any one of spirolactone, amiloride, compound amiloride, ergosterol, triamterene, ethacrynic acid, hydroflumethiazide and bumetanide which can better eliminate side effect of rosiglitazone with rosiglitazone so as to form the compound medicine which not only can reduce the side effect of rosiglitazone, but also better treats diabetes.
Owner:罗国安
Antihypertensive medicine synergist
InactiveCN103565813AImprove complianceLower doseOrganic active ingredientsCardiovascular disorderHypertension medicationsPatient compliance
Owner:刘超
Compound spirolactone nanoemulsion drug
InactiveCN102697900AEvenly distributedSystem transparencyOrganic active ingredientsEmulsion deliveryActive agentSurface-active agents
The invention discloses a compound spirolactone nanoemulsion drug. The nano drug is prepared from the following materials in mass percentage: 1%-15% of spirolactone, 15%-35% of surfactant, 5%-20% of cosurfactant, 5%-20% of oil, 0.5%-10% of hawthorn extract, 0.5%-10% of asarum extract and the balance of distilled water, wherein the sum of the mass percentages of the ingredients is 100%. According to the invention, after the spirolactone is prepared into nanoemulsion dosage form, the ability of penetrating blood brain barrier is obviously increased, the bioavailability of active compound is obviously improved, the half-life period of the drug is prolonged, and the administration times are reduced. The dissolving and penetrating abilities of the drug of the spirolactone are improved by the nanoemulsion, and the stability of the spirolactone is increased. The spirolactone nanoemulsion drug has obvious synergistic effect after being combined with aqueous extract of the hawthorn and asarum, and the curative effect of the drug is brought into full play.
Owner:NORTHWEST A & F UNIV
Process for making spirolactone compounds
This invention relates to a process for making spirolactone compounds of general formula I, having an improved IA / IB ratio, according to the following shceme.
Owner:VOLANTE RALPHP +7
Lacidipine-spirolactone co-amorphous solid dispersion and preparation thereof
ActiveCN109010348AImprove in vitro dissolutionImprove stabilityPowder deliveryOrganic active ingredientsSolventSpirolactone
The invention belongs to the technical field of medicines and in particular relates to lacidipine-spirolactone co-amorphous solid dispersion and a preparation method thereof. According to the preparation method, lacidipine and spirolactone, which have a cooperative blood pressure lowering effect, are carriers for each other, and the co-amorphous solid dispersion is prepared by adopting a solvent volatilization method. The co-amorphous solid dispersion is formed by combining the lacidipine and the spirolactone according to the mol ratio of 1 to (1 to 9); Cu-Kalpha radiation is utilized, and a powder X-ray diffraction spectrum shown as a 2theta angle does not have a sharp diffraction peak; peak positions and peak strength of the co-amorphous solid dispersion are obviously changed in a Fourier infrared spectrum. Compared with a lacidipine crystal and a spirolactone crystal, the co-amorphous solid dispersion has the advantages that the dissolution rates and dissolvability of the lacidipineand the spirolactone are remarkably improved. The preparation method of the solid dispersion is simple and feasible and has good repeatability; amplified production is easy to carry out and industrial transformation is carried out; the preparation method has a good clinical application prospect.
Owner:SHENYANG PHARMA UNIVERSITY
Cleansing cream for preventing and curing acnes and preparation process thereof
InactiveCN102451151AGood effect in removing acneGood curative effectCosmetic preparationsToilet preparationsAdditive ingredientBULK ACTIVE INGREDIENT
The invention relates to a cleansing cream for preventing and curing acnes, comprising plant extracts, thiamphenicol, spirolactone, hydracrylic acid, lecithin, deionized water, pearl powder and 75% of ethanol; the product is obtained by mixing the components; the cleansing cream has better anti-acne effect; at least 95% of effective ingredients can be absorbed; the active ingredients can be delivered to dried and damaged part of skin in a prioritizing manner; the curative effect is improved; the preparation process is simple and does not need any special device; and the cream can be prepared by the production line for common cosmetics.
