473 results about "Benzamide" patented technology

Embodiments of the present invention provide methods and intermediates for the large scale preparation of 2, 4, 6-trifluoro-N-[6-(1-methylpiperidine-4-carbonyl)-2-pyridyl] benzamide hemisuccinate, as well as formulations and product forms prepared by these methods. Embodiments of the present invention further provide for the preparation of lamidetan acetate (2, 4, 6-trifluoro-N-[6-(1-methylpiperidine-4-carbonyl)-2-pyridyl] benzamide acetate) and / or a pharmaceutical composition thereof, and / or the use of lamidetan acetate and formulations thereof in subcutaneous drug delivery.

The invention belongs to the technical field of ETFE film preparation, and particularly relates to a preparation method of a high-strength ETFE film. The preparation method of the ETFE film comprises the following steps: preparing a mixture of modified nano cellulose and calcium magnesium silicate whiskers; carrying out modification treatment on the poly (p-benzamide) fiber; and preparing the ETFE film. According to the preparation method of the high-strength ETFE film, the perfluoroalkoxy copolymer and the ETFE resin are selected and mixed for use, during melt extrusion, the perfluoroalkoxy copolymer can lubricate the ETFE and reduce the overall melt viscosity, the critical shear rate of the perfluoroalkoxy copolymer is higher than that of the ETFE, melt fracture can be inhibited, the film is evenly extruded, the flatness of the film surface is improved, and the high-strength ETFE film is prepared. And meanwhile, the elastic retraction of the ETFE is inhibited during high-temperature setting. And the modified nano cellulose and calcium magnesium silicate whisker mixture and the modified poly-p-benzamide fiber are added to enhance the mechanical strength of the prepared ETFE film.

There is provided an alkali metal salt of 4-chloro-N-[2-[(4-chlorophenyl)methyl]-3-oxo-1,2,4-thiadiazol-5-yl]benzamide and formulations thereof. This salt finds particular utility in the treatment or prevention of a disorder or condition ameliorated by the activation of AMPK.

The invention belongs to the technical field of medicinal chemistry, and particularly relates to a 3-sulfamoyl benzamide compound as well as a preparation method and application thereof. The 3-sulfamoyl benzamide compound has a structure as shown in a formula I. In the formula I, X is chlorine or trifluoromethyl; r1 and R2 are independently C1-4 alkyl or R1, R2 and N atoms connected with R1 and R2 jointly form a heterocyclic group, and the heterocyclic group is a substituted or unsubstituted five-membered or six-membered heterocyclic group; and when the heterocyclic group is a substituted heterocyclic group, the substituent group in the substituted heterocyclic group is one or more of C1-4 alkyl, phenyl and acetyl. The 3-sulfamoyl benzamide compound disclosed by the invention has a remarkable proliferation inhibition effect on HCT116 colon cancer cells, HeLa human cervical cancer cells, MDA-MB-231 human breast cancer cells and A375 human malignant melanoma cells.

The invention relates to preparation of a crystalline allyl covalent organic framework material and application research of the crystalline allyl covalent organic framework material in benzamide cyclization green photocatalytic conversion. The SF-COF material is prepared by adopting a step-by-step synthesis method. The preparation method comprises the following steps: synthesizing a COF precursor by taking 1, 3-benzenetricarboxaldehyde and p-aminophenylacetonitrile as raw materials, and preparing the allylation covalent organic framework material with the electronic push-pull effect from the COF precursor and 5, 5 ', 5'-(benzene-1, 3, 5-triyl) tri (thiophene-2-formaldehyde) through a solvothermal method. The material is applied to the field of photocatalytic organic conversion, and benzamide cyclization and conversion of derivatives of benzamide are achieved under irradiation of a blue light LED. The prepared SF-COF has the advantages of efficient charge separation and electron conduction performance, good structural stability and chemical stability and the like. And a catalyzed organic reaction substrate has the advantages of wide universality range, good cycle stability and the like, and shows excellent photocatalytic conversion capability.

Provided is a method of treating malignant tumor by an azabicyclic compound, particularly, with eye disorder reduced. The present invention provides a method for treating malignant tumor, comprising administering an effective amount of 3-ethyl-4-[3-(1-methylethyl)-4-[4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl]-1H-pyrazolo[3,4-b]pyridin-1-yl]benzamide (compound 1) or a salt thereof to a patient in need thereof according to a dosing regimen, wherein the dosing regimen comprises administering the compound 1 or the salt thereof at a dose from 40 mg / body / day to 240 mg / body / day in terms of the amount of the compound 1 for consecutive days, and then providing a withdrawal period of at least 2 days.

