15results about How to "Good substrate universality" patented technology

The invention discloses a preparation method of alpha-aminoketone compounds, which is characterized in that in the presence of water as a reaction solvent and inorganic base, iodine as an accelerant, propiophenone compounds and amine compounds are subjected to sp3 C-H amination reaction to prepare a series of alpha-aminoketone compounds at high yield. Compared with the prior art, the method has the advantages that the use of an organic solvent and organic alkali is avoided, the production cost and the operation difficulty are remarkably reduced, and meanwhile, the atom economy and the production safety of the preparation process are also remarkably improved. The method disclosed by the invention has good substrate universality, can be carried out at room temperature, is simple in preparation and post-treatment operation and pollution-free, conforms to the green chemical development concept, and is suitable for industrial production.

The invention discloses a pyrazolo [5, 1-a] isoindole derivative as well as a synthesis method and application thereof, and belongs to the technical field of organic chemical synthesis. The invention solves the problems of harsh reaction conditions, limited substrate range and the like of continuous multi-step synthesis of a precursor in the existing pyrazolo [5, 1-a] isoindole compound synthesis process. According to the invention, a polarity reversal strategy is adopted, a cyano group is introduced into 1, 5-enyne to change the electronic characteristics of 1, 5-enyne, diazo, olefin and ethynyl benzene are reacted under mild conditions, two rings and three new chemical bonds are constructed through a series of intermolecular [3 + 2] cycloaddition, intramolecular cycloaddition and elimination reactions, and pyrazolo [5, 5-a]-1, 5-a-phenanthrene is efficiently synthesized. According to the present invention, the 1, 1-a] isoindole derivative has characteristics of good synthesis yield, simple operation of the synthesis method, easily available raw materials, good substrate universality and step economy, and provides the effective strategy for the drug design synthesis.

The invention belongs to the technical field of compound synthesis, and particularly relates to a one-step synthesis method of a phenanthrene cyclic aromatic hydrocarbon derivative, which comprises the following steps of: reacting 2-iodobiphenyl shown in a general formula (1) and alkyne shown in a general formula (2) in the presence of a transition metal Pd catalyst, a ligand, an alkaline substance and a solvent in a nitrogen atmosphere under the irradiation of visible light with the wavelength of 420-500nm to obtain the phenanthrene cyclic aromatic hydrocarbon derivative. The phenanthrene ring compound is generated. According to the reaction, aryl free radicals are generated through single electron transfer and then are subjected to free radical addition with alkyne, and then cyclization is carried out. A series of complex phenanthrene ring derivatives are synthesized under mild conditions. The reaction mode of the method for synthesizing the phenanthrene ring derivative is extremely rare.

The invention provides a chiral phosphonate compound, which belongs to the technical field of organic synthesis and pesticide bacteriostatic activity research, and the structural general formula of the chiral phosphonate compound is as shown in formula 1. The compound has remarkable sterilization performance, and has important research significance on further development and utilization of chiral phosphonate compounds. The invention also provides an application of the chiral phosphonate compound as an agricultural bacteriostatic agent or in preparation of the agricultural bacteriostatic agent.

The invention relates to the technical field of organic synthesis, in particular to a novel alpha-fluoroalkyl substituted fatty alcohol compound as well as a preparation method and application thereof, the molecular structural formula of the novel alpha-fluoroalkyl substituted fatty alcohol compound is as follows: # imgabs0, and the fluoroalkyl alcohol compound can also be used for synthesizing a medicine FFA4 for treating diabetes, a medicine Apo7033 for treating nephropathy and the like. The preparation method provided by the invention realizes free radical three-component reaction in which alpha-fluoroalkyl-alpha-silyl methanol, olefin and a nucleophilic reagent participate, is a new reaction mode, provides a simple and efficient method for synthesizing fluoroalkyl alcohol and fluoroalkyl silyl ether, and in addition, the method can be used for synthesizing fluoroalkyl alcohol by a one-pot method through simple desilicication treatment. The preparation method is simple in reaction condition, efficient and mild. The method has good functional group tolerance and substrate universality, and shows complementarity of a single-electron reaction and a double-electron reaction.

