10 results about "Amine alkylation" patented technology

The invention discloses a synthesis method of Olrabatinib, which comprises the following steps: by taking 2-methyl-5-nitro trifluorotoluene as a raw material, carrying out a Waller-Ziegler reaction, an alkylation / silanization reaction of amine, nitro reduction, a condensation reaction and a Caslow-Stevens coupling reaction, so as to obtain the Olrabatinib. By optimizing process conditions and a reaction system, the synthesis method disclosed by the invention has the remarkable advantages in the following aspects: the raw material cost is greatly reduced by adopting low solvent consumption; the product yield is improved by accurately controlling reaction parameters; a standardized post-treatment process is developed, and large-scale stable production is realized. According to the technical system, the technical bottlenecks of high energy consumption and high pollution in the traditional synthesis route are effectively solved, and an innovative solution is provided for green manufacturing of fine chemicals.

The invention discloses a preparation method of fiazonetin, and belongs to the technical field of medicinal chemistry. According to the route, a 3-methylpyrazine compound is used as a raw material, a compound 3 is obtained through an amine alkylation reaction or a condensation reaction, the compound 3 reacts with orthoester to obtain a compound 4, the compound 4 is subjected to a hydrogenation reduction reaction to obtain a compound 5, and the compound 5 is subjected to chiral resolution or chiral separation to obtain a compound 6. And carrying out condensation reaction on the compound 6 and p-fluorobenzoyl halide to obtain the non-azonepan. The raw materials are simple and easy to obtain, low in cost and more suitable for large-scale industrial production; according to the present invention, the route reaction is simple, the preparation efficiency is high, the yield of each reaction step can achieve about 90%, the ee value of the final product can achieve more than 99.0%, the chiral purity is high, no harsh reaction condition exists, and the method is suitable for large-scale production, and has good market value and profound practical significance. # imgabs0 #

The invention discloses a catalyst for aniline alkylation and a preparation method, and belongs to the technical field of catalysts. The preparation method of the catalyst comprises the following steps: roasting a catalyst carrier precursor, and adding desalted water into a roasted product to prepare slurry; preparing a mixed solution of copper salt, zinc salt and chromium salt; additionally preparing an alkali solution; adding a metal salt mixed solution and an alkaline solution into the slurry, carrying out a co-precipitation reaction, and then aging; repeatedly filtering and pulping the aged slurry to obtain a catalyst precipitation filter cake; and drying, forming and calcining to obtain the catalyst. The invention also discloses the catalyst for aniline alkylation, which is prepared by the method. The catalyst provided by the invention can realize concerted catalysis of aniline alkylation and methanol steam cracking in a single reactor, methanol and aniline are taken as raw materials, N-methylaniline is synthesized with high selectivity, high-purity hydrogen is co-produced, and no wastewater is discharged in the reaction process.

The invention belongs to the technical field of medicine synthesis, and particularly discloses an aminoalkylated paeonol chalcone derivative as well as a preparation method and medical application thereof. The amine alkylation paeonol chalcone derivative is shown as a general formula (I), and is obtained by taking paeonol as a raw material, connecting phenolic hydroxyl groups on the paeonol with organic amine fragments by utilizing different connecting arms, and then carrying out Claisen-Schmidt condensation with various benzaldehydes. In-vitro anti-tumor experiments prove that the derivative has good anti-tumor activity on human colon cancer cells (HCT116), human hepatoma cells (HepG2), human lung cancer cells (A549) and human osteosarcoma cells (U2OS), has obviously better water solubility than paeonol chalcone, is expected to be developed into a medicine for treating various cancers such as colon cancer, osteosarcoma, lung cancer or liver cancer, and has broad application prospects. The clinical application prospect is wide.

The invention discloses a collecting agent compound, a preparation method and a mixed collecting agent, and the preparation method comprises the following steps: measuring 50 mL of 0.6 mol of 1, 3-propane sultone A by using a measuring cylinder, and dissolving the 1, 3-propane sultone A in 0.1-1.0 L of ethyl acetate; slowly adding 155mL and 0.6 mL of N, N-dimethyl octylamine B into the reaction solution obtained in the previous step; stirring the mixture for 1-10 hours at the temperature of 20-100 DEG C to carry out alkylation reaction of amine; after the reaction is finished, filtering a reaction mixture to obtain a white precipitate; washing the precipitate twice with 10ml of ethyl acetate and 10ml of petroleum ether respectively, and finally drying a white solid C in a vacuum oven at the temperature of 100 DEG C; compared with a single-group collecting agent, the prepared collecting agent compound can be selectively adsorbed on the surface of spodumene due to the unique structure and charge distribution after the sulfonic acid and the amino are combined, and the flotation recovery rate of the spodumene can be effectively increased.

