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Alkaline buffering solution for establishing DNA coding compound library and application thereof
ActiveCN109456368AIncrease success rateRich diversitySugar derivativesSugar derivatives preparationDna encodingSodium borohydride
The invention relates to an alkaline buffering solution for establishing a DNA coding compound library and an application thereof. The alkaline buffering solution is a boric acid buffering solution with the concentration of 250mM, the electric conductivity of the boric acid buffering solution is 5177ppm+ / -10 percent, the density is 1.0246 g / mL+ / -3 percent, and the pH is 9.4+ / -0.1. The buffering solution has the characteristics of wide substrate application range and high universality and is applied to the amide synthetic reaction of DNA-CO2H and small molecular organic amine and applied to thereduction ammonolysis reaction for generating imine from DNA-NH2 and small molecular organic aldehyde and reducing the imine by virtue of sodium borohydride, and has the advantage of high conversionrate. The various alkaline buffering solutions prepared in the invention and used for synthesizing the DNA coding compound library is mild in reaction conditions, simple in operation, wide in substrate application range, relatively high in applicability and suitable for the mass synthesis of the DNA coding compound library.
Owner:上海药明康德新药开发有限公司 +1
Chiral 3,3-disubstituted oxoindole derivative, and synthetic method and application thereof
ActiveCN104693092AHigh yieldGood diastereoselectivityOrganic chemistryMetabolism disorderChemical synthesisSynthesis methods
The invention discloses a chemical synthetic method of a novel chiral 3,3-disubstituted oxoindole derivative with PTP1B inhibiting action. With diazoisatin, indole, arylamine and aldehyde ester as raw materials, a metal catalyst as catalyst, chiral phosphoric acid as a co-catalyst, an organic solvent as a solvent, and molecular sieve shown in the specification as an additive, a one-step reaction is performed under the condition of 25 degrees centigrade, and the product undergoes column chromatography purification to obtain the target product. The synthetic method has the advantages of high step economy, strong atom economy, high diastereoselectivity and enantioselectivity, high yield, mild reaction condition, and simple and safe operation. The optically pure chiral 3,3-disubstituted oxoindole derivative with two chiral centers synthesized in the invention is an important intermediate in chemical engineering, chemistry and medicines, and has a wide application prospect in the fields of medicines and the chemical engineering.
Owner:广东和博制药有限公司
Polyphenyltriazole formate, and preparation method and application thereof
ActiveCN106243352APrevent bomb attackImprove solubilityOrganic chemistryFluorescence/phosphorescenceFluorescenceFormate
The invention discloses a polyphenyltriazole formate, and a preparation method and application thereof. A phenylpropargylic acid dibasic ester monomer and a dibasic organic azido monomer used as raw materials are subjected to polymerization reaction in a polar aprotic solvent to obtain the polyphenyltriazole formate. The preparation method has the advantages of accessible reaction raw materials and no byproduct generation in the polymerization reaction process, and conforms to the atom economy. The polymerization reaction has wide substrate applicability and favorable functional group compatibility, and is convenient for introducing multiple functional groups. The polymerization reaction does not use any metal catalyst, and thus, can eliminate the influence of catalyst residues on the biological and photoelectric properties of the polymer material. The polyphenyltriazole formate has the advantages of favorable processability, higher heat stability, higher degradability and higher aggregation-induced luminescence, and has potential application values in the aspects of optical plastics, biomedical materials, fluorescence detection and the like.
Owner:SUZHOU UNIV
Method for synthesizing cis-olefin by catalyzing decarboxylation coupling reaction of NHP ester and aryl-terminated alkyne with iridium
InactiveCN109293468AHigh yieldHigh selectivityCarbamic acid derivatives preparationOrganic compound preparationIridiumAryl
The invention provides a method for synthesizing Z-selective olefin by catalyzing a decarboxylation coupling reaction of an NHP ester and aryl-terminated alkyne with iridium. The aryl-terminated alkyne and its derivative and the NHP ester undergo a one-pot reaction under the irradiation of blue lights under the catalysis of iridium to obtain the corresponding Z-selective olefin compound. The method has the advantages of simple process and high cis-selectivity.