The invention discloses a method for synthesizing a methylated aza-uracil derivative, which comprises the following steps: adding an aza-uracil derivative into a glass reaction container, and stirring to react under the irradiation of a 10W blue lamp with the wavelength of 455 nm by taking DMSO as a methyl source and a solvent, taking fluorescein as a photocatalyst and taking DABCO as alkali. And separating and purifying the crude product by column chromatography to obtain the 6-methyl aza-uracil derivative. According to the invention, fluorescein which is cheap and easy to obtain is used as a photocatalyst, and a metal catalyst and a strong oxidant are not needed. In addition, the reaction conditions are mild, and excellent functional group tolerance is achieved.

The invention discloses a method for synthesizing methylated products of nitrogen heterocyclic and oxygen heterocyclic compounds, which comprises the following synthesis processes: firstly, placing a target heterocyclic compound in a glass reaction container, then adding dimethyl sulfoxide (DMSO) as a methyl donor and a solvent, adopting fluorescein as a photocatalyst, adding 1, 2, 4-trimethyl-1, 3, 4-trimethyl-1, 3, 4-trimethyl-1, 3, 4-trimethyl-1, 3, 4-trimethyl-1, 3, 4-trimethyl-1, 3, 4-trimethyl-1, 3, 4 2, 4-diazabicyclo [2.2. 2] octane (DABCO) is used as an alkaline additive. Under the condition of room temperature, a blue light source with the power being 10 watts and the wavelength being 455 nanometers is used for carrying out illumination stirring reaction. And after the reaction is completed, purifying through a column chromatography separation technology to finally obtain the methyl-substituted nitrogen heterocyclic or oxygen heterocyclic compound. The unique photocatalytic system disclosed by the invention can efficiently realize methylation reaction of nitrogen heterocyclic ring and oxygen heterocyclic ring without depending on a metal catalyst or a strong oxidant, and excellent yield and good functional group compatibility are obtained.

The invention discloses a synthesis method of an aryl phosphine compound as shown in a formula IV, which comprises the following steps: under the irradiation of blue light, reacting a compound as shown in a formula I with a compound as shown in a formula II in an inert atmosphere in an organic solvent in the presence of organic alkali, and then adding S8 to continuously react to obtain the aryl phosphine compound as shown in the formula IV, ar represents a substituted or unsubstituted aryl group, X represents a trifluoromethanesulfonate ion, a hexafluorophosphate ion or a tetrafluoroborate ion, and R1 and R2 each independently represent a substituted or unsubstituted alkyl group, cycloalkyl group or aryl group; and the organic base is selected from any one of N-methyl dicyclohexylamine, triethylamine, tetramethylethylenediamine and N, N-diisopropylethylamine.

The application discloses a kind of solid supported copper-based N-heterocyclic carbene catalytic materials and preparation method and application thereof, and it is related to material synthesis technical field.The preparation method of the catalytic material includes: cuprous oxide is reacted with N-heterocyclic carbene ligand containing bromine group in solvent, and copper-based N-heterocyclic carbene complex is formed;The complex is subjected to Sonogashira coupling reaction with alkyne compound under the action of catalyst, and bromine group on the complex is coupled with alkyne compound and occurs copolymerization, forms porous organic polymer skeleton, and copper-based N-heterocyclic carbene complex is distributed in the skeleton, and solid supported copper-based catalytic material is obtained;Wherein alkyne compound is selected from 1,3,5-triethynylbenzene or 1,3,5-tri (4-ethynylphenyl) benzene.The obtained catalytic material has porous organic polymer skeleton, and copper active species is uniformly distributed in the whole material, belongs to heterogeneous catalytic material, is easy to separate and recycle, can be recycled, and shows excellent catalytic performance in alkyne alkylation reaction of trifluoromethyl ketone.

