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38results about How to "Pharmaceutically active" patented technology
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Lactam derivative and application thereof
InactiveCN106749219APharmaceutically activeOrganic active ingredientsNervous disorderLactamChemistry
The invention relates to the field of medicines, in particular to a lactam derivative and application thereof, and more specifically relates to a lactam derivative and a pharmaceutical composition containing the same as well as application of the composition and the lactam derivative to the preparation of a drug for prevention or treatment of nervous and mental diseases. The lactam derivative has a structure shown as a formula I.
Owner:NHWA PHARMA CORPORATION
P-coumaric acid aromatic derivative and preparation method and application thereof
PendingCN110563617ARealize resource utilizationPharmaceutically activeSulfonic acid esters preparationResource utilizationP-Coumaric acid
The invention discloses a p-coumaric acid aromatic derivative and a preparation method and application thereof. The p-coumaric acid aromatic derivative of the invention has a structural formula as shown in a formula (I) which is described in the specification. In the formula (I), R is described in the specification. The p-coumaric acid aromatic derivative of the invention has potential medicinal activity; and the preparation raw material, namely p-coumaric acid, of the derivative can be obtained by using a natural extraction method, which has positive effect on resource utilization of Spartinaalterniflora Loisel.
Owner:南京施倍泰生物科技有限公司
Furan coumarin derivative and preparation method thereof
ActiveCN106279083APharmaceutically activeCondensation reaction steps are simpleOrganic chemistryFuranDrug activity
The invention relates to the field of medicines and aims to provide a furan coumarin derivative and a preparation method thereof. A furan ring of the furan coumarin derivative is substituted with a methyl; the preparation method of the furan coumarin derivative comprises the following steps: taking 4-hydroxy-3-methylbenzofuran-5-carbaldehyde and weak base, uniformly dispersing in a reaction solvent a to obtain a raw material mixture, then carrying out a reaction for 1-3 hours at a temperature of 70 DEG C, filtering reaction liquid to obtain a precipitate, and washing the precipitate to obtain the furan coumarin derivative. The furan coumarin derivative provided by the invention is an isopsoralen analogue with a novel skeleton and has potential drug activity; the preparation of the compound can provide a support for the research on the activity of a furan coumarin drug; the preparation method provided by the invention is simple in step and low in loss rate.
Owner:ZHEJIANG UNIV
4-((phenoxyalkyl)thio)-phenoxyacetic acids and analogs
The invention features 4-((phenoxyalkyl)thio)-phenoxyacetic acids and analogs, compositions containing them, and methods of using them as PPAR delta modulators to treat or inhibit the progression of, for example, dyslipidemia.
Owner:JANSSEN PHARMA NV
Aspirin-based carbon quantum dot and biological application thereof
InactiveCN104555980APharmaceutically activeHigh fluorescence quantum efficiencyOrganic active ingredientsOrganic chemistryLiver and kidneyDissolution
The invention discloses an aspirin-based carbon quantum dot and application thereof in aspects of cell imaging and anti-inflammatory treatment, belonging to the technical field of nano-drugs. The invention in particular relates to a carbon quantum dot with strong fluorescent properties prepared from a hydrazine hydrate solution by utilizing a microwave heating method under the condition that aspirin dissolution is promoted. The carbon quantum dot prepared by the method is very stable under hyper-salt concentration and physiological pH conditions, blue-fluorescence is maintained, the carbon quantum dot can enter the cell nucleus, and the cells are effectively traced; and meanwhile, the original anti-inflammatory effect of aspirin is remained, and inflammatory cells can be effectively inhibited in an acute inflammation model constructed by utilizing carrageenin. In addition, the prepared aspirin carbon quantum dot is low in toxicity and does not influence liver and kidney functions and organs such as the heart, liver, spleen and kidney in in-vivo application, and the aim that the nanometer material has dual effects of diagnosis and treatment can be achieved.
Owner:JILIN UNIV
Omarigliptin intermediate preparation method
The invention provides an omarigliptin intermediate preparation method. The omarigliptin intermediate preparation method comprises the step of mixing a compound I with a catalyzing enzyme, and reacting to obtain an omarigliptin intermediate. The omarigliptin intermediate preparation method has the beneficial effects that the cost of raw materials is reduced; the problem in the prior art that isomer byproducts are generated during preparation of the omarigliptin intermediate and cannot be utilized is effectively solved; the yield and atom economy are increased; and the omarigliptin intermediate preparation method is simple in operation, mild in conditions, environment-friendly and suitable for industrial production.
