29 results about "Organic Synthesis Methods" patented technology

The present invention relates to a method for synthesizing a novel primary amide using dioxazolone as a starting material and adding a copper salt catalyst, and more specifically, to a method for producing an environmentally friendly primary amide derivative with a short reaction time, low reaction temperature, and the generation of harmless carbon dioxide as a byproduct. The present invention provides an efficient method that enables the safety of compounds and low-cost synthesis even in large-scale reactions. Furthermore, it suppresses the use of highly corrosive ammonia, which was required in the conventional synthesis of primary amides, while simultaneously providing more environmentally friendly synthesis conditions through a water-added co-solvent system. Furthermore, the organic synthesis method of primary amides according to the present invention can be widely applied to the synthesis of pharmaceutical intermediates, natural products, and low-molecular-weight new drug candidate compounds.

The application relates to a method for synthesizing 1,1-bisaryl compounds by using non-activated alkenes, and belongs to the fields of organic synthesis methods and electrochemical catalysis. The application solves the technical problem that the existing reaction technology cannot realize efficient coupling of non-activated alkenes and halogenated arenes to generate 1,1-bisaryl compound products. In the application, a nickel catalyst is reduced on a cathode by a constant current under an inert gas atmosphere, then a secondary oxidative addition is carried out with another halogenated arene, and finally a 1,1-bisaryl compound product is generated through a reductive elimination step. The nickel catalyst circulates in the reaction by maintaining its valence state under electrochemical conditions, effectively avoiding the use of an additional chemical reducing agent, simplifying the operation and reducing the environmental burden. The reaction system of the application has high efficiency and universality, and can be applied to various halogenated arenes and non-activated alkenes under mild conditions, and has significant application value in the modification and synthesis of natural products and drug molecules.

A low-carbon and environment-friendly method for synthesizing a primary amine from a halogenated hydrocarbon in the technical field of organic synthesis is provided. The method includes adding formaldehyde and ammonia in an alcohol solution at a ratio of 8 mol:8 mol for a full reaction, then adding 3 mol of the halogenated hydrocarbon at a suitable temperature, followed by a full reaction, and performing a series of post-treatment steps to obtain a target primary amine product with relatively high purity.

The invention discloses a 2-azabicyclo [3.1. 1] heptene derivative as well as a synthesis method and application of the 2-azabicyclo [3.1. 1] heptene derivative. The 2-azabicyclo [3.1. 1] heptene derivative provided by the invention is obtained by exciting a rhodium complex by visible light to catalyze bicyclo [1.1. 0] butane to perform cycloaddition reaction. The 2-azabicyclo [3.1. 1] heptene derivative constructed by the method can be applied to the aspects of simulating bioisosteres and the like, is expected to obtain more innovative achievements in the field of organic synthesis methodology, and also can provide a brand new thought and a structural basis for developing novel drug molecules; and the medicine with better curative effect and less side effect can be designed.

The invention relates to a quinoxaline derivative containing trimethyl and n-propyl as well as a preparation method and application of the quinoxaline derivative, and the derivative is 1, 6, 7-trimethyl-3-propyl quinoxaline-2 (1H)-ketone and is particularly suitable for inhibiting fusarium oxysporum. The derivative is prepared by an organic synthesis method which comprises the step of carrying out cyclization reaction on N-protected o-phenylenediamine and a carbonyl compound in the presence of trifluoroacetic acid. Experiments show that the compound has a remarkable antibacterial effect on fusarium oxysporum, and the minimum inhibitory concentration is 0.50 mg / mL. The derivatives can destroy the cell membrane structure of fusarium oxysporum and cause leakage of RNA, protein and reducing sugar in cells, so that the growth of thalli is inhibited. The invention provides a theoretical basis and an experimental basis for developing a novel efficient and low-toxicity bacteriostatic agent.