The invention discloses a method for catalytic cracking of a beta-O-4 type lignin model compound by visible light, which comprises the following steps: in an inert atmosphere, mixing a photosensitizer, a beta-O-4 type lignin model compound as shown in a formula I, protonic acid, amine and a solvent, reacting for 6-48 hours under the conditions of visible light irradiation and 25-45 DEG C, and post-treating the reaction liquid to obtain the beta-O-4 type lignin model compound. Respectively obtaining an aromatic ketone compound as shown in a formula II and a phenolic compound as shown in a formula III; the method is mild, efficient, green, economical and suitable for large-scale production; # imgabs0 #

The invention provides a chiral phosphoramide compound, which belongs to the technical field of organic synthesis technology and pesticide bacteriostatic activity research, and the structural general formula of the chiral phosphoramide compound is as shown in formula 1. The chiral phosphoramide compound has remarkable sterilization performance and has remarkable bacteriostatic activity on rice bacterial blight germs and rice leaf streak germs, and the chiral phosphoramide compound has important significance on further development and utilization of the chiral phosphoramide compound. The invention also provides an application of the chiral phosphoramide compound as an agricultural bacteriostatic agent or in preparation of the agricultural bacteriostatic agent.

The application discloses a method for selectively synthesizing 2-amido quinoline-N-oxide compounds from quinoline-N-oxide compounds, which uses copper hexafluorophosphate tetraacetonitrile and silver acetate as catalysts and isoxazolidinone as nitrogen source, does not need to add expensive ligands, and can obtain the product under mild conditions. The application has the advantages of low cost, mild reaction condition, high selectivity and the like, and avoids the use of noble metals such as rhodium, iridium and palladium. The method is suitable for different substituted quinoline-N-oxide compounds and other polysubstituted isoxazolidinone substrates.

This invention discloses a method for preparing aryl carboxylic acids by reacting aryl thioonium salts with carbon dioxide using a copper compound as a catalyst and diethylzinc as a reducing agent. The aryl thioonium salt substrate is reacted with an organic solvent at room temperature under a carbon dioxide atmosphere at one atmosphere. The product is then acidified and purified to obtain the aryl carboxylic acid. This method uses readily available raw materials, is simple to operate, operates under mild conditions, and exhibits good functional group tolerance and substrate versatility. This method can not only synthesize various simply substituted aryl carboxylic acids but can also be used for the late-stage carboxylation modification of complex drug molecules. The practicality of this method has also been verified on a gram-scale, demonstrating promising prospects for industrial application.

The invention relates to a synthesis method of an alpha-aryl cyclohexanone compound, and belongs to the technical field of photocatalytic organic synthesis, and the synthesis method comprises the following steps: taking aryl diazonium tetrafluoroborate and cyclohexene as raw materials, adding an additive, in the presence of a mixed solvent, under the irradiation of visible light and in the presence of a quantum dot catalyst, carrying out a reaction to obtain the alpha-aryl cyclohexanone compound. Reacting to obtain alpha-aryl cyclohexanone; the invention provides a brand-new synthesis route of the aryl cyclohexanone compound, the cheap aryl diazonium salt and cyclohexene are adopted as raw materials, the alpha-aryl cyclohexanone compound is synthesized through photocatalysis under mild reaction conditions, and the dependence on a noble metal catalyst and harsh reaction conditions in a traditional method is avoided.

The application discloses a method for preparing difluoromethyl compounds by using a photocatalytic LMCT strategy and belongs to the technical field of catalytic synthesis, in particular to a method for preparing difluoromethyl compounds by using a photocatalytic LMCT strategy. The application solves the problems of the existing synthesis method, such as being too complicated, needing pre-activation and a stoichiometric oxidant. The method comprises the following steps: adding olefin compounds, difluoroacetic acid, 2,4,6-triisopropylbenzenethiol and Fe(acac)3 into a solvent to obtain a reaction mixed solution, irradiating the reaction mixed solution by using an LED light source under room temperature and in an inert gas atmosphere, and obtaining difluoromethyl compounds. The application embodies the green reaction and the mild reaction. The method is very simple to operate, various raw materials are commercially available, olefins are easy to prepare, and the reaction can be efficiently realized by using a catalytic amount of a cheap metal catalyst through a one-pot method, so that the method has potential industrial application value. The application can be applied to the field of organic synthesis.