Owner:CENT SOUTH UNIV
Method for synthesizing carbamate by using olefin, amine, carbon dioxide and Togni reagent
ActiveCN107188833AImprove compatibilitySimple and safe operationCarbamic acid derivatives preparationOrganic compound preparationCarbamateDistillation
The present invention relates to a method for synthesizing carbamate by using an olefin, an amine, carbon dioxide and a Togni reagent. The method comprises: in a high pressure reaction kettle, sequentially adding an organic solvent, an olefin, an amine and a Togni reagent, adding a copper salt as a catalyst, introducing carbon dioxide, carrying out a stirring reaction for 5-24 h at a temperature of 40-100 DEG C, cooling to a room temperature after completing the reaction, slowly releasing carbon dioxide to achieve an atmospheric pressure, carrying out water washing on the reaction solution, extracting with ethyl acetate, drying with anhydrous magnesium sulfate, carrying out pressure reducing distillation concentration to obtain a crude product, and carrying out column chromatography purification to obtain the carbamate compound. According to the present invention, the synthesis method avoids the use of toxic raw materials such as phosgene or isocyanate, and the like, has characteristics of safe and simple operation, mild reaction condition, good functional group compatibility, wide substrate applicability and high yield, is suitable for industrial production, and has good application prospects in synthesis of pesticides, medicine, and natural products.
Owner:SOUTH CHINA UNIV OF TECH
3-p-*alkene-1-secondary amine type compound and preparing method and weeding application thereof
ActiveCN110105224ALow toxicityImprove securityBiocideOrganic compound preparationSilica gelQuenching
The invention discloses a 3-p-*alkene-1-secondary amine type compound and a preparing method and weeding application thereof. In the method, a 3-p-alkene-1-Schiff base type compound serves as the rawmaterial, in a polarity organic solvent, a reducing agent is put in batches at the temperature from -10 DEG C to 50 DEG C, reaction is conducted for 1-24 hours, reaction liquid is subjected to distilled water quenching, dichloromethane extracting, anhydrous sodium sulfate drying, filtering and depressurized distilling after reaction ends to obtain a crude 3-p-alkene-1-secondary amine type compoundproduct, and the column chromatography on silica gel is conducted to obtain a pure product. The growth injury symptoms of rice barnyard grass roots and stems are measured through a culture dish seedgermination method under the culture of the 3-p-alkene-1-secondary amine type compound with different concentrations, and the weeding activity of the compound is evaluated. The method is simple in process, mild in condition, high in speed, high in yield and wide in substrate application range, and the product 3-p-alkene-1-secondary amine type compound has a quite good restraining effect on the growth of the rice barnyard grass roots and stems.
Owner:INST OF CHEM IND OF FOREST PROD CHINESE ACAD OF FORESTRY
Polyvinyl thioether ester as well as preparation method and application thereof
ActiveCN110483773AWide substrate applicabilityImprove compatibilityFluorescence/phosphorescencePolymer scienceAlkyne
The invention discloses polyvinyl thioether ester as well as a preparation method and application thereof. The polyvinyl thioether ester is obtained through solution polymerization reaction by takinga binary acetylene acid ester internal alkyne monomer and a binary sulfydryl monomer as raw materials. The reaction raw materials are easy to obtain, no by-product is generated in the polymerization reaction process, and the atom economy is met; the polymerization reaction has wide substrate applicability and good functional group compatibility, and various functional groups can be conveniently introduced; no catalyst is used in the polymerization reaction, so that the influence of catalyst residues on photoelectric and biological properties of the polymer material can be eliminated. The polyvinyl thioether ester prepared by the invention has good processability, high thermal stability and aggregation-induced emission performance, and has application value in the aspects of optical plastics, biomedical materials, fluorescence sensing and the like.