Owner:SUZHOU LEAD BIOTECH CO LTD
Eutectic of nifedipine and isonicotinamide
ActiveCN108794383AEasy to prepareEasy crystallization processOrganic active ingredientsOrganic chemistry methodsIsonicotinamidePowder diffraction
The invention relates to an eutectic of nifedipine and isonicotinamide and a preparation method and an application thereof. The eutectic of nifedipine and isonicotinamide is characterized by X-ray single crystal diffraction analysis, X-ray powder diffraction analysis, thermogravimetric analysis, differential scanning calorimetry, infrared spectroscopy and the like, and the eutectic is found to have the advantage of higher light stability than the nifedipine. The preparation method of the eutectic of nifedipine and isonicotinamide is simple, can be easily controlled, is good in reproducibility,and can obtain the stable eutectic of nifedipine and isonicotinamide.
Owner:SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
Application of Alfuzosin to treating or preventing Parkinson's disease and related diseases
InactiveCN110354131APharmaceutically activeOrganic active ingredientsNervous disorderDiseaseAlfuzosin
The invention relates to application of Alfuzosin to treating or preventing the Parkinson's disease and related diseases. The invention belongs to the technical field of medicines, and relates to theapplication of Alfuzosin newly-prepared medicines, in particular to application of the Alfuzosin to treating or preventing the Parkinson's disease and related diseases.
Owner:北京安塞迩生物科技有限公司
Alkyl/alkenyl-modified difunctional biphenyl compounds and preparation method thereof
InactiveCN105837388APharmaceutically activeLow yieldCarboxylic acid nitrile preparationOrganic compound preparationOrganic solventSynthesis methods
The invention relates to alkyl / alkenyl-modified difunctional biphenyl compounds and a preparation method thereof. The preparation method comprises the following step: by controlling the reaction temperature at 50-110 DEG C in an organic solvent, carrying out reaction on 2-iodobiphenyl, chloralkane and olefin by using the Pd element as a catalyst for 2-24 hours in the presence of an alkali, a reducer and additives, thereby obtaining the alkyl / alkenyl-modified difunctional biphenyl compounds. Compared with the prior art, the synthesis method of the alkyl / alkenyl-modified difunctional biphenyl compounds is completed for the first time. The method has the advantages of mild conditions, high yield, wide substrate application range and the like, and is simple to operate.
Owner:TONGJI UNIV
Benzofuran fluoroflavanone derivative and preparation method thereof
ActiveCN106905340APharmaceutically activeSimple stepsOrganic active ingredientsOrganic chemistryPhenyl groupBenzene
The present invention relates to the field of pharmaceutical chemistry. A purpose of the present invention is to provide a benzofuran fluoroflavanone derivative and a preparation method thereof, wherein the product has a structure represented by a formula (I), the ring B is selected from phenyl or furyl, and R1, R2 and R3 are independently and respectively selected from hydrogen atom, halogen, cyano, nitro, a C1-C7 alkyl chain and C1-C7 alkoxy. According to the present invention, the benzofuran fluoroflavanone derivative is a class of the benzofuran flavone analogs having the new skeleton, and has potential pharmacological activity; the preparation of the compound can provide the support for the research of the pharmacological activity of the benzofuran flavone; and the preparation method has advantages of simple step and low loss rate, is the completely-new benzofuran flavone derivative synthesis route from the non-aromatic raw material, and provides important significance for the industrial production. The formula (I) is defined in the specification.
Owner:ZHEJIANG UNIV
Trifluoroethanol/difluoroethanol reagent as well as preparation method and application thereof
InactiveCN112457340APharmaceutically activeSimple preparation stepsSilicon organic compoundsCarboxylic acid nitrile preparationArylSimple Organic Compounds
The invention relates to a trifluoroethanol / difluoroethanol reagent and a preparation method and an application thereof, the chemical structural formula of the trifluoroethanol reagent is shown in thespecification, in the formula, R1, R2 and R3 represent substituent groups on silicon atoms, and R1, R2 and R3 are independently selected from aryl, heteroaryl and alkyl respectively. The trifluoroethylation reagent and the difluoroethylation reagent provided by the invention can be used as synthesis intermediates of a plurality of organic compounds, some of the compounds have pharmaceutical activity, the preparation steps of the compounds are simplified, and the synthesis method is mild in condition and wide in substrate applicability.
