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78results about How to "The synthesis method is scientific and reasonable" patented technology

Method for preparing isoxazolo-isoquinolinone derivative under electro-catalysis

The invention belongs to the technical field of organic synthesis, and discloses a method for preparing an isoxazolo-isoquinolinone derivative under electro-catalysis. The method comprises the following steps of adding a substituted N-alkoxy benzamide substance and tetra-n-butyl ammonium hexafluorophosphate with a molar ratio of 1 : 1 into a reactor, adding 95% ethanol as a solvent, and promotinga reaction to be carried out through the electro-catalysis strategy; and after the reaction is finished, carrying out concentration by a rotary evaporator to obtain a crude product, and carrying out silica gel column chromatography separation to obtain a target product. The synthesis method of the polysubstituted isoxazolo-isoquinolinone derivative has the characteristics of scientificity and reasonability, environment-friendly synthesis way and no metal catalyst; the reaction solvent is the 95% ethanol, and replaces a toxic solvent; a substrate can react under a weak current; the synthesis method is simple and rapid in reaction; and the yield of a target compound is high, and the derivative is easy to purify. A reaction equation is as shown in the description.
Owner:QINGDAO UNIV OF SCI & TECH

Compound as well as synthesis thereof and method for synthesizing double-UPy substituted compound by using same

The invention discloses a compound which is 2[2-(1-ethanethiol)] urea-4 [1H]-pyrimidone. The invention also discloses a synthesis method of the compound, which comprises the steps: enabling cystamine dihydrochloride to react with activated ureido pyrimidine S1 to obtain a 2-urea-4[1H]-pyrimidine disubstituted sulfur-sulfur compound S2; and reducing the sulfur-sulfur compound S2 by using DTT (Dithiothreitol) to obtain the compound. The invention also discloses a method for synthesizing a double-UPy substituted compound by using the compound disclosed by the invention. According to the method, the compound has a free radical thiol-alkynyl click chemical reaction with an alkane alkynyl-terminated compound CHR to obtain the double-UPy substituted compound. According to the method disclosed by the invention, the thiol-alkynyl click chemical reaction is utilized to synthesize the double-UPy substituted compound for the first time; raw materials are easy to obtain, the application range is wide, the separation yield is high, and the synthesis method is scientific and reasonable; therefore a general method is provided for synthesizing the double-UPy substituted compound.
Owner:TECHNICAL INST OF PHYSICS & CHEMISTRY - CHINESE ACAD OF SCI

Synthesis method of polysubstituted silole derivative

The invention provides a synthesis method of a polysubstituted silole derivative. The polysubstituted silole derivative is prepared by reacting a 2-(trimethylsilyl)aryl trifluoromethane sulfonate derivative with alkyne in the presence of a catalyst. The synthesis method is pretty high in yield rate, scientific, reasonable, accessible in raw materials, wide in application range, high in separation yield rate, simple in experiment equipment, simple and easy in operation implementation, and conductive to further development and application.
Owner:INST OF CHEM CHINESE ACAD OF SCI +1

Preparation method of 2-benzofuranone compound

The invention discloses a preparation method of a 3-benzofuranone compound and belongs to the technical field of organic synthesis. The method comprises the steps of adding a phenol derivative (0.2mmol, 30mg), phenylpropiolic acid (0.2mmol, 29mg), a 5% rhodium catalyst, a cobalt acetate hydrate, a sodium trimethylacetate hydrate, and 1.0mL methanol into a 15mL thick-wall pressure pipe, stirring for 12h at a room temperature with an orifice being opened, and after a reaction, performing silicagel column chromatographic separation to form a pure target product. The preparation method of the 3-benzofuranone compound has the characteristics that the method is scientific, reasonable, mild in condition, simple to operate, short in reaction time and the like. A reaction equation of the method isas follows as shown in the specification.
Owner:郯城县经开区医药发展有限公司

Preparation method of polysubstituted thiapyran diindyl derivative

The invention discloses a preparation method of a polysubstituted thiapyran diindyl derivative, which belongs to the technical field of pharmaceutical synthesis and photoelectric material synthesis. The method comprises the steps of adding diaryl hypervalent iodonium salts, o-alkynyl isothiocyanate, potassium carbonate and copper salt into a reactor, pumping and injecting nitrogen for three times, adding a solvent, and heating until a reaction is over; adding water or a salt solution for a quenching reaction after cooling a system, performing extraction by using ethyl acetate separately for three times, combining organic phases, adding magnesium sulfate for drying, filtering, concentrating filtrate by a rotary evaporator to obtain a crude product, and performing column chromatography isolation by using an eluent to obtain a product. The preparation method of the polysubstituted thiapyran diindyl derivative, provided by the invention, is scientific and reasonable, and higher in yield, and the product is easy to purify.
Owner:QINGDAO UNIV OF SCI & TECH