The invention belongs to the technical field of organic synthesis methodology, and particularly relates to a photoinduced beta-cyano sulfone compound synthesis method based on a triarylamine electron donor acceptor compound and application of the photoinduced beta-cyano sulfone compound. According to the method, a substituted sulfonium salt serves as an electron acceptor, triarylamine serves as an electron donor to form an EDA compound, and under the action of visible light, the EDA compound is synthesized into a beta-cyano sulfone compound based on the triarylamine electron donor acceptor compound. The method comprises the following steps: by taking substituted cyanohydrin as a raw material and 4-diazabicyclo [2.2. 2] octane di (sulfur dioxide) adduct [(DABCO). (SO2) 2] as a sulfur source, adding an organic solvent, reacting in an inert gas at a certain temperature, and realizing a bifunctionalization process of olefin through far-end functional group migration, thereby obtaining the beta-cyano sulfone compound. The method does not need harsh reaction conditions, the reaction can be completed in one step, the reaction conditions are mild, and the method is green and environment-friendly. The beta-cyano sulfone compound and the derivative thereof prepared by the method are expected to be applied to the research and development fields of anti-cancer, antiviral and antibacterial medicines and the like.

The application belongs to the technical field of organic synthesis and relates to an organic synthesis method for benzyl protection of a hydroxyl group. The application provides an organic synthesis method for benzyl protection of a hydroxyl group, which comprises the following steps: dissolving benzyl chloride and KI in DMF, adding NaH, and then adding a DMF solution containing a substrate drop by drop to perform a temperature control reaction. The application provides a new idea for protection of a non-conventional hydroxyl group.

This invention discloses a method for preparing a seawater desalination evaporator based on an organic three-dimensional light-trapping and biomimetic suspension protection mechanism, including a. a synthesis route of small molecule photothermal materials; and b. a preparation process of the seawater desalination evaporator. This method for preparing a seawater desalination evaporator based on an organic three-dimensional light-trapping and biomimetic suspension protection mechanism uses low-cost wood pulp sponge as a matrix. The material is synthesized through a simple one-step organic synthesis method, dissolved in an organic solvent, and drop-coated onto the matrix to prepare a seawater desalination evaporator with a three-dimensional light-trapping and suspension protection mechanism. The evaporator preparation method provided by this invention enables more convenient, lower-cost, and higher-efficiency seawater desalination. The one-step high-yield organic synthesis method reduces the preparation cost of the evaporator.

The invention belongs to the technical field of organic synthetic chemistry, and discloses an efficient synthesis method of an indoline and azepine ketone derivative. The derivative has a structure as shown in a formula (I), and is prepared according to the following steps: reacting 1 equivalent of carboxylic acid, 1 equivalent of o-alkynylaniline, 1 equivalent of pyridine-2-formaldehyde and 1 equivalent of isocyanide as reaction raw materials at room temperature for 5 hours under the condition that methanol is used as a solvent to obtain an intermediate Ugi compound. Then, spin-drying a reaction solvent, adding n-butyl alcohol (1.5 mL), XPhosAuCl (0.01 mmol, 0.05 equivalent) and silver acetate (0.01 mmol, 0.05 equivalent), and transferring a reaction system to a microwave condition of 110 DEG C to react for 1 hour, so as to finally obtain the indoline and azepine ketone derivative as shown in the formula (I). The indoline azepine ketone derivative is efficiently prepared through a one-pot method, the compound is a quasi-natural product compound with a novel structure, and the developed organic synthesis method has the advantages of being high in atom economy, simple in step and the like. Meanwhile, the compound also shows good anti-tumor cell proliferation activity. # imgabs0 #

The application belongs to the technical field of organic synthesis, and discloses a method for preparing n-butyl ether and butyl phenyl ether simultaneously through etherification reaction. Phenol, n-butanol and a phosphoric acid catalyst are mixed, and then etherification reaction is carried out under a protective gas to obtain n-butyl ether and butyl phenyl ether. The method can prepare n-butyl ether and butyl phenyl ether simultaneously, the combined selectivity of n-butyl ether and butyl phenyl ether can reach 98-99%, the reaction has few by-products, the conversion efficiency of raw materials is high, the products obtained by the reaction are important chemical raw materials, and the method has high economic benefits. The preparation method does not need to add strong acid and strong base, the reaction condition is mild, the safety coefficient of the preparation process is high, there is no defect of damage and corrosion to the equipment, and the method belongs to a more green and environmental protection organic synthesis method.

