79results about How to "With structural diversity" patented technology

The invention discloses a method for synthesizing trichlorine methoxyl chlorobenzene and trichlorine methoxyl phenylamine. One of 4-chlorine trichlorine methoxyl benzene, 3-chlorine trichlorine methoxyl benzene and 2-chlorine trichlorine methoxyl benzene is synthesized by performing photochlorination reaction on one of 4-chloroneb, 3-chloroneb and 2-chloroneb serving as a raw material and chlorine in a solvent under the action of a catalyst. The corresponding 4-chlorine trichlorine methoxyl benzene, the 3-chlorine trichlorine methoxyl benzene and the 2-chlorine trichlorine methoxyl benzene are obtained by separating the solvent. One of the 4-chlorine trichlorine methoxyl benzene, the 3-chlorine trichlorine methoxyl benzene and the 2-chlorine trichlorine methoxyl benzene is mixed with hydrogen fluoride, and the mixture is fluorinated and ammoniated and then is rectified to obtain the corresponding 4-trichlorine methoxyl phenylamine, the 3-trichlorine methoxyl phenylamine and the 2-trichlorine methoxyl phenylamine. The method has the characteristics of simple operation, mild reaction condition, no three-waste emission, easiness in separation of a product and the solvent and the like, and forbidden chemical substances required by the international and national environment protection organizations are not used.

The invention discloses application of a sludge carbon catalyst with a modified surface in reaction of inserting O-H into carbene and constructing a C-O bond. Alpha-diazonium ester and a phenolic compound serve as starting materials, modified sludge carbon treated by perchloric acid serves as a catalyst, the construction of the C-O bond is achieved by forming metal carbene to complete O-H insertion under the conditions of heating and air atmosphere, and an alpha-(phenoxy)acetate derivative is generated in one step. The catalyst is prepared by sludge remaining after municipal sewage treatment,and has the advantages of having a wide source, being prepared easily, having low cost, and being green and environmentally friendly; the reaction raw materials are easy to obtain, the conditions aremild, the yield is good, the gram-scale reaction can be achieved, the catalyst has an industrial prospect, the reuse of waste is achieved, and the purpose of green environmental protection and green chemistry is achieved.

The invention discloses a 1,2,3-triazole derivative and a synthesis method thereof. S,N-Substituted internal olefin and aryl diazonium salt are used as initial raw materials, copper salt is used as acatalyst, and cyclization is performed in the presence of alkali and an oxidizing agent in an organic solvent to obtain 1,2,3-triazole derivative. By designing the substrate configuration, 1,2,3-triazole derivative with potential biological activity is simply and conveniently synthesized. The method has the advantages of accessible raw materials, wide substrate range, mild synthesis reaction conditions and high reaction product yield, is simple to operate, and has diversified functional groups.

The invention discloses a synthesis method of a 3-(2-cyanovinyl)indole derivative. An indole derivative cheap, easy to obtain and having structural diversity is used as a raw material and performs continuous Friedel-Crafts reaction / elimination reaction with 3-dimethylamino acrylonitrile in the presence of acid, and the 3-(2-cyanovinyl)indole derivative is synthesized. Compared with a reported 3-(2-cyanovinyl)indole derivative synthesis method, the raw material is cheap, easy to obtain and low in toxicity, operation is easy and simple, the reaction conditions are mild, and the efficiency is high.

The invention discloses a synthesis method of an indole derivative with wide bioactivity. The method includes: taking a simple pyrrole derivative and a beta-chloroketone derivative as the raw materials, using a palladium salt as the catalyst, adding an oxidant and an additive, and under an alkaline condition, carrying out Domino pyrrole alkenylation-Diels-Alder cycloaddition-dehydro-aromatization reaction to synthesize the indole derivative. Compared with the reported indole derivative synthesis method, the method provided by the invention has the advantages of easily available raw materials, simple operation, wide application range, and mild synthesis reaction conditions.

The invention discloses a circulating tumor cell detection method. The circulating tumor cell detection method is characterized in that highly heterogeneous circulating tumor cells are accurately marked through glucose metabolism engineering independent of tumor cell types, the marked circulating tumor cells are subjected to lossless capture through a biological orthogonal reaction, and the captured circulating tumor cells are subjected to nondestructive release through reversible reaction, so that accurate and nondestructive detection of the circulating tumor cells is realized.

The invention discloses a method for synthesizing polychloroalkane. According to the invention, C10-13 straight-chain polyene hydrocarbon is adopted as a raw material, and is subjected to a catalytic addition reaction with a chlorination reagent trimethylchlorosilane under the effects of potassium permanganate and benzyl triethyl ammonium chloride, such that polychloroalkane chlorinated at a specific position is synthesized. With separation purification methods such as column chromatography, reduced-pressure distillation, re-crystallization, and the like, a polychloroalkane compound with a single structure is obtained. The method can be effectively applied in short-chain chlorinated paraffins (SCCPs) monomer compound synthesis. Compared with reported short-chain chlorinated paraffin monomer compound synthesis methods, the method provided by the invention has the characteristics such as convenient operation, mild synthesis reaction condition, wide application range, and easy separation property of product.