Method for preparing multi-substituted benzo-[4,5]imidazo-[1,2-b] pyrazole derivative

The invention belongs to the technical field of organic synthesis and discloses a method for preparing a multi-substituted benzo-[4,5]imidazo-[1,2-b] pyrazole derivative. The method comprises the steps of adding N-(2-bromoaryl)-5-aryl-1H-pyrazole-3-amine compounds, caesium carbonate, catalyst cuprous iodide and ligand 3-(imidazolidine-2-subunit)pentane-2,4-diketone and solvent dimethylsulfoxide (DMSO) into a reactor, performing heating until the reaction is over, cooling a system to room temperature, adding water, using ethyl acetate to perform extraction three times, combining organic phases, adding anhydrous magnesium sulfate to perform drying and filtration, using a rotary evaporator to concentrate filtrate to obtain a crude product, and performing separation through silica gel column chromatography to obtain a product. The method for preparing the multi-substituted benzo-[4,5]imidazo-[1,2-b] pyrazole derivative has the advantages that the method is scientific and reasonable, the reaction is quick, a synthetic method is simple, the yield is high, and the product is easy to purify. The reaction equation is as follows: .
Owner:QINGDAO UNIV OF SCI & TECH

Polysubstituted thienoindole derivative and preparation method thereof

The invention discloses a method for preparing a polysubstituted thienoindole derivative, and the method belongs to the technical field of organic synthesis. The method comprises the following steps: adding ortho-alkynyl isothiocyanate and isonitrile into a reactor; under the catalysis of nickel, heating an obtained mixture in a solvent, cooling an obtained reaction product to a room temperature after completing the reaction, extracting a system by ethyl acetate, then concentrating a filtrate by a rotary evaporator to obtain a crude product, and finally separating the crude product by a column chromatography to obtain a product. The method for preparing the polysubstituted thienoindole derivative, which is provided by the invention, is scientific and reasonable, the productivity is relatively high and the product is purified easily.
Owner:QINGDAO UNIV OF SCI & TECH

Preparation method for polysubstituted isoquinoline derivative

The invention discloses a preparation method for a polysubstituted isoquinoline derivative and belongs to the technical field of organic synthesis. The method includes the steps that isothiocyanate and diaryl high-price iodate are added into a reactor, heating is conducted in a solvent under copper catalysis, the material is cooled to room temperature after the reaction is completed, the system is extracted with ethyl acetate, filtrate is concentrated with a rotary evaporator, a crude product is obtained, and finally the product is obtained after column chromatography isolation. The synthesis method is easy to operate, the raw materials are easy to prepare, multiple substituent groups can be introduced at the same time, the product is easy to purify and separate, the yield is high, and the method is suitable for synthesizing the polysubstituted isoquinoline derivative. The reaction equation in the method is shown in the description.
Owner:QINGDAO UNIV OF SCI & TECH

Preparation method of 6-phosphoryl substituted phenanthridine derivative

The invention discloses a preparation method of a 6-phosphoryl substituted phenanthridine derivative, and belongs to the technical field of organic synthesis. The method comprises the steps that biphenyl isothiocyanate and diaryl oxygen and phosphorus are added into a reactor, by being catalyzed by manganese, heating is conducted in a solvent, after a reaction is completed, cooling is conducted to reach room temperature, a system is diluted with ethyl acetate and washed with saturated sodium chloride, an organic phase is combined, a filtrate is concentrated through a rotary evaporator, a coarse product is obtained, and finally a product is obtained through column chromatography separation. The synthetic method is easy to implement, raw materials are easy to prepare, multiple substituent groups are introduced simultaneously, the product is easy to purify and separate, the yield is high, and the method is suitable for synthesizing the 6-phosphoryl substituted phenanthridine derivative. The reaction equation of the derivative is defined in the description.
Owner:蚌埠弘景科技有限公司

Preparation method of isoxazole and isoquinoline ketone derivative

The invention discloses a preparation method of a polysubstituted isoxazole and isoquinoline ketone derivative and belongs to the technical field of inorganic synthesis. The preparation method comprises the steps that substituted N-alkyl benzamide and iodobenzene diacetate are added into a reactor, after stirring reaction is completed in a solvent, filtrate is concentrated by using a rotary evaporator, thus a coarse product is obtained, the coarse product is subjected to chromatographic separation through a silica gel column, and thus a target compound is obtained. The synthesis method of thepolysubstituted isoxazole and isoquinoline ketone derivative has the characteristics that the synthesis method is scientific, reasonable and simple, the yield of the target compound is high, a productis easy to purify, reaction is fast, and the reaction temperature is the room temperature. A reaction equation of the polysubstituted isoxazole and isoquinoline ketone derivative is shown as the formula (please see the specifications for the formula).
Owner:QINGDAO UNIV OF SCI & TECH