The present invention discloses a bimetallic catalyst, a preparation method thereof, and its application in the alkylation reaction of alcoholamines, relating to the technical field of metal catalysts. The bimetallic catalyst comprises a carrier and an active component supported on the carrier; the active component comprises Ni and Cu; and the loading amounts of Ni and Cu are 8-15% and 3-7% of the weight of the carrier, respectively, in weight percentage. The present invention utilizes a method combining femtosecond laser technology with gradient pressure cryogenic freezing technology to modify and activate alumina, effectively increasing its specific surface area and optimizing its pore structure. Furthermore, by loading appropriate amounts of Ni and Cu active components onto the carrier to form a bimetallic catalyst, the selectivity and yield of the target product, tert-butylaminoethoxyethanol, in the alkylation reaction of alcoholamines using diethylene glycol and tert-butylamine as raw materials are significantly improved, showing broad application prospects.

This invention belongs to the field of pharmaceutical synthesis technology, specifically disclosing an aminoalkylated paeonol chalcone derivative, its preparation method, and its pharmaceutical uses. The aminoalkylated paeonol chalcone derivative of this invention is shown in general formula (I). It is obtained by using paeonol as a raw material, linking the phenolic hydroxyl groups on paeonol to organic amine fragments using different linking arms, and then performing Claisen-Schmidt condensation with various benzaldehydes. In vitro antitumor experiments have demonstrated that the derivative of this invention exhibits good antitumor activity against human colon cancer cells (HCT116), human liver cancer cells (HepG2), human lung cancer cells (A549), and human osteosarcoma cells (U2OS), and has significantly better water solubility than paeonol chalcone. It holds promise for development as a therapeutic drug for various cancers such as colon cancer, osteosarcoma, lung cancer, and liver cancer, with broad clinical application prospects.

The application discloses application of a supported Ni-Cu catalyst in alcohol amine alkylation reaction, wherein the alcohol is a fatty alcohol, and the amine is an organic amine, and the alcohol amine alkylation reaction is carried out under the action of the supported Ni-Cu catalyst. The application can reduce the production cost of the catalyst, reduce the energy consumption of the alcohol amine alkylation reaction, and inhibit the side reaction caused by the breakage of C-N bonds in the raw material amine.

The invention belongs to the technical field of amine compounds, particularly relates to the field of IPC C07C213, and more particularly relates to a preparation method of steric hindrance amine. Comprising the following steps: step 1, ammoniating alcohol: carrying out ammoniation reaction on alcohol and amine under the condition of hydrogen in the presence of a heterogeneous catalyst to obtain a secondary amine intermediate; 2, secondary amine alkylation: carrying out a hydrogenation reaction on the secondary amine intermediate and an alkylation reagent in the presence of a heterogeneous catalyst in the presence of hydrogen to obtain a crude product; and step 3, rectification: removing water and light fractions from the crude product to obtain the product. Compared with a traditional tertiary amine catalyst, such as bis (dimethylamino) ethyl ether, pentamethyldiethylenetriamine and triethylene diamine, the steric hindrance amine prepared by the preparation method disclosed by the invention has excellent catalytic activity and ageing resistance.

The invention discloses a method for hydrogenation of aliphatic olefins by nickel catalysis. The reaction process is as follows: in a nitrogen atmosphere, a compound 2, a nickel catalyst, an aromatic boronic acid, a base, a solvent, an additive, a phosphine ligand and a compound 1 are sequentially mixed, stirred at 80-120°C for reaction for 18-36 hours, cooled to room temperature, decompressed to remove the solvent, and separated by column chromatography to obtain a target product. When the phosphine ligand is tri-tert-butyl phosphine, the target product is compound 3, and when the phosphine ligand is diphenylethyl phosphine, the target product is compound 4. The molar ratio of the compound 2, the phosphine ligand, the nickel catalyst, the aromatic boronic acid, the base and the additive is 1:(0.1-0.4):(0.05-0.2):(0.2-1.2):(0.4-1.2):(0.05-0.2), the equivalent ratio of the compound 1 to the compound 2 is 1:(1-3), R 1 is an alkyl group or a silicon group, R 2 is an alkyl, aryl or heteroaryl group, R 3 The present invention can selectively synthesize branched or chain alkylamine compounds only by regulating the ligand in the nickel catalyst.