The invention relates to the field of organic synthesis methodology, in particular to a quinazoline dihydroimidazole thione derivative and a preparation method and application thereof.The quinazoline dihydroimidazole thione derivative is prepared by reacting aryl glyoxal, o-aminobenzene amine, aryl isothiocyanate and an additive at a certain temperature under the closed condition and the solvent condition. The method has the characteristics that the catalyst is cheap and easy to obtain, the raw materials are easy to obtain, the operation is simple, the reaction time is short, the yield is relatively high, the functional group compatibility of the substrate is good, a series of quinazoline and dihydroimidazole thione derivatives can be synthesized, and the method has a good potential application value.

The invention relates to the technical field of organic synthesis methodology, in particular to a high-throughput screening method for polypeptide compound peptide bond construction, which comprises the following steps: step 1, using a 24-pore plate as an experimental carrier, constructing 6 * 4 reaction systems according to 6 condensation reagents and 4 solvents, the solvent corresponds to the solvent of the solution A and the solvent of the solution B; 2, adding the solution A containing the carboxyl substrate, a condensation reagent and organic alkali into the reaction container, and reacting at 10-40 DEG C for 0.5-4 hours; and 3, adding a solution B containing an amino substrate into the reaction container, and carrying out a stirring reaction at 0-100 DEG C for 10-30 h to obtain the polypeptide compound as shown in the formula I. According to the method, the application of a high-throughput screening method in the field of organic chemistry is enriched, the optimal reaction reagent for constructing the peptide bond of the target compound can be quickly determined in a short time, and the efficiency and purity of synthesizing the peptide bond are greatly improved.

The present invention relates to a substrate for solid-phase organic synthesis and a solid-phase organic synthesis method using the same. More specifically, the present invention relates to a substrate having a larger reactive surface area compared to conventional solid-phase resins, thereby improving the efficiency of solid-phase organic synthesis reactions, and also being applicable to continuous organic synthesis via a roll-to-roll process.

The invention belongs to the technical field of organic synthesis methodology, and particularly relates to a visible light promoted aliphatic primary amine compound synthesis method and application, the method uses substituted sulfonium salt and substituted styrene as raw materials, ammonium thiocyanate as an amine source, alkali as an additive, an organic solvent is added, reaction is carried out in inert gas at a certain temperature, and the visible light promoted aliphatic primary amine compound is obtained. Under visible light, under the catalytic action of a metal copper complex, the aliphatic primary amine compound is prepared. The method is mild in reaction condition, safe, green and environment-friendly, can be completed in one step, and accords with atom economy and step economy. The aliphatic amine compound and the derivative thereof prepared by the method are expected to serve as lead compounds to be applied to the research and development fields of anti-tumor and antibacterial drugs and the like.

The invention discloses a preparation method of a steroid compound 4, 5-position epoxy compound, and relates to the technical field of organic matter synthesis methods, 17beta-hydroxy-2, 4-ene-androstane [2, 3-d] isoxazole, a medium polar solvent, hydrogen peroxide and an anhydride reagent are used as raw materials for reaction, then alcohol recrystallization is carried out, and the compound 4, 5-position epoxy compound is obtained. Finally, a target product, namely the 4 alpha, 5 alpha-epoxy-17 beta-hydroxyl-2-ene-androstane [2, 3-d] isoxazole, is obtained. The medium polar solvent comprises dichloromethane and chloroform; the anhydride reagents are acetic anhydride and acetic acid. The preparation method provided by the invention has the advantages of short process reaction time and few byproducts, is favorable for improving the purity of the product, and has important guiding significance for the synthesis of subsequent derivative products.

