327 results about "Benzamide" patented technology

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.

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 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 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 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.

The present disclosure relates to a fungicidal combination comprising at least one Pyridinyl-ethyl-benzamide fungicide, at least one triazole fungicide, and at least one dithiocarbamate fungicide The present disclosure also relates to a fungicidal composition comprising the fungicidal combination and at least one agrochemically acceptable excipient. Additionally, the present disclosure relates to a method for controlling growth of fungal disease in a plant, the method comprising applying a fungicidal composition comprising the fungicidal combination to the plant, or a locus, or a plant propagation material thereof.

The application belongs to the technical field of pesticide synergists, and discloses a use of an amide compound as a pesticide synergist. The application takes CYP6AE48 of Spodoptera litura as a main target, adopts a method combining computer-aided drug design technology and biological effect screening, and screens an amide compound, which is N-{5-[2-(2-{3-[2-(2-methylphenoxy)ethoxy]benzyl}hydrazino)-2-oxoethyl]-1,3,4-thiadiazol-2-yl}benzamide. It is known through experiments that the compound has a good inhibitory effect on CYP6AE48 of Spodoptera litura, can prevent degradation of lambda-cyhalothrin and chlorantraniliprole, and can play a synergistic effect as a pesticide synergist in pest control.

The invention belongs to the technical field of organic matter preparation, and provides an isoxazoline compound containing benzamide as well as a preparation method and application thereof.Chemical modification and molecular design are performed on a compound with an isoxazoline structure, a substituent group is introduced to N of an amide group, and the benzamide-containing isoxazoline compound is prepared. A series of high-efficiency compounds which can be used for killing insects or mites in agriculture or forestry and have excellent activity are obtained, and particularly, the compounds have very good biological activity on pests of lepidoptera, hemiptera and the like. When being used at an extremely low concentration, the compound disclosed by the invention also shows an excellent control effect on various pests or pest mites, has insecticidal or acaricidal activity in each stage (such as eggs, larvae (nymphs), pupae and adults) of the life cycle of the pests or pest mites, and has an excellent control effect on the pests or pest mites which have drug resistance to traditional insecticides or acaricides. And the composition also shows excellent control activity.

The invention discloses a synthesis method of a high-purity and high-yield antihypertensive drug, and relates to the technical field of medical chemistry. The method comprises the following steps: taking glycollic acid as an initial raw material, and carrying out acylation to obtain glycollic acid acyl chloride; carrying out Friedel-Crafts reaction on the 2-hydroxyl-5-(2-hydroxyacetyl) benzamide and salicylamide to obtain 2-hydroxyl-5-(2-hydroxyacetyl) benzamide; then, a Dess-Martin oxidizing agent is used for oxidation, and 2-hydroxy-5-(2-oxoacetyl) benzamide is obtained; the preparation method comprises the following steps: taking 2-hydroxyl-5-((4-phenylbutylamine-2-yl)-ethyl) benzamide as a raw material, then carrying out reductive amination on the 2-hydroxyl-5-(4-phenylbutylamine-2-yl)-ethyl) benzamide and 1-methyl-3-phenylpropylamine under the condition that sodium borohydride is taken as a reducing agent to obtain 2-hydroxyl-5-(1-hydroxyl-2-((4-phenylbutylamine-2-yl)-amino) ethyl) benzamide, namely And finally salifying with concentrated hydrochloric acid, crystallizing and separating to obtain the labeolol hydrochloride. The method is novel in route, convenient to operate, high in product total yield, high in purity, capable of effectively avoiding generation of dibromo impurities and suitable for large-scale production.

The present application belongs to the technical field of pesticides, and particularly relates to an insecticidal composition containing an isoxazoline-substituted benzamide compound and application thereof. The insecticidal composition contains active ingredient A and active ingredient B, wherein the active ingredient A is oxadiazylfluazaim or the active ingredient B is one or more selected from the following compounds: fluoromethane sulfide, pyridaben and fluoromethane bisether. The composition has reasonable components, good insecticidal effect, low pesticide cost, and the characteristics of reducing the application amount, being safe to crops, reducing the amount of pesticide residues, etc.