Synthesis method for multi-substituted 2-imidoimidazoline-4,5-diketone

The invention discloses a synthesis method for multi-substituted 2-imidoimidazoline-4,5-diketone. The method comprises the following steps of: firstly reacting substituted carbodiimide and oxalyl chloride in an ether solvent; and then adding organic base of primary amine and non-primary amine to continuously react to produce the multi-substituted 2-imidoimidazoline-4,5-diketone. The method has is a universal method for synthesizing a multi-substitutent 2-imidoimidazoline-4,5-diketone derivative, has the advantages of high yield, readily available raw materials, easiness in operation, high separation yield and convenience in further development and application.
Owner:PEKING UNIV

Preparation method of thiocyano-containing thiazoline compound

The invention discloses a preparation method of a thiocyano-containing thiazoline compound, and belongs to the technical field of organic synthesis. The method comprises the following steps: adding thioamide, ammonium thiocyanate and a solvent into a reactor, performing reacting under the action of electrification, and after the reaction is finished, performing separating by silica gel column chromatography to obtain a pure target product. The preparation method of the thiocyano-containing thiazoline compound provided by the invention has the characteristics of scientificity, reasonability, mild conditions, simplicity in operation, short reaction time and the like. The reaction equation is shown in the specification.
Owner:QINGDAO UNIV OF SCI & TECH

1, 3-thiazole derivative

The invention provides a 1, 3-thiazole derivative and a synthesis method thereof. A 2-acylamino thiazole derivative is prepared from carbodiimide, acyl chloride, a terminal alkyne compound and elemental sulfur. The yield is higher, and the synthesis method is scientific and reasonable, so that a universal method for synthesizing the 2-acylamino thiazole derivative with various substituent groups is provided. The method has the advantages that the raw materials are easily available, and the application range is large, the separating rate is high, experimental devices and operations are simple and easy to operate; therefore, the 1, 3-thiazole derivative can be further developed and used.
Owner:PEKING UNIV

Process for preparing polysubstituted silole

The invention provides a general method for synthesizing silole derivate with a plurality of substituents. The general method comprises the following steps that: firstly, 1-trialkylated silicone base-1, 4-dihalo-1 and 3-butadiene derivate are reacted with lithium alkyl in ether solvent at a low temperature; secondly, quaternary amine or acylammonia ligand is added and the mixture is heated up to continue the reaction; thirdly, the mixture is cooled down and electrophilic reagent E+ is added; finally, polysubstituted silole derivate is obtained through the post treatment and the purification of reaction liquid. The method, being scientific and reasonable, has easily obtained raw material, wide application range, high separation yield and simple experimental equipment and operation, and is convenient for further development and application.
Owner:PEKING UNIV

Preparation method of benzyl isothiocyanate compound

The invention discloses a preparation method of a benzyl isothiocyanate compound, and belongs to the technical field of organic synthesis. The method comprises the following steps: adding benzyl benzene, trimethylsilyl isothiocyanate, an electrolyte and a solvent into a reactor, reacting under the action of constant current, and after the reaction is finished, separating by silica gel column chromatography to obtain the pure target product. The preparation method of the benzyl isothiocyanate compound provided by the invention has the characteristics of being scientific and reasonable, mild in condition, simple to operate and the like. The reaction equation is shown in the specification.
Owner:QINGDAO UNIV OF SCI & TECH

Alkynyl imine derivative

The invention provides an alkynyl imine derivative and a synthesis method thereof. According to the method, the 1-o-amino aryl substituted alkynyl imine derivative is prepared from carbodiimide, terminal alkyne, benzyne precursors and activated fluorine ions, the yield is high, and the synthesis method is scientific and reasonable, so that the universal method for synthesizing the alkynyl imine derivative with multiple substituent groups is provided. The method has the advantages of easily-obtained raw materials, wide application range and high separation yield; and experimental equipment and operation are simple and feasible, and further development and application are facilitated.
Owner:PEKING UNIV

Benzenesulfonamide compound containing five-membered heterocycle and preparation method and application thereof