Owner:黄卫忠
A preparation method of near-infrared emitting xanthene fluorescent dye with large Stokes shift
The invention discloses a preparation method and application of near-infrared emission xanthene fluorescent dye with large Stokes shift. The preparation method has the advantages that xanthene fluorescent dye with maximum absorption wavelength exceeding 600 nm, maximum fluorescent emission wavelength exceeding 730 nm and Stokes shift exceeding 100 nm is designed and synthesized through a strategy of prolonging a xanthene conjugated system linearly, and the xanthene fluorescent dye is one of the fluorescent dyes with largest Stokes shift in the existing known rhodamine fluorescent dyes. According to a cell imaging experiment, the dye has good water solubility, biocompatibility, small biotoxicity and is used for positioning lysosome in a targeted mode. Besides, the dye structurally contains a spirolactone structure, and can be used as a near-infrared emission dye fluorescence reporter group to design various near-infrared emission fluorescence opening type biological fluorescent probes. In a word, the invention provides a design and synthesis method for the novel near-infrared emission xanthene fluorescent dye with large Stokes shift, and the novel near-infrared emission xanthene fluorescent dye is used for novel fluorescence probe design and development.
Owner:TIANJIN UNIVERSITY OF TECHNOLOGY
Process for obtaining 17-spirolactones in steriods
The invention relates to processes for obtaining steroids with a spirolactone group in position 17, particularly to industrially obtaining 6β,7β; 15β,16β-dimethylene-3-oxo-17α-pregn-4-ene-21,17-carbolactone, commonly known as Drospirenone, as well as to intermediates useful in said process.
Owner:CRYSTAL PHARMA SA
Cell permeable, fluorescent dye
ActiveUS9346957B2Silicon organic compoundsPyronine/xanthon/thioxanthon/selenoxanthan/telluroxanthan dyesQuantum yieldHydrogen
Owner:ECOLE POLYTECHNIQUE FEDERALE DE LAUSANNE (EPFL)
Compound antihypertensive drug combination preparation containing furosemide and spirolactone and preparation method of compound antihypertensive drug combination preparation
InactiveCN105687210AIncrease dissolution rateSmall particle sizeOrganic active ingredientsPharmaceutical non-active ingredientsAntihypertensive drugLubricant
The invention discloses a compound antihypertensive drug combination preparation containing furosemide and spirolactone and a preparation method of the compound antihypertensive drug combination preparation. The compound antihypertensive drug combination preparation comprises a tablet core and a coating, wherein the tablet core is prepared from the following components counted according to the total weight of the table core: 10 to 40 percent of furosemide, 20 to 50 percent of spirolactone, 2 to 4 percent of solubilizer, 10 to 60 percent of filling agent, 4 to 8 percent of disintegrating agent, 0.5 to 1 percent of lubricating agent and 0.1 to 2 percent of binding agent.
Owner:KANGYA OF NINGXIA PHARMA
Hybridoma cell strain for secreting spirolactone and metabolite monoclonal antibody thereof and application of hybridoma cell strain
ActiveCN114181911AEfficient and stable secretionRealize detectionTissue cultureImmunoglobulinsMicroorganismMetabolite
The invention relates to a hybridoma cell strain secreting spirolactone and metabolite monoclonal antibodies thereof, the hybridoma cell strain is named as a monoclonal cell strain PRM, and the hybridoma cell strain is preserved in China General Microbiological Culture Collection Center on May 13, 2021, the preservation address is No.3, Yard 1, Beichen West Road, Chaoyang District, Beijing, and the preservation number is CGMCC No.22341. The hybridoma cell strain disclosed by the invention can efficiently and stably secrete the monoclonal antibody of the spirolactone and the metabolite of the spirolactone, provides a powerful detection method and means for detecting the residual quantity of the spirolactone and the metabolite of the spirolactone in animal-derived food and cosmetics, and has relatively good sensitivity and specificity.