The invention relates to the technical field of preparation of N-(2, 4-dinitrophenyl)-4-nitrobenzoyl aniline, in particular to a method for preparing a nitro amide compound by adopting a microreactor. The method for preparing the nitro amide compound comprises the following steps: introducing a sulfuric acid solution of 4-nitro-N-phenylbenzamide and a nitric acid aqueous solution into a microreactor, and reacting to obtain N-(2, 4-dinitrophenyl)-4-nitrobenzamide; the microreactor is provided with at least two reaction modules which are connected in series, and a sulfuric acid solution of 4-nitro-N-phenylbenzamide is divided into at least two strands which are respectively fed into a first reaction module of the microreactor and other reaction modules except the first reaction module; and the nitric acid aqueous solution enters the microreactor in a way of at least one stream. According to the method, the microreactor is used as a reaction carrier, the temperature in the reaction process is controllable, the raw material conversion rate is increased, and the residual amount of an intermediate N-4-nitro-(4-nitrophenyl) benzamide is reduced.

The invention relates to the technical field of benzamide, in particular to a preparation process of 4-hydroxythiobenzamide, which comprises the following steps: S1, preparing raw materials: preparing the 4-hydroxythiobenzamide from the following raw materials in parts by weight: 80-100 parts of formic acid, 80-100 parts of hydrochloric acid, 20-30 parts of 4-hydroxybenzaldehyde, 8-12 parts of hydroxylamine hydrochloride, 8-12 parts of thioacetamide and 4-6 parts of sodium hydroxide. According to the preparation method, after 4-hydroxybenzaldehyde is subjected to activating treatment reaction, part of positive charges on aldehyde carbon are dispersed, oxygen atoms in an acetal structure are connected with the aldehyde carbon through covalent bonds to generate an electron withdrawing induction effect, the reaction sequence and the reaction path of the 4-hydroxybenzaldehyde can be controlled through aldehyde activation, and the reaction efficiency of the 4-hydroxybenzaldehyde is improved. Therefore, the generation of byproducts is reduced, and the purity of a reaction product obtained from 4-hydroxybenzaldehyde is improved.

The invention relates to an effective amount of novel benzamide derivative as shown in a general formula (I), a preparation method thereof and application of a pharmaceutical composition containing the derivative as a medicine, compared with the prior art, the compound has better metabolic stability, can be orally taken and has a wider application prospect. # imgabs0 #

The invention discloses a polymer based on side-chain liquid crystal polynorbornene as well as a preparation method and application thereof, a monomer based on side-chain liquid crystal polynorbornene has a structure as shown in a general formula 1, and the polymer based on side-chain liquid crystal polynorbornene has a repeating unit as shown in a general formula 8. According to the monomer structure, a benzamide group is introduced into a side chain liquid crystal molecular structure, adjacent liquid crystal side chains generate hydrogen bond interaction after polymerization, on one hand, the mechanical property of the material is improved, on the other hand, stacking arrangement of a layered structure can be promoted during film preparation, and the gas barrier performance is improved.

The invention discloses a method for detecting related substances in imaric acid dihydrochloride by HPLC (High Performance Liquid Chromatography), and belongs to the technical field of chemical engineering and pharmacy, the related substances in the imaric acid dihydrochloride are detected by high performance liquid chromatography, a phosphate buffer solution (0.05 mol / L of monopotassium phosphate solution, and pH adjusted to 2.5 by phosphoric acid) is used as a mobile phase A, acetonitrile is used as a mobile phase B, gradient elution is carried out, the flow rate is 1.0 ml / min, the detection wavelength is 250nm, and the detection wavelength is 250nm. The column temperature is 40 DEG C, and the detection wavelength is 235nm; the method can be used for effectively separating and quantitatively detecting imatamide, demethylated imaric acid dihydrochloride, ortho-imaric acid, meta-imaric acid, p-hydroxymethyl benzamide, an intermediate B, p-hydroxymethyl benzoic acid, an imaric acid dimer, p-cyanobenzyl alcohol, p-chloromethyl benzamide, p-toluic acid and p-chloromethyl benzoic acid in the imaric acid dihydrochloride. The method disclosed by the invention is simple and convenient to operate, strong in specificity, high in sensitivity and accuracy, good in linearity and capable of effectively controlling the quality of a p-imaric acid dihydrochloride product.