Owner:SUZHOU UNIV
Synthesis method of [60]fullerene dihydropyrrole derivative
InactiveCN107118150AImprove compatibilityWide substrate applicabilityOrganic chemistryChemistryFullerene derivatives
The invention discloses a synthesis method of a [60]fullerene dihydropyrrole derivative, and belongs to the technical field of synthesis of fullerene derivatives. The synthesis method of the [60]fullerene dihydropyrrole derivative, disclosed by the invention, is characterized in that a specific process comprises the following steps: by taking [60]fullerene, a sulfonyl hydrazone compound and a nitrile compound as reaction raw materials, carrying out cyclization reaction at 110 DEG C to 120 DEG C under the acceleration effect of Ag (I) to prepare a target product, i.e., the [60]fullerene dihydropyrrole derivative. The synthesis process disclosed by invention has wide substrate applicability and relatively good functional group compatibility, and can be used for synthesizing fullerene macromolecular compounds; the reaction can be used for synthesizing raw materials, which are simple and easy to obtain, into the fullerene derivative with various substituent groups.
![Synthesis method of [60]fullerene dihydropyrrole derivative](https://images-eureka.patsnap.com/patent_img/4e08b435-e80f-4159-bd83-990f5570af4e/BDA0001298876530000011.png "Synthesis method of [60]fullerene dihydropyrrole derivative")
![Synthesis method of [60]fullerene dihydropyrrole derivative](https://images-eureka.patsnap.com/patent_img/4e08b435-e80f-4159-bd83-990f5570af4e/BDA0001298876530000012.png "Synthesis method of [60]fullerene dihydropyrrole derivative")
![Synthesis method of [60]fullerene dihydropyrrole derivative](https://images-eureka.patsnap.com/patent_img/4e08b435-e80f-4159-bd83-990f5570af4e/BDA0001298876530000031.png "Synthesis method of [60]fullerene dihydropyrrole derivative")
Owner:HENAN NORMAL UNIV
Method for synthesizing trifluoromethyl-containing carbamate by using carbon dioxide
ActiveCN107188832AImprove compatibilityHigh yieldCarbamic acid derivatives preparationOrganic compound preparationCarbamateDistillation
The invention relates to a method for synthesizing trifluoromethyl-containing carbamate by using carbon dioxide. The method comprises the steps of sequentially adding an organic solvent, alkyne, amine and a Togni reagent into a high-pressure reaction kettle, and then adding copper salt serving as a catalyst and an organic compound containing nitrogen or phosphor serving as a ligand; after that, replenishing the high-pressure reaction kettle with carbon dioxide, and stirring for carrying out a reaction for 5-24h at the temperature of 40-80 DEG C; after the reaction is finished, cooling to the room temperature, slowly discharging carbon dioxide to normal pressure, washing reaction liquid with water, extracting by using ethyl acetate, drying by using anhydrous magnesium sulfate, and then carrying out reduced pressure distillation and concentration to obtain a crude product; then, purifying by means of column chromatography to obtain a trifluoromethyl-containing carbamate compound. The method for synthesizing the trifluoromethyl-containing carbamate has the advantages of being easy in obtaining of raw materials, safe and simple in operation, mild in reaction conditions, good in functional group compatibility, wide in substrate applicability, high in yield of target product, and the like, is beneficial to industrial production, and has potential application prospect in synthesis of pesticides and medicines.
Owner:SOUTH CHINA UNIV OF TECH
Recombinant bacterium expressing D-threonine aldolase and construction method and application of recombinant bacterium
ActiveCN110272856AGood catalyticWide substrate applicabilityBacteriaMicroorganism based processesCatalytic effectThreonine aldolase
The invention discloses a recombinant bacterium expressing a D-threonine aldolase and a construction method and application of the recombinant bacterium, and belongs to the technical field of enzyme engineering. The recombinant bacterium of the present invention expresses the D-threonine aldolase with an amino acid sequence as shown in SEQ ID NO. 2. The invention provides the D-threonine aldolase which can be used as a catalyst for the synthesis of chiral beta-hydroxy-alpha-amino acid, the catalytic efficiency (conversion rate) is high to 65%, the stereoselectivity is high with (e.e.) of 99% and (d.e.) of 95%, and the suitable reaction condition is mild and environment-friendly. According to the present invention, the D-threonine aldolase has good catalytic effect, wide substrate applicability, and good application and development prospect.