The invention relates to a benzenesulfonamide compound containing five-membered heterocycle shown as a formula I, enantiomer, diastereoisomer, racemate and mixture thereof, pharmaceutically acceptablesalts, crystalline hydrates and solvates thereof, an application of the compounds in preparation of CA inhibitors, and a pharmaceutical composition containing the compound. The compound is used as acarbonic anhydrase inhibitor. Compared with a clinically common carbonic anhydrase (CA) inhibitor aceturamide, the compound provided by the invention has stronger inhibitory activity on CAI, shows very strong inhibitory ability on CAI and CAII, has IC50 of nanomole level, and is expected to avoid in-vivo drug effect loss caused by imbalance of aceturamide.
Owner:ACADEMY OF MILITARY MEDICAL SCI

Preparation method of selenium-containing thiazoline compound

The invention discloses a preparation method of a selenium-containing thiazoline compound, and belongs to the technical field of organic synthesis. The method comprises the following steps: adding thioamide, a diselenide compound, a solvent and an electrolyte into a reactor, carrying out a reaction process under the action of electrification, and carrying out silica gel column chromatography separation after the reaction is finished to obtain a pure target product. The preparation method of the selenium-containing thiazoline compound provided by the invention has the characteristics of simpleoperation, mild conditions, short reaction time and the like. The reaction equation is shown in the specification.
Owner:QINGDAO UNIV OF SCI & TECH

Polysubstituted quinazoline imine derivative and preparation method thereof

The invention discloses a polysubstituted quinazoline imine derivative and a preparation method thereof, belonging to the technical field of chemicals preparation. The structural formula of the polysubstituted quinazoline imine derivative is shown in a formula (I). The preparation method comprises the step as follows: carrying out a heating reaction on diaryl hypervalent iodine salt and o-aminoacrylonitrile in a solvent under the catalysis of a copper salt for 2-24 hours at 70-150 DEG C to obtain the polysubstituted quinazoline imine derivative shown in the formula (I). The synthesis method of the polysubstituted quinazoline imine derivative disclosed by the invention is scientific and reasonable; the polysubstituted quinazoline imine derivative with various substituent groups, which cannot be synthesized by other methods, can be synthesized; the preparation method has the characteristics of simple synthesis process, high productive rate and the like; and the polysubstituted quinazoline imine derivative is easy to purify.
Owner:TSINGHUA UNIV

Synthesis method of aryl thiophthene derivative

The invention discloses a synthesis method of an aryl thiophthene derivative, which belongs to the field of organic synthesis. The method comprises the following steps of: a) mixing and reacting a compound shown as a formula I and a compound shown as a formula II in an ether solvent, wherein a reaction temperature is between the freezing point of the solvent and room temperature; b) adding zinc powder, raising the reaction temperature to be between 110 DEG C and the boiling point of the solvent and reacting so as to obtain the aryl thiophthene derivative shown as a formula III, wherein R1 and R2 independently represent substituted or unsubstituted alkyl with 1 to 18 carbon atoms, naphthenic base with 3 to 6 carbon atoms, aryl with 6 to 12 carbon atoms or heterocyclic aryl with 2 to 12 carbon atoms; Ar represents aryl with 6 to 12 carbon atoms or heterocyclic aryl with 2 to 12 carbon atoms; and X represents halogen. The synthesis method can be applied to organic photoelectric materials and relevant fields.
Owner:PEKING UNIV

Method for synthesizing quinolin-2-imide derivative

The invention discloses a method for synthesizing a quinolin-2-imide derivative. According to the method, the quinolin-2-imide derivative is prepared by using diaryl iodonium ions, carbodiimide, alkyne and a copper catalyst, the yield is relatively high, the synthesis method is scientific and reasonable, and thus, a universal method for synthesizing the quinolin-2-imide derivative with a variety of substituents by a three-component-reaction one-pot process is provided. According to the method, the raw materials are cheap and readily available, the catalyst is cheap, the applicable range is wide, the yield of separation is high, the regioselectivity is good, and the experimental facilities and operation are easy and feasible, so that further development and application are facilitated.
Owner:PEKING UNIV

Method for synthesizing 1,2,3,4-tetrahydropyridine derivatives from chain 1,3-dicarbonyl compound in one-pot method

The invention belongs to synthesis of organic intermediates, more particularly relates to a method for synthesizing 1,2,3,4-tetrahydropyridine derivatives from a chain 1,3-dicarbonyl compound in one-pot method. The method comprises the following steps of: adding the chain 1,3-dicarbonyl compound, primary amine and a formaldehyde water solution into a reaction vessel, then adding a solvent and reacting for 4 to 8h, concentrating and purifying after the reaction is finished to obtain the 1,2,3,4-tetrahydropyridine derivatives. The invention provides a synthesis method of the 1,2,3,4-tetrahydropyridine derivatives and has scientific and reasonable synthesis method, mild conditions, simple and easy operation and production yield of up to more than 80 percent.
Owner:ZHENGZHOU UNIV
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