The invention is suitable for the technical field of fine chemical engineering, and provides a synthesis method of sulpiride impurity 2-hydroxy-5-sulfanilamide benzamide, which comprises the following specific steps: Step 1, taking salicylic acid as a raw material, taking DMF as a catalyst, and carrying out acylation reaction with thionyl chloride to obtain acylation liquid, and entering the next process; 2, ammoniating the acylation liquid with ammonia water at a low temperature to obtain salicylic acid formamide, and drying to obtain an intermediate 1; 3, TMS-Cl is used for protecting phenolic hydroxyl groups, then chlorosulfonic acid is dropwise added, a chlorosulfonation reaction is carried out, and an intermediate 2 solution is obtained after the reaction is completed; and Step 4, dropwise adding the solution of the intermediate 2 into stronger ammonia water for reaction, carrying out suction filtration, and recrystallizing with ethanol to obtain the sulpiride impurity 2-hydroxy-5-sulfanilamide benzamide. The route synthesis is simple, and the quality can reach 95% or above; in addition, the method has the advantages of cheap and easily available raw materials, mild reaction conditions, low energy consumption, simple process structure, easy operation and the like.

The invention relates to the field of organic chemical synthesis, in particular to a quinazolinone compound synthesized by carbon dioxide and a preparation method of the quinazolinone compound. According to the preparation method for synthesizing the quinazolinone compound from carbon dioxide, carbon dioxide, a 2-aminobenzamide compound and aryl halide are taken as raw materials, and are subjected to a heating reaction in the presence of a palladium metal catalyst, a ligand, a reducing agent, alkali and an organic solvent to generate the quinazolinone compound. The mechanism is as follows: carbon dioxide forms an intermediate A under the conditions of alkali and a reducing agent, aryl halide and the intermediate A form a carbonyl metal compound B under the action of a palladium metal catalyst, and then the carbonyl metal compound B reacts with a 2-aminobenzamide compound under the action of the alkali and the reducing agent to obtain the quinazolinone compound. The catalyst system has universality to various types of 2-aminobenzamide and derivatives and aryl halides thereof, the raw materials are wide in source, cheap and easy to obtain, and the reaction process is simple and controllable.

The present invention relates to fungicidal compositions comprising as component 1) the compound (I) methyl (2Z)-3-methoxy-2-[(4-methylbiphenyl-3-yl)oxy]prop-2-enoate) and as active component 2) the compound (II) N-(2-fluorophenyl)-4-[5-(trifluoromethyl)-1,2,4-oxadiazol-3- yl]benzamide wherein the weight ratio of compound (I) to compound (II) is from 10:1 to 1:10.

The present application relates to the technical field of medicine (IPC classification A61P31 / 22), and particularly relates to a preparation method and application of a tetrahydroindazole antitumor compound, the preparation method comprising: reacting a compound of formula I with adamantanol to obtain a 4-(4-hydrazone-3,6,6-trimethyl-1-tetrahydroindazole)-2-(4-hydroxycyclohexylamino) benzamide compound, compared with a 4-(4-hydrazone-3,6,6-trimethyl-1-tetrahydroindazole)-2-(4-hydroxycyclohexylamino) benzamide compound in the prior art, the compound has stronger inhibition of tumor cell growth activity, has generally lower IC50 values, and in particular can significantly reduce the clonogenicity of non-small cell lung cancer at a low concentration, and causes apoptosis of non-small cell lung cancer cells, and has great significance for development of a novel antitumor drug.

The subject of the invention is N-substituted derivatives of l-(l-phenyl-3-aryl)-lH-pyrazol-4-yl)methanamine with the general formula 1, where ¥ represents CH or N, R1 represents hydrogen, R2 represents no substituent, R3 represents hydrogen, while R4 represents N-propylbenzamide, benzo[b]furan, dihydrobenzo [b] furan, methylenedioxybenzene, ethyl benzoate, or propyl benzoate, substituted accordingly, their method of production and application, and the method of obtaining and application of N-substituted derivatives of l-(l-phenyl-3-aryl)-IH-pyrazol-4-yl)methanamine with the general formula 1, where Y represents C, CH, or N, R1 represents hydrogen or a methyl group, R2 represents a methyl group or no substituent, R3 represents hydrogen or a methyl group, while R4 represents dimethylpyrazole, methylpyrazole, dimethylimidazo[l,2-a]pyrimidine, or isopropoxybenzene, substituted accordingly. The compounds that are the subject of the invention are obtained through reductive amination using borohydride derivatives as the reducing agent, advantageously sodium triacetoxyborohydride, in the amount of 1.4-2.0 eq, amine in the amount of 1.0-1.1 eq, advantageously in slight excess, base, advantageously triethylamine in the amount of 1.0-1.1 eq (in the case of using amine in the form of hydrochloride), and the starting aldehyde. The reaction is conducted in a nonpolar solvent environment, advantageously dichloroethane at a concentration of about 0.1 M. The crude product is purified by column chromatography on silica gel using a methanol in dichloromethane mixture as the eluent, in concentration ranges from 2% to 5%. In order to obtain a solid form and improve the physicochemical parameters, the free bases are converted into hydrochloride form, and then crystallized from a polar solvent, advantageously ethanol or propanol.