Owner:JIANGNAN UNIV
New method for synthesis of alkenyl thiocyanate derivative
ActiveCN106167459AReduce usageGood configuration selectivityOrganic chemistryChemical synthesisOrganic solvent
Belonging to the technical field of pharmaceutical chemical synthesis, the invention discloses a method for synthesis of an alkenyl thiocyanate derivative. The method comprises the steps of: adding haloalkyne and thiocyanate as raw materials into a reaction vessel, taking a silver salt as the catalyst and using an organic solvent as the solvent, carrying out heating reaction, then cooling the obtained reacted solution to room temperature, and then performing purification, thus obtaining the alkenyl thiocyanate derivative. The method provided by the invention adopts haloalkyne and thiocyanate as the raw materials to carry out thiocyanation reaction for one-step synthesis of the alkenyl thiocyanate derivative. Use of concentrated sulfuric acid, mercury salt and other dangerous goods is avoided, the reaction raw materials are easily available, the reaction operation is safe and simple, the reaction process is environment-friendly, the substrate has wide applicability, the functional group has strong compatibility, the separation yield is high, the product configuration selectivity is good, the product can be enlarged to gram scale, and the product reserved halogen can be convenient for further conversion.
Owner:SOUTH CHINA UNIV OF TECH
Application of immobilized lipase Lipozyme TLIM as catalyst for unsymmetrical Michael addition reaction
The invention relates to novel application of substance, in particular to application of immobilized lipase Lipozyme TLIM as a catalyst for an unsymmetrical Michael addition reaction. The invention has the advantages of wide substrate applicability, good and catalysis activity and selectivity, easy operation, and can be recycled. The invention further provides a method of using the immobilized lipase Lipozyme TLIM to catalyze the unsymmetrical Michael addition reaction. The method has high yield and favorable selectivity.
Owner:SOUTHWEST UNIVERSITY
Novel beta-glucosidase and genes thereof and application of beta-glucosidase to glucoside synthesis
InactiveCN102676478AImprove thermal stabilityQuick responseBacteriaMicroorganism based processesProtein proteinAlglucerase
The invention provides a new protein with beta-glucosidase activity. A coding nucleic acid of the protein comprises an expression vector of the nucleic acid and a transformant containing the nucleic acid or the expression vector. The invention also provides an application of the new protein as a catalyst in catalyzing a monosaccharide and alcohol to carry out counter hydrolysis reaction to form glucoside. Compared with the traditional beta-glucosidase in almonds, the beta-glucosidase provided by the invention has better thermal stability, and compared with the beta-glucosidase from many other microorganisms, the beta-glucosidase provided by the invention can endure glucoses with higher concentrations and has a good industrial application prospect in glucoside synthesis.
Owner:EAST CHINA UNIV OF SCI & TECH
Reductase, reductase gene, recombinant enzyme, preparation method of recombinant enzyme and application
InactiveCN101979527AGood catalyticWide substrate applicabilityBacteriaOxidoreductasesEntire cellWild type
The invention discloses reductase, a reductase gene, a recombinant expression vector containing the gene, a recombinant expression transformant containing the gene, a recombinant enzyme of the reductase, a preparation method for the recombinant enzyme and application of the reductase or the recombinant enzyme of the reductase which serves as a catalyst to preparing optical active chiral alcohol from an asynchronous reductive prochiral carbonyl compound. The reductase or the recombinant enzyme of the reductase can be derived from Bacillus sp. China General Microbiological Culture Collectio Center (CGMCC) No. 2549 and applied to preparing the optical active chiral alcohol from the asynchronous reductive prochiral carbonyl compound when used as the catalyst, and has high catalysis efficiency and stereoselectivity, and the reaction conditions are mild and environment-friendly. Compared with the entire cell of the wild Bacillus sp. CGMCC No. 2549, the reductase of the invention has better catalysis effect, wider substrate applicability and excellent industrial application development prospect.