Owner:JIANGNAN UNIV
Acne treatment, itching relieving liniment and preparation method thereof
InactiveCN103301320ATo promote metabolismGrowth inhibitionOrganic active ingredientsInorganic boron active ingredientsBolbostemma paniculatumSide effect
The invention relates to an acne treatment, itching relieving liniment which comprises the following components in parts by weight: 9-15 parts of polygonum cuspidatum, 8-12 parts of oriental wormwood, 8-12 parts of bolbostemma paniculatum, 8-12 parts of edible tulip, 8-12 parts of gentian 0.08-0.12 part of borax, 0.2-0.3 part of chloramphenicol, 0.08-0.12 part of diphenhydramine, 0.04-0.06 part of chlortrimeton, 0.12-0.18 part of promethazine and 0.16-0.24 part of spirolactone. The acne treatment, itching relieving liniment has the functions of enriching yin and nourishing kidney, promoting blood circulation to remove blood stasis, clearing heat and expelling toxicity; a plurality of traditional Chinese components supplement each other to cool blood, eliminate spots, clear internal heat, dispel wind and dissipate heat; the body internal secretion is adjusted, the in vivo hormonal balance is maintained, sebum metabolism is prompted, and bacterial growth is inhibited; the acne treatment, itching relieving liniment is remarkable in curative effect and free of toxic and side effect.
Owner:彭中平
Amorocoelophoma sp. and application thereof in preparation of spirolactone derivative
The invention belongs to the technical field of microorganisms, and relates to an Amorocoelophoma sp. and application thereof in preparation of a spirolactone derivative. The Amorocoelophoma sp. YE3351 is preserved in China center for type culture Collection on August 7, 2020, the address is Wuhan University, Wuhan City, China, the preservation number is CCTCC NO. M2020407, and the taxonomic name is Amoro-elophoma sp. According to the Amorocoelophoma sp. and the application thereof in preparation of the spirolactone derivative, the Amorocoelophoma sp. YE3351 is separated from the root bark part of Chinese catalpa in Yunnan for the first time, the spirolactone derivative is separated from the metabolite of the Amorocoelophoma sp. YE3351, and the blank of the prior art is filled.
Owner:YUNNAN UNIV
Composition of medication for treating high blood pressure
InactiveCN1695738BLower blood pressureOrganic active ingredientsCardiovascular disorderBumetanideHigh pressure
Owner:苏金平
Synthesis process of steroid compound, canrenone and spirolactone
PendingCN111892638ASynthetic conditions are mildHigh molar yieldLactone steroidsMedicineStructural formula
The invention relates to the technical field of medicine synthesis, in particular to a synthesis process of a steroid compound, canrenone and spirolactone. An embodiment of the invention provides thesteroid compound. The steroid compound has a structural formula as shown in the specification. In the structural formula, R is selected from H or an alkyl group. The steroid compound can be used for synthesizing canrenone and spirolactone, synthesis conditions are mild, synthesis efficiency is high, the amount of wastewater is small, the quality of the formed products is high, and production costcan be effectively reduced.
Owner:ZHEJIANG LANGHUA PHARMA
Tinidazole and spirolactone cream and preparation method thereof
InactiveCN104055781AImprove stabilityPromote transdermal absorptionOrganic active ingredientsAerosol deliveryStearic acidStearate
The invention discloses tinidazole and spirolactone cream and a preparation method thereof, in order to solve problems of current tinidazole and spirolactone cream, such as poor stability and moderate sensitization. According to the formula, the cream comprises tinidazole, spirolactone, laurocapram, stearic acid, albolene, sorbitol anhydride monostearate, hexadecanol, light liquid paraffin, lauryl sodium sulfate, polysorbate-80, propylene glycol, sodium benzoate and purified water. The cream disclosed by the invention can inhibit formation of acne through such links as inhibiting bacteria, diminishing inflammation and reducing sebum secretion, and has an excellent curative effect on inflammatory skin lesion and non-inflammatory skin lesion caused by acne.