The invention belongs to the field of nano material preparation, and particularly relates to a two-dimensional conductive metal phthalocyanine organic framework nanosheet as well as a preparation method and application thereof. An organic ligand 2, 3, 9, 10, 16, 17, 23, 24-octahydroxy metal phthalocyanine containing a metal phthalocyanine unit is synthesized by adopting an organic synthesis method, and a two-dimensional metal phthalocyanine-organic framework is further synthesized by utilizing a solvothermal reaction of the ligand and a metal salt of acetylacetone. Stripping the two-dimensional metal phthalocyanine organic framework by adopting a ball milling method to obtain a two-dimensional metal phthalocyanine organic framework nanosheet; the two-dimensional metal phthalocyanine organic framework nanosheet is used for modifying a substrate electrode to obtain the electrode modified by the two-dimensional metal phthalocyanine organic framework nanosheet, and the electrode is used for constructing an electrochemical sensor for detecting dopamine, uric acid, 5-hydroxytryptamine and ascorbic acid and has an extremely low detection limit. By improving the conductivity of the organic framework material and increasing active sites, the sensitivity and resolution of electrochemical detection are improved.

The invention belongs to the technical field of organic synthesis methodology, and particularly relates to a method for synthesizing allene nitrile compounds based on a visible light / metal copper dual-catalysis strategy and application of the allene nitrile compounds. According to the method, substituted sulfonium salt and substituted enyne are used as raw materials, trimethylsilyl cyanide is used as a cyano source, alkali is used as an additive, and an organic solvent is added; and reacting in inert gas at a certain temperature, and preparing the allene nitrile compound under the dual catalytic action of the photocatalyst and the metal copper / ligand catalyst. The method does not need harsh reaction conditions, the reaction can be completed in one step, the reaction conditions are mild, and the method is green and environment-friendly. The allene nitrile compound and the derivative thereof prepared by the method are expected to serve as lead compounds to be applied to the research and development fields of anti-cancer, antiviral and antibacterial drugs and the like.

The application discloses a kind of di (propyl-2-alkenyl) furan-2, 5-dicarboxylic acid ester and preparation method thereof, it is related to biomass-based organic synthesis method technical field.The method with 2, 5-furan dicarboxylic acid as base material, by esterification reaction under the action of inorganic metal catalyst, will be grafted in 2, 5-furan dicarboxylic acid on allyl, obtains di (propyl-2-alkenyl) furan-2, 5-dicarboxylic acid ester.Compared with traditional synthesis method, the required reaction condition is relatively mild, without high temperature and high pressure environment, not only reduce energy consumption, also reduce operating risk and equipment cost.Mild reaction condition is also more conducive to keeping the activity and selectivity of catalyst, improves reaction efficiency.The obtained product is high in purity, without complex post-processing step can be directly used in subsequent application or further chemical conversion, improves overall production efficiency.The application provides a new idea for 2, 5-furan dicarboxylic acid and other biomass materials to realize high value-added utilization.

The application discloses an environment-friendly synthesis method of 28-homobrassinolide, wherein (2,22)-diene-24S-ethyl-5alpha-cholesta-6-ketone P1 is used as a starting material, double bonds on a ring of P1 are simultaneously epoxidized, namely, double epoxidation, ring opening, acetylation, one-time hydrolysis and two-time hydrolysis are carried out to obtain a tetrahydroxy compound, and finally, lactonization is carried out to obtain the target 28-homobrassinolide. The 28-homobrassinolide is synthesized by a brand-new organic synthesis method, which is energy-saving, efficient, environment-friendly, simple in process and good in industrial application value.