The invention discloses a synthetic method of polysubstituted benzoic acid. Benzoic acid which is simple and easy to obtain and aziridine which is easy to prepare are used as raw materials, synthesisof polysubstituted benzoic acid is achieved in one step, and the obtained polysubstituted benzoic acid can be further converted into a functional product. The method has the advantages of easily available raw materials, simple operation, mild synthesis reaction conditions, high reaction efficiency, and diversity of functional groups.

The invention discloses a method for synthesizing a cyanoalkyl substituted tetra-substituted olefin derivative with potential biological activity. According to the method, 3,3-dialkylthio-2-propylene-1-one and cyclobutanone oxime ester which are easy to prepare and have structural diversity and multiple reaction centers are used as raw materials, free radicals are generated through cyclobutanone oxime ester to carry out olefin addition, and the cyanoalkyl-substituted tetra-substituted olefin derivative is generated in one step. The method has the advantages of easily available raw materials, simple operation, mild synthesis reaction conditions, high reaction efficiency, and diversity of functional groups.

The invention discloses a method for preparing pyrazole derivatives and a clinic breast cancer treatment drug tetra-substituted olefin (Z)-Tamoxifen from sulfopolysubstituted olefin. The method comprises the following steps: carrying out a condensation cyclization reaction of a raw material alpha-carbonyloxo ketene monothioacetal and a nucleophilic reagent hydrazine to prepare the pyrazole derivatives; and carrying out a coupling reaction of the alpha-carbonyloxo ketene monothioacetal raw material and arylboric acid to prepare the tetra-substituted olefin Tamoxifen. Compared with pyrazole derivatives and (Z)-Tamoxifen prepared through reported preparation methods, the above products in the invention have the advantages of good regioselectivity and stereoselectivity, easily available raw materials, simple operation, mild preparation reaction conditions and high efficiency.

The invention discloses an acid catalytic synthesis method and application of phenoxyacetate derivatives. In the method, an O-H insertion reaction is performed on one diazo ester compound and one phenolic compound by an acid catalyst to form a C-O bond to generate one corresponding phenoxyacetate derivative. The method provided by the invention adopts an acid as the catalyst, has mild conditions (room temperature), is green and high-efficiency, can realize a gram-scale reaction, and has industrial application prospects; the method does not need transition metal catalysis, avoids pollution to the environment caused by metal ions in post-treatment, and conforms to the purpose of green chemistry; and in addition, the developed methodology is applied to certain natural phenolic products or phenolic medicines with significant pharmacological activity to obtain one corresponding O-H insertion product, natural product magnolol and honokiol are taken as examples, experiments find that the anti-tumor and anti-inflammatory activity of the O-H insertion products are generally higher than those of the magnolol and the honokiol respectively, the anti-tumor activity is particularly obvious, andthe derivatives have the possibility of becoming a medicine and provides more choices for sources of the novel medicine.

The invention discloses a method for synthesizing a bicyclic pyridone derivative with potential bioactivity, comprising the following steps that: 5,5-bisalkylthio-2,4-pentadienoic acid ester used as a raw material with the characteristics of being easy to prepare, having structural diversity and multiple reactive centers and a bimolecular nucleophilic reagent organic diprimary amine is subject tosubstitution / condensation in refluxing to synthesize the bicyclic pyridone derivative. Compared with the reported synthetic methods of the bicyclic pyridone derivative, the method disclosed in the invention has the advantages of being convenient for raw materials, simple operation, mild reaction conditions and high efficiency.

The invention discloses a method for synthesizing a bisindole derivative. An indole derivative which is cheap and easy to obtain and rich in structure diversity is adopted as a raw material which is reacted with 3-dimethylamino acrylonitrile in the presence of an acid, and the bisindole derivative can be synthesized. Compared with a reported bisindole derivative synthesis method, the method has the advantages of being cheap and easy in raw material obtaining, low in toxicity, simple and convenient to operate, gentle in synthesis reaction condition, high in efficiency, and the like.

The invention discloses a method for synthesizing a chiral boron compound containing trifluoromethyl and having a potential biological activity. With beta-trifluoromethyl-alpha,beta-unsaturated ketone and bis(pinacolato)diborane as raw materials, and a chiral ligand copper salt as a catalyst, an asymmetric boronizing reaction is carried out for synthesis of the chiral boron compound. Compared with a reported method for synthesizing the chiral boron compound, the method has the advantages of easily obtained raw materials, simple operation, wide application range and mild reaction conditions, the product contains a carbon chiral center connected with trifluoromethyl, and the product has the potential biological activity.