Owner:WUHAN UNIV
Trifluoromethyl allyl compound as well as preparation method and application thereof
ActiveCN113200856AEasy to synthesizeImprove conversion rateEsterified saccharide compoundsPreparation from carboxylic acid halidesTrifluoromethylationPtru catalyst
The invention discloses a trifluoromethyl allyl compound as well as a preparation method and application thereof. According to the method, allyl alcohol is directly used as a raw material, CF3SO2Na is selected as a trifluoromethylation reagent, a metal-free and cheap photooxidation reduction catalyst is used, and under the catalysis of an organic photooxidation reduction agent, a byproduct SO2 generated in situ is reused as an activated C-OH bond, so that the reaction is carried out in an environment-friendly manner under a mild condition. The allyl alcohol used in the preparation method disclosed by the invention is a MoritA-Baylis-Hillman alcohol allyl alcohol raw material which is simple to synthesize and high in conversion rate, the applicable substrate range is wide, and the preparation cost is low. In addition, the preparation method disclosed by the invention is simple in steps, and has the characteristics of convenience in operation, environment friendliness, excellent stereoselectivity and broad-spectrum functional group tolerance. The trifluoromethyl allyl compound provided by the invention is a general precursor for preparing related CF3 molecules, has potential pharmaceutical activity and biological activity, and can be widely applied to biological and pharmaceutical active molecules.
Owner:NANJING UNIV OF TECH
Selenium-containing chalcone derivative Compound 1, synthesis method thereof, and application of Compound 1 in nonalcoholic steatohepatitis-resistant drugs
ActiveCN110143902APharmaceutically activeThe synthesis method is simpleOrganic chemistryDigestive systemSynthesis methodsStereochemistry
The invention relates to a selenium-containing chalcone derivative Compound 1. The structural formula of the selenium-containing chalcone derivative Compound 1 is shown in the description. The selenium-containing chalcone derivative Compound 1 has nonalcoholic steatohepatitis inhibition activity, and is simple to synthesize and purify. The Compound 1 has the nonalcoholic steatohepatitis inhibitionactivity, can be used for treating nonalcoholic steatohepatitis, and can be used for preparing nonalcoholic steatohepatitis-resistant drugs.
Owner:TIANJIN UNIV OF SCI & TECH
Benzofuran fluoroflavanone derivatives and preparation method thereof
ActiveCN106905340BPharmaceutically activeSimple stepsOrganic active ingredientsOrganic chemistryBenzeneHydrogen atom
The present invention relates to the field of pharmaceutical chemistry. A purpose of the present invention is to provide a benzofuran fluoroflavanone derivative and a preparation method thereof, wherein the product has a structure represented by a formula (I), the ring B is selected from phenyl or furyl, and R1, R2 and R3 are independently and respectively selected from hydrogen atom, halogen, cyano, nitro, a C1-C7 alkyl chain and C1-C7 alkoxy. According to the present invention, the benzofuran fluoroflavanone derivative is a class of the benzofuran flavone analogs having the new skeleton, and has potential pharmacological activity; the preparation of the compound can provide the support for the research of the pharmacological activity of the benzofuran flavone; and the preparation method has advantages of simple step and low loss rate, is the completely-new benzofuran flavone derivative synthesis route from the non-aromatic raw material, and provides important significance for the industrial production. The formula (I) is defined in the specification.
Owner:ZHEJIANG UNIV
Co-crystal of nifedipine and isonicotinamide
ActiveCN108794383BPharmaceutically activeGood light stabilityOrganic active ingredientsOrganic chemistry methodsNifedipineSingle Crystal Diffraction
The invention relates to a co-crystal of nifedipine and isonicotinamide, its preparation method and application. The co-crystal of nifedipine and isonicotinamide was comprehensively characterized by means of X-ray single crystal diffraction analysis, X-ray powder diffraction analysis, thermogravimetric analysis, differential scanning calorimetry analysis, and infrared spectroscopy, and it was found that the Compared with nifedipine, the co-crystal has the advantage of higher light stability. The preparation method of the co-crystal of nifedipine and isonicotinamide is simple, easy to control and good in reproducibility, and stable co-crystal of nifedipine and isonicotinamide can be obtained.