Owner:EAST CHINA UNIV OF SCI & TECH
Polysubstituted tetrahydrofuran derivatives as well as synthesis method and application thereof
ActiveCN104744410AHigh yieldGood diastereoselectivityOrganic chemistryMetabolism disorderMolecular sieveCarbonyl group
The invention relates to polysubstituted tetrahydrofuran derivatives and a chemical synthesis method thereof. The chemical synthesis method comprises the following steps: carrying out one-step reaction on raw materials (a diazo compound and a 3-hydroxyl-carbonyl flavone compound) in an organic solvent in the presence of a metal catalyst and an additive which is a molecular sieve shown in the specification; and carrying out column chromatography purification to obtain the target product. The chemical synthesis method of the polysubstituted tetrahydrofuran derivatives has the advantages of environmental benefit, step economy, atom economy, diastereoselectivity and high yield; in addition, the reaction conditions are mild, the applicability of the substrate range is wide and the operation is simple and safe. The invention discloses that the polysubstituted tetrahydrofuran derivatives with multiple chiral centers have PTPlB inhibiting effect; and therefore, the polysubstituted tetrahydrofuran derivatives are important chemical engineering, chemical and medical intermediates and have a wide prospect in the field of pharmaceutical chemicals.
Owner:EAST CHINA NORMAL UNIVERSITY
Synthetic method of diaryl sultam compounds
The invention discloses a synthetic method of diaryl sultam compounds. According to the method, transition metal palladium is taken as a catalyst, N-methoxybenzenesulfonamide compounds and aryne precursors are subjected to a cyclization reaction based on functionalization of a C-H bond in an ortho-position of -SO2NHOMe in N-methoxybenzenesulfonamide in presence of fluoride, and a series of diarylsultam compounds are synthesized efficiently and conveniently. The method has the advantages of simple and easily available raw materials, simple reaction operation, high substrate applicability, highatom utilization ratio and the like.
Owner:SHAANXI NORMAL UNIV
Zirconium-based metal organic framework material as well as preparation method and application thereof
InactiveCN112808311ALow priceEasy to makeOrganic-compounds/hydrides/coordination-complexes catalystsBenzoic acidSuperoxide
The invention discloses a zirconium-based metal organic framework material as well as a preparation method and application thereof. The chemical formula of the zirconium-based metal organic framework material is Zr6O4 (OH) 4 (L-S) 1.2 (L-2Me) 4.8, in the formula, L-S is 2',5'-dimethyl [1,1':4',1''-triphenyl]-4,4,dicarboxylic acid, L-2Me is 4, 4'-(benzo [c] [1, 2, 5] thiadiazole-4, 7-diyl) dibenzoic acid. The zirconium-based metal organic framework material disclosed by the invention can simultaneously generate superoxide anion free radicals (O2.-) and singlet oxygen (1O2) under an illumination condition, is environment-friendly, low in price and simple to prepare, has the advantages of high catalytic activity, mild reaction conditions, convenience in operation, high substrate applicability and the like when being used for a photo-induced aerobic oxidation reaction, and has a good application prospect.
Owner:SOUTH CHINA UNIV OF TECH
Coding gene of meso-2,3-butanediol dehydrogenase, recombinase and preparation method and application of recombinase
InactiveCN105200068AGood catalyticWide substrate applicabilityBacteriaMicroorganism based processesBacillus licheniformisDiol
The invention discloses a coding gene of meso-2,3-butanediol dehydrogenase, a recombinant expression vector and recombinant expression transformant with the gene, a preparation method of recombinase, and application of the recombinase as a catalyst in an asymmetrically reducing prochiral dicarbonyl compound for preparing optical activity chiral diols. The meso-2,3-butanediol dehydrogenase comes from Bacillus licheniformis CICIMB0109, can be used as a catalyst for efficiently synthesizing chiral diols, is high in catalytic activity and stereoselectivity, mild in suitable reaction condition and friendly to the environment, and has quite good application and development prospects.