The invention belongs to the technical field of organic synthesis, and particularly relates to a diisoindole iridium (III) complex which is characterized in that the structural general formula of the diisoindole iridium (III) complex is as shown in a formula I defined in the description, wherein R1, R2 and R3 are respectively and independently selected from one of H, alkyl with the carbon atom number of 1-12 and naphthenic base with the carbon atom number of 3-12; and Ar1 and Ar2 are each independently selected from a group containing an aromatic ring. The diisoindole iridium (III) complex has structural diversity and high molar absorption coefficient, the maximum absorption wavelength can reach a near-infrared region, and the diisoindole iridium (III) complex has good application prospects in the fields of biomedicine, material science and the like as a photosensitizer, an imaging reagent, a strong near-infrared absorber and the like.

The invention discloses a method for synthesis of 2-imino oxazole derivatives having potential bioactive activity. The method comprises that 3, 3-diarylamino-2-propen-1-one, which is easy to prepare and has structural diversity and multiple reaction centers, is used as a raw material and undergoes an oxidative cyclization-Baldwin rearrangement reaction in air to produce a 2-imino oxazole derivative. Compared with the reported synthesis methods of 2-imino oxazole derivatives, the method provided by the invention utilizes easily available raw materials, can be simply operated and has mild reaction conditions and a high yield.

The invention discloses a method for preparing hydrogen by alkali-promoted nitrogen heterocyclic dehydrogenation. According to the method, hydrogen is prepared by using indoline, 1,2,3,4-tetrahydroquinoline and 1,2,3,4-tetrahydroquinoxaline as initial raw materials under the action of a cheap and easily available alkali while indole, quinoline and quinoxaline compounds are obtained. The method hasthe advantages of accessible raw materials, high reaction efficiency and diversified functional groups, and is simple to operate.

The invention discloses a synthesis method of a 3-arylsulfonyl indole derivative. A 1,5-eneyne compound which is easy to prepare and has structural diversity is used as a raw material to react with aryl diazonium salt and DABCO.(SO2)2 in a solvent to obtain the 3-arylsulfonyl substituted indole derivative. The method is simple and convenient to operate, wide in substrate range and mild in synthesis reaction condition, and functional groups of the method are diversified.

The invention discloses a method for synthesizing a 4-alkylthio polysubstituted thiophene derivative with potential biological activity. According to the invention, the 4-alkylthio polysubstituted thiophene derivative is generated in one step through intermolecular in-situ generation of sulfur ylide and intramolecular cyclization reaction by using a 3,3-dialkylthiomethylene-1,3-dicarbonyl compoundwith characteristics of easy preparation, structural diversity and multiple reaction centers and a diazo compound as raw materials, has a certain potential pharmaceutical activity, and can be furtherconverted into a functional product. The method has the advantages of easily available raw materials, simple operation, mild synthesis reaction conditions, high reaction efficiency, and diversity offunctional groups.

The invention provides an alkyl borane derivative and a synthesis method thereof. The method comprises the steps that an aliphatic carboxylic acid derivative and bis-pinacol diborane serve as initial reaction raw materials, palladium salt serves as a catalyst, silver salt serves as an oxidizing agent, C-H bond activation and one-step synthesis reaction are conducted in a solvent in the presence of alkali and an additive, the reaction has good regioselectivity, functional group diversity and wide applicability, amide groups in the skeleton structure of the alkyl borane derivative can be hydrolyzed to obtain corresponding carboxylic acid, alkyl boron groups can be further functionalized, and the alkyl borane derivative can be used as intermediates of structures of drugs and chemical products.

The invention discloses a screening method and application of a small molecular compound for targeted inhibition of vitamin K epoxide reductase, and belongs to the technical field of molecular cell biology and biochemistry. By constructing a vitamin K circulation small molecule inhibitor screening system (namely a double-reporter-gene cell system), high-throughput screening can be rapidly performed on a drug small molecule library, and a small molecule compound for targeted inhibition of vitamin K circulation is obtained; furthermore, by detecting the inhibition effect of the screened small molecular compound on the activity of the VKOR protein, the small molecular compound capable of specifically inhibiting the activity of the VKOR protein can be obtained. By adopting the method, compounds of which the structures are different from those of coumarin derivatives and phenylindanedione derivatives are screened for the first time, can specifically inhibit the activity of VKOR protein, have potential application value of being developed into rodenticide and anticoagulant drugs, and are lead compounds for developing rodenticide and anticoagulant drugs.