The invention discloses a device and a method for chemical organic wastewater treatment and carbon dioxide synergistic conversion. The device comprises an advanced oxidation reaction tank, a gas purification and collection system and a carbon dioxide conversion system which are connected in sequence, the advanced oxidation reaction tank is used for degrading organic matters in the chemical organic wastewater to generate carbon dioxide; the gas purification and collection system is used for removing impurities in the carbon dioxide gas and collecting purified carbon dioxide; the carbon dioxide conversion system converts carbon dioxide through an organic synthesis method. Aiming at the problem that a large amount of carbon dioxide is directly or indirectly discharged in the traditional chemical organic wastewater treatment process, the invention provides a method for degrading and mineralizing organic matters through advanced oxidation, and converting the generated carbon dioxide into chemicals with high added value through an organic chemical synthesis method, so that the synchronous pollution reduction and carbon reduction are realized.

The present invention discloses a method for synthesizing γ-carbolinone compounds, comprising the following steps: in the presence of a cobalt catalyst, an oxidant and a base, a 3-indolecarboxamide compound and an alkyne are reacted in a solvent, and after the reaction is completed, the γ-carbolinone compound is obtained through post-treatment. This method uses inexpensive metals cobalt and manganese as a catalytic system, does not require additional ligands and indole nitrogen protecting groups, and provides an organic synthesis method for synthesizing γ-carbolinone compounds with wide application value.

A method for synthesizing a pimozide intermediate, the present invention relates to the field of organic synthesis and electrochemical catalysis. The present invention solves the technical problem of efficiently coupling non-activated olefins with halogenated aromatics to generate 4,4,-bis(4-fluorobenzene)chlorobutane in the prior art. The present invention utilizes electrochemical catalysis means, and under an inert gas atmosphere, a nickel catalyst is reduced by a constant current, an oxidative addition reaction occurs with the halogenated aromatics, and then added to the non-activated olefin, a nickel migration reaction occurs, and an aromatic-displaced nickel compound intermediate is formed. The present invention greatly reduces the synthesis steps, improves the efficiency and selectivity of the reaction, and especially when synthesizing the pimozide intermediate, can significantly reduce production costs and reaction time, showing stronger industrial application potential. The pimozide intermediate prepared by the present invention is used to treat the field of chronic mental disorders.

The present application relates to the field of organic synthesis methodology, in particular to a kind of iron-mediated preparation method of hydrogenation alkylation of azauracil under light condition.The method first applies ligand-metal charge transfer (LMCT) mechanism to the hydrogenation alkylation reaction of uracil, uses cheap and easily available abundance metal iron as catalyst, uses alkane as alkylation raw material without pre-functionalization, reaction condition is mild, functional group tolerance is good, product yield can reach 75%~94%, suitable for late modification of drug molecules and bioactive molecules.

The present application relates to the technical field of organic synthesis, and particularly relates to a method for preparing 2-methylbenzoisothiazolin-3-ketone at room temperature by NCS participation. In the prior art, 2-methylbenzoisothiazolin-3-ketone is obtained by an organic synthesis method, the reaction condition is relatively harsh, the steps are relatively complicated, and the production efficiency is low. In view of the above technical problems, the present application provides a method for preparing 2-methylbenzoisothiazolin-3-ketone at room temperature by N-chlorosuccinimide (NCS) participation. NCS is used as a key additive, and 2-methylbenzoisothiazolin-3-ketone is successfully prepared by reacting 2-methylbenzoisothiazolin-3-ketone with 2-methylbenzoisothiazolin-3-ketone in a solvent at room temperature under the condition of severe stirring. The synthesis method of the present application is more efficient, the reaction condition is more mild, and has a good application prospect.

The present invention provides a method for the C-H nucleophilic substitution reaction of the bisanthene aromatic ring bay area and its application, belonging to the field of organic synthesis methodology. This reaction uses bisanthene as the raw material, dichloromethane and acetonitrile as solvents, and is subjected to nitrosylation with hexafluorotellurous acid, and reacts with nucleophilic reagents such as carbanions, oxygen-containing, sulfur-containing, chlorine-containing, nitrogen-containing, phosphorus-containing and cyano groups in one step to synthesize a series of functionalized products modified in the bisanthene bay area; when this reaction method is further applied to the nucleophilic substitution reactions of perylene and N,N'-bis(1,3-diisopropylbenzene)-3,4,9,10-perylene diimide (PDI), it shows good generality. The reaction of the present invention has mild reaction conditions, does not require the introduction of a transition metal as a catalyst, the product is easy to separate and purify, and has the advantages of low cost, high efficiency and greenness; the series of functionalized derivatives constructed by this method can provide important intermediates for the synthesis of larger polycyclic aromatic hydrocarbon molecules in the system; this method has good industrial production prospects.