N-(1H-imidazol-2-yl)benzamide compound of formula (I), or a pharmaceutically acceptable salt, a prodrug, a solvate, or a stereoisomer thereof which is a novel compound exhibiting excellent inhibitory activity against IRAK-4, can be used without side effects for efficient prevention and treatment of diseases mediated by IRAK-4 receptors, particularly autoimmune diseases or lymphomas.

This invention relates to the fields of pesticide formulations and pesticide pest control, specifically to a composite nano-slow-release suspension of emamectin benzoate and chlorantraniliprole, its preparation, and application. The nano-slow-release suspension comprises emamectin benzoate, chlorantraniliprole, a nanocarrier, a wetting agent, a dispersant, a synergist, a thickener, an antifoaming agent, an antifreeze, a preservative, and water. The nanocarrier is an NX-CMCS & MOF composite nanocarrier. Spraying this composite nano-pesticide onto crops improves the adhesion and penetration of the pesticide on leaves, enhances its resistance to rain washout, and effectively kills major crop pests such as bollworms, diamondback moths, cowpea thrips, and rice planthoppers. Compared with traditional pesticide formulations, it has a significant effect of reducing dosage and increasing efficacy, and has broad application prospects in the field of agricultural pest control and promoting green agriculture.

The present invention relates to the technical field of organic synthesis, and specifically to a method for synthesizing Fast Blue BB Salt. The method includes: (1) obtaining 1,4-dibromo-2,5-diethoxybenzene by bromination reaction of 1,4-diethoxybenzene; (2) reacting 1,4-dibromo-2,5-diethoxybenzene with benzamide to obtain N-(4-bromo-2,5-diethoxyphenyl)benzamide; (3) reacting N-(4-bromo-2,5-diethoxyphenyl)benzamide with trifluoroacetamide to obtain N-(2,5-diethoxy-4-(2,2,2-trifluoroacetylamino)phenyl)benzamide; and (4) obtaining Fast Blue BB Salt by hydrolysis of N-(2,5-diethoxy-4-(2,2,2-trifluoroacetylamino)phenyl)benzamide. The method has a short reaction route, mild reaction conditions, and meets the requirements of green and safe development.

The application discloses a kind of deuterated benzamide diazepine compounds and preparation method and purposes thereof, and structure is as shown in general formula I.The compound is used as selective OX2R antagonist, and shows good activity, selectivity, brain exposure, brain blood ratio (the ratio of drug concentration in brain and drug concentration in blood, is called B / P), little toxic side effect, moderate half-life effect etc..It can be used for preventing, treating and / or reducing the disease related to orexin receptor.General formula I

The present invention discloses compounds according to Formula I:wherein R1a, R1b, R1c, R2a, W1, W2, X1, X2, X3, Y, and Z are as defined herein.The present invention relates to compounds, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment using the same, for the prophylaxis and / or treatment of inflammatory diseases, autoinflammatory diseases, autoimmune diseases, proliferative diseases, fibrotic diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformation, diseases involving impairment of bone turnover, diseases associated with hypersecretion of IL-6, diseases associated with hypersecretion of TNFα, interferons, IL-12 and / or IL-23, respiratory diseases, endocrine and / or metabolic diseases, cardiovascular diseases, dermatological diseases, and / or abnormal angiogenesis associated diseases by administering the compound of the invention.

The present invention belongs to the technical field of organic synthesis, and particularly relates to a method for photocatalytic preparation of N-dimercaptobenzamide and its derivatives. The method comprises the following steps: using a compound of formula 1 as a raw material and a compound of formula 2 as a disulfur source, and carrying out a reaction through a photocatalytic system to prepare a compound of formula 3, wherein R<supgt;1< / supgt> and R<supgt;2< / supgt> are each independently selected from an aryl group, an alkyl group or an electron-withdrawing group. The synthesis method of the present invention has simple operation, does not involve metals, has a wide range of applicable reaction substrates, good regioselectivity, high yield, and can greenly and efficiently synthesize a series of novel N-dimercaptobenzamide derivatives, and has broad application prospects in agrochemicals, drug preparation and fluorescent materials.