Owner:SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
Cefazolin derivative and its preparation method, oral antibiotic preparation
ActiveCN103755728BChange in water solubilityPharmaceutically activeAntibacterial agentsOrganic chemistryCefazolinAntibiotic Y
The invention discloses a cefazolin derivative and a preparation method thereof as well as an oral antibiotic preparation. The molecular structural formula of the cefazolin derivative is (I) shown in description. The preparation method comprises the following steps: preparing a low-temperature reactant mixed solution of a cefazolin mother nucleus and cefazolin acid and carrying out condensation reaction on the low-temperature reactant mixed solution through heating. The oral antibiotic preparation contains the cefazolin derivative with the structural formula (I). The cefazolin derivative disclosed by the invention has the activity of a cefazolin medicine, has a suitable lipid-water partition coefficient and is suitable for gastro-intestinal tract dosing. The preparation method has easily-controlled reaction conditions, a simple process and a high product yield. The oral antibiotic preparation has a good efficacy, is convenient and safe to use, and can effectively reduce the occurrence rate of abusing antibiotics; meanwhile, the range of selecting the oral antibiotic preparation in China is expanded.
Owner:SHENZHEN CHINA RESOURCES GOSUN PHARMA CO LTD
Cefazolin ester and preparation method thereof as well as oral antibiotic preparation
ActiveCN103739618APharmaceutically activeChange in water solubilityAntibacterial agentsOrganic active ingredientsCefazolinAntibiotic Y
The invention discloses a cefazolin ester and a preparation method thereof as well as an oral antibiotic preparation. The molecular structural formula of the cefazolin ester is as shown in (I) in descriptions. The preparation method of the cefazolin ester comprises preparation of cefazolin ester acid-base salt and esterification reaction of cefazolin ester acid-base salt and carbonic acid-1-iodine ethyl ester ochxl cyclohexyl ester. The oral antibiotic preparation contains the cefazolin ester, the structural formula of which is as shown in (I). The cefazolin ester has the activity of cefazolin medicines and proper lipid / water partition coefficients and is suitable for drug administration of gastrointestinal tracts. The preparation method has the advantages that reaction conditions are easy to control, the process is simple, and the product yield is high. The oral antibiotic preparation has a good medicine effect and is safe and convenient to use; the occurrence rate of antibiotic misuse can be effectively reduced; and meanwhile, the selective range of oral antibiotics at home is expanded.
Owner:SHENZHEN CHINA RESOURCES GOSUN PHARMA CO LTD
Chiral amino indoline derivative as well as preparation method and application thereof
PendingCN114773252APharmaceutically activeEfficient synthesisOrganic active ingredientsOrganic chemistry methodsIndolineCombinatorial chemistry
The invention relates to a chiral aminoindoline derivative and a preparation method and application thereof.The chiral aminoindoline derivative has pharmaceutical activity or can be used for preparing a chiral aminoindoline derivative precursor with pharmaceutical activity, the preparation steps are simple, the conditions are mild, and the chiral aminoindoline derivative is suitable for industrial production. The technical problems that in the prior art, a chiral amino indoline derivative synthesis catalyst is expensive, and reaction conditions are harsh are solved.
Owner:HUAZHONG NORMAL UNIV
2,3,5,6-tetrasubstituted-3H-1,2,4-triazine derivative and synthesis method thereof
The invention discloses a 2,3,5,6-tetrasubstituted-3H-1,2,4-triazine derivative and a synthesis method thereof. Alpha-carbonylenamine and a diazonium salt are taken as starting materials for constructing two C-N bonds in one the step through substitution and cyclization reaction under alkaline conditions in the presence of a copper salt as a catalyst to generate the 2,3,5,6-tetrasubstituted-3H-1,2,4-triazine derivative, and the obtained triazine derivatives have certain potential drug activity. The method has the advantages of easily available raw materials, simple and convenient operation, mild synthesis reaction conditions, high reaction efficiency and diversity of functional groups.
Owner:NANJING NORMAL UNIVERSITY
A kind of method for preparing alogliptin intermediate
The invention provides an omarigliptin intermediate preparation method. The omarigliptin intermediate preparation method comprises the step of mixing a compound I with a catalyzing enzyme, and reacting to obtain an omarigliptin intermediate. The omarigliptin intermediate preparation method has the beneficial effects that the cost of raw materials is reduced; the problem in the prior art that isomer byproducts are generated during preparation of the omarigliptin intermediate and cannot be utilized is effectively solved; the yield and atom economy are increased; and the omarigliptin intermediate preparation method is simple in operation, mild in conditions, environment-friendly and suitable for industrial production.