Owner:JIANGNAN UNIV
Alcohol compound-based in-situ deoxygenation fluorination synthesis method and alcohol compound-based <18>F radiolabeling method
PendingCN110724026ASimple and fast operationSimple processSugar derivativesCarboxylic acid nitrile preparationOrganic basePotassium fluoride
The invention discloses an alcohol compound-based in-situ deoxidation fluorination synthesis method and an alcohol compound-based <18>F radiolabeling method. Alkyl alcohols such as 4-phenyl-1-butanol,which are used as raw materials, react with trifluoromethylsulfonyl fluoride gas, generated by N-phenylbis(trifluoromethanesulphonimide) and potassium fluoride in a short time, under the catalysis ofan organic alkali to realize the deoxygenation fluorination reaction of alcoholic hydroxyl groups, and monofluoro-substituted compounds are obtained after separation and purification. The synthesis method has the characteristics of high atom economy, simplicity in preparation, greenness, high efficiency, high selectivity and few elimination byproducts, is suitable for large-scale production, andcan be applied to the radioactive isotope <18>F labeling process to label drug molecules containing alcoholic hydroxyl groups.
Owner:HEFEI UNIV OF TECH
Epoxy hydrolase, gene thereof and application thereof
ActiveCN102242085AHigh catalytic efficiencyDeepen understandingBacteriaHydrolasesEpoxyBacillus megaterium
The invention discloses a novel epoxy hydrolase, a gene of the epoxy hydrolase, a recombination expressor and a recombination expression transformant containing the gene, a method for preparing a recombinase by using the recombination expression transformant, and an application of the recombined epoxy hydrolase in catalyzing racemic epoxide enantioselective hydrolysis for producing chiral epoxideand diol. The recombined epoxy hydrolase provided by the invention is originated from bacillus megaterium. The epoxy hydrolase can be used for synthesizing various optically active epoxides and vicinal diols. The epoxy hydrolase has advantages of high catalysis efficiency, high enantioselectivity, and mild reaction condition. The epoxy hydrolase is environment-friendly. Compared with wild bacterium whole cells, the epoxy hydrolase provided by the invention contributes to a better catalysis effect and a better applicability of substrates. The epoxy hydrolase has a good prospect to be applied in industrial productions.
Owner:SUZHOU BAIFUAN ENZYME TECH
4-aza-aryl alkanol compound and synthetic method thereof
ActiveCN108658853AImprove compatibilityAtom economy is highOrganic chemistryThermal energyLight energy
The invention discloses a 4-aza-aryl alkanol compound and a synthetic method thereof. The synthetic method comprises the following steps: reacting an aza-aryl compound as shown in formula I with alcohol as shown in formula II under the condition of thermal energy and / or light energy and / or microwave in an organic solvent in an anaerobic atmosphere and in the presence of a hypervalent iodine aryl compound Ar-IIII to obtain the 4-aza-aryl alkanol compound as shown in formula III. By the synthetic method of the 4-aza-aryl alkanol compound, alkanol can be directly used as a substrate, 4-position C(sp3)-H is activated in a regioselective manner and is subjected to functionalization, and the synthetic method has the advantages of simplicity in reaction, gentle condition, zero metal, high atom economy and the like; and the synthesized 4-position aza-aryl substituted alcohol compound can be widely applied to synthesized building blocks designed by total synthesis and new drug derivatives.
Owner:SUZHOU UNIV
Method for compounding nitrogenous polynary heterocyclic compound
ActiveCN107602570AImprove compatibilityRaw materials are easy to obtainOrganic chemistryChemical synthesisCatalytic effect
The invention belongs to the field of chemical synthesis and discloses a method for compounding a nitrogenous polynary heterocyclic compound. The method comprises the following steps: (1) performing Ugi four-component reaction on aldehyde RCHO, iso-nitrile compound R'NC, o-halide arylamine and substituted propiolic acid R2-C is equivalent to C-CO2H under the solvent existence condition and removing the solvent after ending the reaction, thereby acquiring a product of the step (1); (2) performing consecutive reaction on the product acquired in the step (1) and 1,3-dipole reaction reagent underthe catalytic effect of cupric salt under the solvent existence condition and the inert atmosphere and then purifying the acquired reaction solution, thereby acquiring the product acquired in the step(2); (3) performing acid promotion reaction on the product acquired in the step (2) and the acid under a heating condition with or without solvent and purifying the acquired reaction solution after ending the reaction, thereby acquiring a target product. The method has wide substrate applicability; the preparation method is simple and efficient; the nitrogenous polynary heterocyclic compound hashigh functional group compatibility and wide popularizing prospect.