Owner:南充市中心医院
Method for preparing spirolactone intermediate canrenone
ActiveCN113512086AReduce thermal degradationAvoid generatingLactone steroidsPtru catalystPyrrolidinones
The invention provides a method for preparing spirolactone intermediate canrenone. The method comprises the following operation steps: a lactone substance (I) is dissolved in an organic solvent, a catalyst and an auxiliary agent are added, and the mixture is stirred at 50-80 DEG C to prepare the canrenone (II), wherein the organic solvent is at least one of cyclohexane, toluene or methyl tetrahydrofuran; the auxiliary agent is at least one of dimethyl formamide, N,N - dimethyl acetamide and N-methyl pyrrolidone; and the catalyst is poly-4-vinylpyridine. The reaction route is shown in the specification. Compared with the prior art, the method has the advantages that the reaction temperature is low, pressurization is not needed, the quality of canrenone can be improved, the energy consumption can be effectively reduced, and the production cost can be reduced.
Owner:TIANJIN JINJIN PHARMA
Synthesis method of chiral spiro[chroman-4,1'-dihydroindene] molecule
ActiveCN109970697BEconomical large-scale preparationGood for mass manufacturingOrganic chemistry methodsPropanoic acidPtru catalyst
The invention relates to a synthesis method of chiral spiro[chroman-4,1'-dihydroindene] molecule. Using phenylpropionic acid as the starting material, react with monoethylmagnesium malonate to obtain β-ketoester, and then construct the spirolide structure through acid-catalyzed series Friedel-Crafts reaction in one pot, and then through trifluoroform The sulfonate ester activates the phenolic hydroxyl group, and finally removes the occupying atom and the sulfonate group by palladium-carbon hydrogenation to complete the synthesis of the chiral spiro[chroman-4,1'-dihydroindene] molecule. The racemate was optically resolved under the action of N-benzylhalogenated cinchonidine. The synthesis method overcomes the problems of poor atom economy, many synthetic wastes, and low practical value of the original method, and realizes simple and economical large-scale preparation of the target molecule; the separation method is green and efficient, and the separation reagent, solvent It can be used multiple times; the product molecule and synthesis method have important application value and potential in catalyst skeleton design and natural product drug synthesis.
![Synthesis method of chiral spiro[chroman-4,1'-dihydroindene] molecule](https://images-eureka.patsnap.com/patent_img/26a7905c-7291-44c1-9928-222127a967de/DEST_PATH_IMAGE002.png "Synthesis method of chiral spiro[chroman-4,1'-dihydroindene] molecule")
![Synthesis method of chiral spiro[chroman-4,1'-dihydroindene] molecule](https://images-eureka.patsnap.com/patent_img/26a7905c-7291-44c1-9928-222127a967de/BDA0002048279860000011.png "Synthesis method of chiral spiro[chroman-4,1'-dihydroindene] molecule")
![Synthesis method of chiral spiro[chroman-4,1'-dihydroindene] molecule](https://images-eureka.patsnap.com/patent_img/26a7905c-7291-44c1-9928-222127a967de/BDA0002048279860000021.png "Synthesis method of chiral spiro[chroman-4,1'-dihydroindene] molecule")
Owner:NANKAI UNIV
Combined combination drug for resisting heart failure and application of combined combination drug in preparation of drug for resisting heart failure
ActiveCN112089843AImprove the anti-heart failure effectImprove survival rateOrganic active ingredientsCardiovascular disorderAntioxidantNebivolol
The invention discloses a combined combination drug for resisting heart failure and application of a steroid aldosterone receptor antagonist and beta-cyclodextrin in preparation of a drug for resisting heart failure. The combined drug contains a diluent, an adhesive, a disintegrating agent, an antioxidant, an emulsifier, a solubilizer, the steroid aldosterone receptor antagonist and beta-cyclodextrin. According to the combined combination drug for resisting heart failure, compared with drugs such as spirolactone, beta-cyclodextrin, nebivolol and amlodipine which are independently used, the combined combination drug of the steroid aldosterone receptor antagonist and beta-cyclodextrin can significantly increase the cell survival rate, can reduce the ROS content in cells treated by adriamycin, can significantly improve the antioxidant ability of the cells, and can further greatly improve the anti-heart failure effect of the drug.
