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

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 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 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 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 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-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 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 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.