Owner:JINAN UNIVERSITY
Method for preparing D-aromatic amino acid by cascade reaction
ActiveCN110699396AGood catalyticWide substrate applicabilityHydrolasesFermentationPtru catalystCombinatorial chemistry
The invention discloses a method for preparing D-aromatic amino acid by cascade reaction. D-N-carbamoylase as shown in an amino acid sequence SEQ ID NO.2 serves as a catalyst, and the D-aromatic aminoacid is prepared in hydantoinase process cascade reaction. The D-N-carbamoylase can serve as the catalyst applied to preparation of optical pure D-aromatic amino acid in a hydantoinase process, the D-N-carbamoylase is good in solubility, high in catalysis efficiency (conversion rate) reaching 99%, high in stereoselectivity (e.e.) reaching 99.9%, applicable to mild reaction conditions and environmentally friendly. The D-N-carbamoylase is excellent in catalysis effect, wide in substrate applicability and excellent in application and development prospect.
Owner:JIANGNAN UNIV
Polysubstituted benzothienopyridine compound and preparation method thereof
InactiveCN112592352AImprove toleranceRaw materials are easy to obtainOrganic chemistryOrganic synthesisCitalopram
The invention belongs to the technical field of organic synthesis, and discloses a polysubstituted benzothienopyridine compound and a preparation method thereof. The preparation method comprises the steps of dissolving nitrile amino metal salt and alkali in an organic solvent in a reactor, stirring to react at the temperature of 90-130 DEG C, and separating and purifying the reaction product to obtain the polysubstituted benzothienopyridine compound, wherein the reaction formula of the preparation method is shown as a formula (I) in the description. According to the method disclosed by the invention, a series of polysubstituted benzothienopyridine compounds are synthesized by taking simple and readily available 2-methyl-3-alkynyl benzothiophene and nitrile as reaction raw materials. The method has the characteristics of simple and readily available raw materials, convenience in operation, no transition metal, high step economy, high atom economy, wide substrate applicability, good tolerance of functional groups and the like; and part of application research is carried out, and a derivative product of a drug molecule citalopram is synthesized.
Owner:SOUTH CHINA UNIV OF TECH
Iron-based catalyst for synthesizing compound with quinazolinone structure, and preparation method and application of iron-based catalyst
ActiveCN108144634AMagneticEasy post-processingPhysical/chemical process catalystsOrganic chemistryPrimary alcoholPeroxide
The invention belongs to the technical field of liquid phase oxidation, and discloses an iron-based catalyst for synthesizing a compound with a quinazolinone structure, and a preparation method and application of the iron-based catalyst. The iron-based catalyst mainly consists of carbon and nitrogen elements, wherein the weight ratio of various elements is as follows: 5-10 wt% of iron, 55-70 wt% of carbon and 1-20 wt% of nitrogen, and the particle size of the iron nano particles of the iron-based catalyst is 5-20 nm. The iron-based catalyst is prepared by taking a magnetic ion liquid as a precursor and sucrose as a carbon source, and carrying out pyrolysis in an inert atmosphere. In the presence of the iron-based catalyst in a very low usage amount, peroxide used as an oxidant and no otheradditives, the quinazolinone compound is synthesized by taking anthranilamide compounds and primary alcohols as raw materials. The iron-based catalyst provided by the invention is easy to synthesizemassively, has magnetism, can be recycled, and has the advantages of mild reaction condition, greenness, environmental protectiveness, easy separation of products, high selectivity and yield of products, and a good application prospect.