The invention discloses a 2-(3-isoquinolyl)-ethyl propionate derivative and a synthesis method thereof. Using O-acetyl oxime, which is easy to prepare, has structural diversity and multiple reaction centers, as a raw material, under the action of rhodium salt, the ortho-position C–H bond of the aromatic ring in O-acetyl oxime is activated to react with allenoate A series of 2‑(3‑isoquinolinyl)‑ethyl propionate derivatives with different structures were synthesized through the coupling reaction, and the products could be further transformed into functionalized products. The method has easy-to-obtain raw materials, simple operation, mild reaction conditions, and the diversity of functional groups without pre-functionalization.

The invention discloses a 2-hydroxypyridine compound and a synthesis method and application thereof. According to the method, enaminone is used as a starting raw material, tempo salt is used as an oxidizing agent, and the 2-hydroxypyridine compound is generated through an oxidation reaction and a coupling cyclization reaction under a heating condition. The reaction functional group is high in compatibility, the yield is as high as 80%, and the product has functional group diversity. The compound can be used as an organic synthesis precursor, and 2-hydroxyl and 6-hydrogen atoms in the structurecan be further functionalized to obtain a drug molecular skeleton or a compound with potential biological activity and the like.

The invention discloses the application of a surface-modified sludge charcoal catalyst in carbene insertion O-H reaction and construction of C-O bonds. Using α-diazo esters and phenolic compounds as starting materials, the modified sludge charcoal treated with perchloric acid as a catalyst, under heating conditions and in an air atmosphere, O-H insertion is completed by forming metal carbene to achieve C-O Bond construction, a one-step reaction to generate α-(phenoxy) acetate derivatives. The catalyst used in this method is prepared from the remaining sludge after urban sewage treatment, and has a wide source, easy preparation, low cost and environmental protection; the reaction raw materials are easy to obtain, the conditions are mild, and the yield is good, and the reaction on a gram scale can be realized. It has the prospect of industrialization, and at the same time realizes the reuse of waste, which is in line with the purpose of green environmental protection and green chemistry.

The invention discloses a 4-chloro(bromo)-5-alkylthio-3-pyrrolidone derivative and its synthesis. By using 1-alkylthio-1-amino-5- aromatic (heterocyclic) ring-1,4-pentadiene-3-ketone as a starting material, using CuCl2 or CuBr2 as a promoter and using LiCl or LiBr as an auxiliary agent, intramolecular cycloamination and halogenating reaction are carried out under the heading condition so as to generate the 4-chloro(bromo)-5-alkylthio-3-pyrrolidone derivative by one step. The obtained 3-pyrrolidone derivative can undergo further conversation to generate a functional product. The method has the following advantages: raw materials are easily available; synthesis reaction conditions are mild; reaction efficiency is high; and stereoselectivity of the product is good, and its functional group has diversity.

The invention relates to 1, 2, 3-triazole-2-oxide and a preparation method thereof, and belongs to the technical field of chemical organic synthesis. The structure of the 1, 2, 3-triazole-2-oxide is as shown in formula 1 in the specification, wherein, R1 is C1-4 alkyl, aryl or aryl vinyl, the aryl of R1 is phenyl, aryl with a substituent group on a benzene ring or heterocyclic aryl, R2 is C1-4 alkyl or benzyl, R3 is C1-4 alkyl or aryl, and the aryl of R3 is phenyl, aryl with a substituent group on a benzene ring or heterocyclic aryl. The 1, 2, 3-triazole-2-oxide with various structures is obtained from simple and easily available raw materials, an azide is not required to be used in the reaction, the operation is simple and convenient, the substrate application range is wide, and the product is easy to convert.

The invention discloses a 2-alkylthioenamide derivative and a synthesis method thereof. Using 1-alkylthio-1-amino-1-en-3-one and iodobenzene acetate as starting materials, under solvent-free or solvent-free milling conditions, through 3-position acetic acidification, 1,3 ‑Carbonyl migration and 2,3‑alkylthio group migration react to generate 2‑alkylthioenamide derivatives in one step, and the resulting amide derivatives can be further transformed into functionalized products. The method has easy-to-obtain raw materials, simple operation, mild synthesis reaction conditions, high efficiency, wide substrate adaptability, good stereoselectivity of products, and diverse functional groups.

The invention discloses a synthesis method of a 2-alkylthio polysubstituted furan derivative. Ketene dithioacetal and aryl methyl ketone which are easy to prepare and have structural diversity and multiple reaction centers are used as raw materials, the 2-alkylthio polysubstituted furan derivative is generated in one step through intermolecular oxidation cross-coupling and intramolecular cyclization reaction, and the obtained polysubstituted furan derivative has certain potential drug activity and can be used for preparing drugs. And functional products can be further generated through conversion. The method has the advantages of easily available raw materials, simple operation, mild synthesis reaction conditions, high reaction efficiency and diversity of functional groups.