The present invention relates to an improved process for the preparation of benzamide compound. More particularly, the present invention relates to an improved process for the preparation of Fluopyram of Formula (VI).

The application belongs to the technical field of chemical medicine raw materials, and particularly relates to a benzamide piperazine derivative, a preparation method and application thereof. The structure of the compound is shown as formula I. It is verified through experiments that the compound provided by the application has good TRPC6 channel inhibition effect, and the compound provided by the application is a novel TRPC6 channel small molecule inhibitor in structure, which lays a foundation for the development of a drug for treating or preventing diseases related to TRPC6 channel-mediated calcium ion influx abnormalities.

The present disclosure relates, in part, to SARS-CoV-2 papain-like protease (PLpro) inhibitor compounds of Formula (I), pharmaceutical compositions thereof, and methods of using the same for promoting an antiviral effect in a subject and / or treating, preventing, and / or ameliorating a viral infection in a subject:

The invention relates to the technical field of organic synthesis, in particular to a method for preparing 4-nitro-N-phenylbenzamide by a one-pot process, which comprises the following steps: under the protection of inert gas, adding an inert solvent, p-nitrobenzoic acid and a composite catalyst into a reactor, and heating to dissolve, the composite catalyst comprising NFM and TPPO; slowly adding thionyl chloride into a reaction system for acylation reaction; then slowly adding aniline into the reaction system to carry out condensation reaction; and after the reaction is finished, carrying out post-treatment to obtain the 4-nitro-N-phenylbenzamide. According to the method, one-pot reaction can be realized, and high-risk intermediates do not need to be separated. In the composite catalyst, NFM efficiently catalyzes acylating chlorination, and TPPO stabilizes an acyl chloride intermediate and promotes condensation, so that the reaction is performed efficiently, stably and highly selectively, and the product is high in yield and purity. And the catalyst is easy to recycle, and the process is green, safe, economical and suitable for industrial production.

The present disclosure relates to a process for the preparation of Acarrabutinib. The present disclosure relates generally to an improved process for the preparation of 4-{8-amino-3-[(2S)-1-(butyl-2-alkynol) pyrrolidin-2-yl] imidazo [1, 5-a] pyrazin-1-yl}-N-(pyridin-2-yl)-benzamide, in particular to an improved process for the preparation of 4-{8-amino-3-[(2S)-1-(butyl-2-alkynol) pyrrolidin-2-yl] imidazo [1, 5-a] pyrazin-1-yl}-N-( The present invention relates to a large scale process for the manufacture of 4-{8-amino-3-[(2S)-1-(butyl-2-alkynol) pyrrolidin-2-yl] imidazo [1, 5-a] pyrazin-1-yl}-N-(pyridin-2-yl) benzamide, and intermediates employed in such processes.

The invention belongs to the technical field of medicine detection methods, and particularly relates to a quantitative detection method for an antiviral drug in a biological sample. According to the present invention, the antiviral drug is 2-(((1S, 5S)-5-hydroxyadamantane-2-yl) amino)-4-(3, 6, 6-trimethyl-4-oxo-4, 5, 6, 7-tetrahydro-1H-indazole-1-yl) benzamide, and the drug is subjected to quantitative analysis by using a liquid chromatography-mass spectrometry detection method, the detection method is strong in specificity and high in accuracy, the in-vivo and in-vitro absorption, distribution, metabolism and excretion conditions of the medicine and the in-vivo and in-vitro targeted treatment effect of the medicine are determined by measuring the content of the medicine in a biological sample, and the detection method is beneficial to promoting medicine development, determining the pharmacokinetic condition of the medicine and assisting medicine toxicology evaluation.

Crystalline 4-chloro-N-(4-(morpholinomethyl)phenyl)benzamide, crystalline 4-chloro-N-(4-(morpholinomethyl)phenyl)benzamide hydrochloride, methods of preparing the crystalline compounds, pharmaceutical compositions containing the crystalline compounds, and methods of treatment using the crystalline compounds are disclosed.