The present invention relates to use of a pharmaceutical composition for multiple myeloma containing 5-fluoro-2-[(4-{7-[(1S,3S,4R)-5-methylidene-2-azabicyclo[2.2.2]octane-3-carbonyl]-2,7-diazaspiro[3.5]nonan-2-yl}pyrimidine-5-yl)oxy]-N,N-di(propan-2-yl)benzamide.

This application relates to the field of organic chemical synthesis, specifically to a method for synthesizing quinazolinone compounds from carbon dioxide and its preparation. The method uses carbon dioxide, 2-aminobenzamide compounds, and aryl halides as raw materials, and reacts under heating in the presence of a palladium metal catalyst, a ligand, a reducing agent, a base, and an organic solvent to generate quinazolinone compounds. The mechanism is as follows: carbon dioxide forms intermediate A under alkaline and reducing conditions; the aryl halide reacts with intermediate A under the action of a palladium metal catalyst to form a carbonyl metal compound B, which then reacts with the 2-aminobenzamide compound under the action of an alkaline and reducing agent to obtain the quinazolinone compound. This catalyst system is universally applicable to various types of 2-aminobenzamides and their derivatives, as well as aryl halides; the raw materials are widely available, inexpensive, and readily available; and the reaction process is simple and controllable.

The invention relates to an insecticide composition and an application method thereof, the composition comprises an active component A and an active component B. The component A is selected from benzamide compounds represented by a general formula I, and the component B is selected from pyriproxyfen. The composition has the advantages of obvious synergism, resistance delaying and the like, and can be used for preventing and treating various pests.

To provide a compound that expands the spectrum of pesticides.SOLUTION: Provided is a compound represented by formula (b*): (in the formula, E is hydrogen or a C1-C6 alkyl group; A is -CN, chlorine, or fluorine; and L is S, SO, or SO2).SELECTED DRAWING: None

The present application relates to the technical field of chemical medicines, in particular to a pyrimidine compound containing nitrogen methoxy benzamide and a preparation method and application thereof.The present application provides a brand-new pyrimidine compound containing nitrogen methoxy benzamide, which is a brand-new compound newly synthesized.The pyrimidine compound containing nitrogen methoxy benzamide is novel in structure, has good water solubility, has a strong inhibitory effect on tumor cells, and has a good application prospect in the preparation of antitumor drugs.

In some aspects, disclosed herein are compounds of the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions thereof. In some aspects, the compounds and compositions provided herein may be used to modulate the activity of Staphylococcus aureus. Also provided are methods of administering compounds and composition provided herein to a patient in need thereof, for example, for the treatment or prevention of diseases or disorders.

The invention belongs to the technical field of biological medicines, relates to application of a compound 1 in treatment or prevention of diseases related to RET fusion and / or RET mutation, and provides application of N (3-chloro-5 (trifluoromethyl) phenyl) 3 ((6 (4-hydroxypiperidine-1-yl) imidazo [1, 2-a] pyridin-2-yl)-1, 3, 4-triazolo [1, 2, 4] triazolo [1, 2, 4] triazolo [1, 2, 4] triazolo [1, 2, 4 The invention relates to application of (2R, 2R, 2b) pyridazin-3-yl) ethynyl) 2-methylbenzamide or pharmaceutically acceptable salts thereof in treatment or prevention of RET fusion and / or RET mutation related diseases, and application of the (2R, 2R, 2b) pyridazin-3-yl) ethynyl) 2-methylbenzamide or pharmaceutically acceptable salts thereof in treatment or prevention of RET fusion and / or RET mutation related diseases in treatment or prevention of RET fusion and / or RET mutation related diseases by utilizing broad-spectrum and efficient RET inhibition activity, excellent drug-resistant mutation covering ability and higher safety The technical problems of drug resistance, off-target toxicity, high medication frequency and the like of the existing RET inhibitor are solved, and a new effective means is provided for accurate treatment of RET-driven tumors.

A 2-[2-({12,12-dimethyl-4-oxo-6-phenyl-3,11-dioxatricyclo[8.4.0.0,2,7]tetradeca-1,5,7,9-tetraen-8-yl}oxy)acetamido]benzamide compound and related derivatives, as well as the use thereof in the preparation of a medicament for treatment and / or prevention of diseases or disorders associated with the circadian rhythm are provided. The compound of the invention is a CLOCK-binding small molecule and also an inhibitor of CLOCK:BMAL1 interaction, and is therefore useful, as pharmaceutical agent, especially in the treatment and / or prevention of disorders associated with the circadian rhythm.