Owner:DALIAN INST OF CHEM PHYSICS CHINESE ACAD OF SCI
Poly-substituted alkynyl amidine compounds, preparation method and application thereof
ActiveCN110317221AImprove toleranceRaw materials are easy to obtainGroup 4/14 element organic compoundsBulk chemical productionOrganic solventOrganic synthesis
The invention belongs to the technical field of organic synthesis, and discloses poly-substituted alkynyl amidine compounds, a preparation method and an application thereof. The preparation method includes adding and dissolving an alkynyl bromide palladium salt catalyst, an additive and alkali in an organic solvent in a reactor, finally, adding isonitrile and stirring the mixture to react at 90-100 DEG C, and separating and purifying the reaction product to obtain the poly-substituted alkynyl amidine compounds, wherein the reaction formula is shown in a formula (I). The method uses simple andeasily available alkynyl bromide, amine and isonitrile as reaction raw materials to synthesize a series of poly-substituted alkynyl amidine compounds. The method has the characteristics of simple andeasily-available raw materials, convenient operation, mild conditions, high step economy, wide substrate applicability, good tolerance of functional groups and the like; and some of application studies of the method are carried out and a variety of useful nitrogen-containing heterocycles are synthesized.
Owner:SOUTH CHINA UNIV OF TECH
Cis-p-alkyl-1,8-disecondary amine compound, and preparation method and weeding application thereof
Owner:RES INST OF FORESTRY NEW TECH CHINESE ACAD OF FORESTRY +1
Novel five-substituted 2,3-dihydropyrrole derivative and preparation method and application thereof
InactiveCN107721895AHigh stereoselectivityWide substrate applicabilityOrganic chemistryMetabolism disorderSynthesis methodsSolvent
The invention relates to a synthesis method of five-substituted 2,3-dihydropyrrole. The synthesis method comprises the specific steps that amine, aldehyde and alpha-keto-amide which are simple and areeasy to obtain are used as raw materials, an ethyl alcohol is used as a solvent and glacial acetic acid is used as a catalyst to perform reaction under the condition of 60-80 DEG C, and a cis-form dihydropyrrole compound is obtained. The method has the advantages that the method is simple and easy to operate, the reagents are cheap and easy to obtain, the atom economy is good, reaction stereoselectivity is high and the substrate applicability is good. In addition, the alpha-glucosidase inhibiting activity of the compound is evaluated for the first time, a result shows that the compound can very well inhibit alpha-glucosidase and is better than acarbose. The synthesis method has the wide prospect on the aspects of development and application of diabetes treating drugs.
Owner:TIANJIN UNIV OF SCI & TECH +1
Method for green oxidation synthesis of N-substituted 2H-indazole compound
ActiveCN112574112AHigh yieldSimple and fast operationOrganic chemistryPotassium persulfatePersulfate
The invention relates to a green oxidation synthesis method of an N-substituted 2H-indazole compound shown as a formula (I); the method comprises the following steps: dissolving a 2H-indazole compoundshown as a formula (II) and pyrazole in a solvent, adding an oxidant, reacting at 60-100 DEG C for 10-12 hours, and carrying out aftertreatment on the obtained reaction solution to obtain the N-substituted 2H-indazole compound shown as the formula (I). The molar ratio of the 2H-indazole compound shown in the formula (II) to the pyrazole to the oxidizing agent is 1: 1.5-3: 2-4; and the oxidant issodium persulfate, potassium persulfate or ammonium persulfate; according to the method, the N-substituted indazole compound is synthesized by adopting the cheap and easily available oxidant potassiumperoxodisulfate, so that the method is simple and convenient to operate, high in product yield and wide in substrate applicability, and meets the requirements of green chemistry.
Owner:ZHEJIANG UNIV OF TECH
Vinyl sulfone-based silicon nano material surface functionalization method
The invention discloses a vinyl sulfone-based silicon nano material surface functionalization method which comprises the step: enabling a vinyl sulfone derivative to directly react with silicon hydroxyl on the surface of a material under a catalysis condition, thereby achieving covalent functionalization of a silicon-based material. By adopting the method, functionalization of multiple silicon nano materials can be achieved, and the method is wide in substrate application range; the material does not need to be pretreated, and the method is high in operability and high in reproducibility; themethod is gentle in reaction condition, simple to operate and good in environment protection; a single-layer function surface can be generated, and high reaction controllability can be achieved; and the method is a broad spectrum silicon nano material surface functionalization method with great potential.
Owner:DALIAN UNIV OF TECH
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