Owner:SUZHOU LEAD BIOTECH CO LTD
A kind of method for synthesizing indole quinoline compounds
ActiveCN109503572BMild reaction conditionsGood repeatabilityOrganic chemistryAgainst vector-borne diseasesQuinolineCombinatorial chemistry
The invention relates to a method for synthesizing indole quinoline compounds. Indole amide having a directing group and a benzyne precursor are subjected to carbon-hydrogen synthesis under the combined action of a catalyst, an inorganic base, an additive, a solvent and oxygen. The bond / nitrogen-hydrogen bond activates the cyclization reaction to generate the core skeleton of the indole quinoline compound, and then removes the directing group, and undergoes multi-step chemical transformation to synthesize the indole quinoline compound. Compared with the prior art, the method of the present invention can synthesize indoquinoline compounds under the action of cheap, easy-to-obtain and environment-friendly copper catalyst, the reaction conditions are relatively mild, and the reproducibility is good. The Isocryptolepine, which is synthesized by the method of the present invention, Isoneocryptolepine and other indolequinoline alkaloids can fight against malaria that affects human life, which is of great significance to the development of new drugs and has a good application prospect.
Owner:SHANGHAI JIAOTONG UNIV
Substituted furan isoflavone derivatives and preparation method thereof
The invention relates to the field of medicinal chemistry, aims to provide a substituted furan isoflavone derivative and a preparation method thereof. The substituted furan isoflavone derivative has a structure represented by the formula (I), wherein R1 and R2 are separately independently selected from the group consisting of a hydrogen atom, methyl, methoxyl or halogen. The product is a natural furan isoflavone analogue having a novel skeleton, and has potential pharmaceutical activity; the preparation of the compound can provide a support for research of the pharmaceutical activity of furan isoflavones; the preparation method has the advantages of simple steps and low loss rate and has great significance for industrialized production.
Owner:ZHEJIANG UNIV
Selenium-containing chalcone derivative compound 1, its synthesis method and its application in anti-nonalcoholic steatohepatitis drugs
ActiveCN110143902BPharmaceutically activeThe synthesis method is simpleOrganic chemistryDigestive systemHepatitisPerylene derivatives
The present invention relates to a selenium-containing chalcone derivative Compound 1. The structural formula of the selenium-containing chalcone derivative Compound 1 is as follows: the selenium-containing chalcone derivative Compound 1 has the drug activity of non-alcoholic steatohepatitis, The synthesis and purification method is simple, has nonalcoholic steatohepatitis activity, can be used for anti-nonalcoholic steatohepatitis treatment, and can be applied to the preparation of nonalcoholic steatohepatitis medicine.
Owner:TIANJIN UNIV OF SCI & TECH
Substituted benzofuroylhydrazone derivatives and preparation method thereof
ActiveCN106749135BPharmaceutically activeSimple stepsOrganic active ingredientsOrganic chemistryFuranHalogen
The invention relates to the field of medical chemistry, and aims at providing a substituted benzofuran hydrazone derivative and a preparation method thereof. The product has a structure as shown in a formula (I), wherein B ring is selected from phenyl, furyl, thienyl and naphthyl; and R1, R2 and R3 are independently selected from hydrogen atoms, halogen, hydroxy, alkyl chain of C1-C7, alkoxy of C1-C7, nitryl or cyan. The benzofuran hydrazone derivative is a natural furan hydrazone derivative with a new frame, has potential medicinal activity; and the preparation of the compound can be used for supporting researches of benzofuran hydrazone medicinal activity. The preparation method is simple and easily available in steps, and has an important meaning for industrial production.
Owner:ZHEJIANG UNIV
Preparation method of difunctional biphenyl compound modified by alkyl and alkenyl
InactiveCN105837388BPharmaceutically activeLow yieldCarboxylic acid nitrile preparationOrganic compound preparationOrganic solventSynthesis methods
The invention relates to alkyl / alkenyl-modified difunctional biphenyl compounds and a preparation method thereof. The preparation method comprises the following step: by controlling the reaction temperature at 50-110 DEG C in an organic solvent, carrying out reaction on 2-iodobiphenyl, chloralkane and olefin by using the Pd element as a catalyst for 2-24 hours in the presence of an alkali, a reducer and additives, thereby obtaining the alkyl / alkenyl-modified difunctional biphenyl compounds. Compared with the prior art, the synthesis method of the alkyl / alkenyl-modified difunctional biphenyl compounds is completed for the first time. The method has the advantages of mild conditions, high yield, wide substrate application range and the like, and is simple to operate.