Owner:HEFEI UNIV OF TECH
Medicine for treating diastolic cardiac insufficiency and preparation method of medicine
InactiveCN105687149AImprove stabilityImprove bioavailabilityOrganic active ingredientsPill deliveryCholesterolPolyethylene glycol
The invention relates to a medicine for treating diastolic cardiac insufficiency and a preparation method of the medicine. The medicine contains metoprolol lipidosome, hydrochlorothiazide, spirolactone, filler, a disintegrating agent and a surfactant, wherein metoprolol lipidsome comprises metoprolol, cholesterol, soybean lecithin, (distearoyl-phosphatidylethanolamine)-polyethylene glycol, propylgallate and Span. The medicine has the advantages that the accumulative dissolutive degree is high, the medicine is slowly and constantly released, the biological utilization rate is high, the stability is good, the medicine has a remarkable treatment effect on diastolic cardiac insufficiency, a preparation process is simple and suitable for industrial production and the like.
Owner:QINGDAO CENT HOSPITAL
Method for preparing spirolactone by chemical-enzymatic method
ActiveCN113528607AStrong specificityIncrease catalytic rateLactone steroidsFermentationOrganic synthesisDehydrogenation
The invention discloses a method for preparing spirolactone by a chemical-enzyme method, and belongs to the technical field of organic synthesis. According to the method for preparing the spirolactone through the chemical-enzymatic method, 4AD serves as a raw material, and the spirolactone is obtained through enol etherification, epoxidation, lactonization, enzymatic dehydrogenation and sulfo-reaction. The enzymatic dehydrogenation method adopted by the spirolactone synthesis process route is good in specificity, mild in condition, free of special equipment and high in catalytic rate; the reaction product in each step involved in the method is easy to purify, the total mass yield of the final product is higher than 92%, and the HPLC purity is higher than 99.8%; the method is low in cost and suitable for industrial large-scale production, and has good economic benefits.
Owner:ZHEJIANG SHENZHOU PHARMA
Application of thiospirolactone in intracellular hypochloric acid detection
The invention relates to a fluorescence detection method and provides a fluorescent probe which has high sensitivity and high selectivity and is used for detecting intracellular hypochloric acid and an application of thiospirolactone in intracellular hypochloric acid detection. The structure of the fluorescent probe for detecting the intracellular hypochloric acid is a triphenylmethane fluorescent probe with a Xanthone ring parent structure; and the fluorescent probes of the thiospirolactone all adopt corresponding spirolactones as raw materials. The thiospirolactone has high-sensitivity fluorescent response characteristics on hypochloric acid, and when being used in the fluorescent probe for detecting the intracellular hypochloric acid, the selectivity is high. The probe has strong lightstability, no illumination self oxidation, rapid response to an aimed compound, good cell permeability and no strong cytotoxicity, and a product formed by combining the fluorescent probe and the aimed compound has strong photobleaching resistance. The thiospirolactone used for detecting the hypochloric acid of the aimed compound has high sensitivity and strong specificity and other active oxygen in cells has no interference on the detection.
Owner:XIAMEN UNIV
Process for obtaining 17-spirolactones in steroids
The invention relates to processes for obtaining steroids with a spirolactone group in position 17, particularly to industrially obtaining 6β,7β; 15β,16β-dimethylene-3-oxo-17α-pregn-4-ene-21,17-carbolactone, commonly known as Drospirenone, as well as to intermediates useful in said process.
Owner:CRYSTAL PHARMA SA
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