This invention discloses an asymmetric method for synthesizing fluorine-containing chiral quaternary carbon compounds, relating to the field of organic synthesis techniques. The method includes: using a carboxylic acid compound of Formula 1 and isopropanol as starting materials, and under the action of a catalyst, activating reagent, and base, with a fluorinated reagent as the fluorine source, reacting in an organic solvent to obtain an α-fluoro-α-substituted isopropyl carboxylate as shown in Formula 2. Using a carboxylic acid compound and isopropanol as starting materials, and under the action of a specific catalyst, activating reagent, and base, with a fluorinated reagent as the fluorine source, a specific reaction route is used to achieve highly enantioselective construction of α-fluoro-α-substituted carboxylic acid ester structures. This method has advantages such as mild reaction conditions, simple operation steps, and a wide range of applicable substrates, providing a new and effective approach for enriching the methods for constructing fluorine-containing chiral quaternary carbon compounds.

The invention provides a novel organic synthesis method which comprises the following steps: taking methanol as a solvent under electric assistance, enabling halide salt and alkali to participate in electrode reaction, and performing selective hydrogenation reduction on various alpha-ketoamide substrates a under electrochemistry to obtain a series of alpha-hydroxyamide products b. The method has the following advantages of adopting an electrolytic reaction strategy, being free of metal catalysis, using a solvent as a hydrogen source, and having green synthetic chemical characteristics of selective reduction and the like.

The application discloses an electrochemical organic synthesis method of benzyl alcohol fluorination product using sulfur hexafluoride as a fluorination reagent, comprising the following steps: uniformly mixing benzyl alcohol, an electrolyte, a solvent and an alkali, introducing sulfur hexafluoride, performing an electrolysis reaction in a sulfur hexafluoride gas atmosphere with zinc as an anode and tin as a cathode, and obtaining the benzyl alcohol fluorination product after post-treatment; wherein the benzyl alcohol is a mixture of one or more of diphenyl carbinol, (2-chlorophenyl)-benzyl alcohol, (3,4-dichlorophenyl)-benzyl alcohol, 3-(trifluoromethyl)diphenyl carbinol, (4-cyanophenyl)benzyl alcohol, 1,3-diphenyl-1-propanol and 1-(4-fluorophenyl)-3-phenyl-1-propanol. The application provides a novel benzyl alcohol dehydroxylation fluorination conversion method which is safe, inexpensive, mild and good in substrate compatibility, and solves the problems of excessively high reagent activity, harsh reaction conditions, dangerous operation and excessively high cost in the existing benzyl alcohol dehydroxylation fluorination method.

The invention relates to a cyclohexyl-containing quinoxaline derivative as well as a preparation method and application thereof, and the cyclohexyl-containing quinoxaline derivative is 3-cyclohexyl-1-methylquinoxaline-2 (1H)-ketone and is particularly suitable for inhibiting fusarium oxysporum. The derivative is prepared by an organic synthesis method which comprises the step of carrying out cyclization reaction on N-protected o-phenylenediamine and a carbonyl compound in the presence of trifluoroacetic acid. Experiments show that the compound has a remarkable antibacterial effect on fusarium oxysporum, and the minimum inhibitory concentration is 0.50 mg / mL. The derivatives can destroy the cell membrane structure of fusarium oxysporum and cause leakage of RNA, protein and reducing sugar in cells, so that the growth of thalli is inhibited. The invention provides a theoretical basis and an experimental basis for developing a novel efficient and low-toxicity bacteriostatic agent.