Owner:TONGJI UNIV
Substituted furan isoquinolinone derivatives and preparation method thereof
The invention relates to the field of medical chemistry, and aims at providing a substituted furan flavonol derivative and a preparation method thereof. The substituted furan flavonol derivative has a structure represented by formula (I) shown in the description; and in the formula (I), B ring is selected from a phenyl group or a furyl group; and R1, R2 and R3 are respectively independently selected from the hydrogen atom, a hydroxyl group, a methoxy group, a dimethylamino group, a nitro group and a cyan group. The above product is a new skeleton natural furan isoquinolone analog and has potential drug activity, and the preparation method of the compound provides support for the drug activity researches of furan isoquinolones. The preparation method of the derivative has the advantages of simple steps and easiness in obtaining, and is of great significance to industrial production.
Owner:ZHEJIANG UNIV
A kind of aza 11-membered ring compound and its preparation method, use and medicine containing the compound
ActiveCN112142683BPharmaceutically activeEasy accessOrganic active ingredientsOrganic chemistryBenzylideneacetoneStructural formula
Owner:CHENGDU UNIV
A kind of oxindole spirocyclopropane derivative and its synthetic method
ActiveCN104098507BRaw materials are easy to obtainImprove stabilityOrganic chemistryOrganic synthesisCyclopropane
The invention discloses an oxindole spiro-cyclopropane derivative and a synthetic method thereof and belongs to the technical field of organic synthesis. Alpha-keto ester and an alpha,beta-unsaturated oxindole compound react under the promotion of a phosphorus reagent to obtain the oxindole spiro-cyclopropane derivative. Used raw materials are simple, easy to obtain and good in stability; the synthetized oxindole spiro-cyclopropane derivative contains multiple quaternary carbon centers, and substituent groups on quaternary carbon atoms are rich in kind and can be transformed flexibly; the synthetized compound has the potential drug activity, and a candidate compound is provided for design, synthesis and development of novel drug molecules which contain oxindole spiro-cyclopropane structures.
Owner:TAIYUAN UNIV OF TECH
A kind of furanocoumarin derivative and its preparation method
ActiveCN106279083BPharmaceutically activeCondensation reaction steps are simpleOrganic chemistryFuranDrug activity
The invention relates to the field of medicines and aims to provide a furan coumarin derivative and a preparation method thereof. A furan ring of the furan coumarin derivative is substituted with a methyl; the preparation method of the furan coumarin derivative comprises the following steps: taking 4-hydroxy-3-methylbenzofuran-5-carbaldehyde and weak base, uniformly dispersing in a reaction solvent a to obtain a raw material mixture, then carrying out a reaction for 1-3 hours at a temperature of 70 DEG C, filtering reaction liquid to obtain a precipitate, and washing the precipitate to obtain the furan coumarin derivative. The furan coumarin derivative provided by the invention is an isopsoralen analogue with a novel skeleton and has potential drug activity; the preparation of the compound can provide a support for the research on the activity of a furan coumarin drug; the preparation method provided by the invention is simple in step and low in loss rate.
Owner:ZHEJIANG UNIV
A kind of 2,2,5-trisubstituted 1,3,4 oxadiazole derivative and its synthesis method
ActiveCN107445914BImprove toleranceMild reaction conditionsOrganic chemistryOrganic synthesisSynthesis methods
The invention discloses a 2,2,5-tri-substituted 1,3,4-oxadiazole derivative and a synthetic method thereof and belongs to the technical field of organic synthesis. The synthetic method comprises the following steps: reacting N-acyl biazolefin and an alpha-dicarbonyl compound in presence of a three-coordinate phosphrus reagent, thereby obtaining the 2,2,5-tri-substituted 1,3,4-oxadiazole derivative. The synthetic method disclosed by the invention is mild in reaction conditions, wide in substrate application range and high in functional group tolerance; a synthetic technique for efficiently synthesizing the 2,2,5-tri-substituted 1,3,4-oxadiazole derivative with a novel structure is provided; and the invention provides a candidate compound for developing novel oxadiazole pharmaceutical molecules.
Owner:TAIYUAN UNIV OF TECH
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