45 results about "Chloroquinocin" patented technology

The invention provides an industrial production method for hydroxychloroquine sulfate, which includes the following steps: enabling 4.7-dichloroquinoxaline and 5-(N-ethyl-N-ethoxyl)-2-amino pentane to react under gas shield for 13-24 h at a gradually increased temperature of 120-130 DEG C to obtain hydroxychloroquine; preparing the hydroxychloroquine sulfate after the reaction between the hydroxychloroquine and an alcohol sulfate solution at the temperature of 20-30 DEG C. According to the method, the yield of the obtained crude product of the hydroxychloroquine is not smaller than 85%, the yield of the obtained hydroxychloroquine sulfate is not smaller than 85%, the yield of the obtained hydroxychloroquine sulfate HPLC is not smaller than 99.5%, the yield of single impurity is not larger than 0.1%, so that requirements of United States Pharmacopeia is met; the novel method is simple in procedure, is environment-friendly and easy in industrial production.

The invention discloses a processing technology of a non-hormonal anti-inflammatory drug intermediate, which is based on 2-(3-(3-(2-(7-chloro-2-quinolyl)vinyl)phenyl)- (3-carbonyl) propyl) methyl benzoate, ketone reductase, triethanolamine buffer solution, isopropanol and toluene are raw materials, add cofactor aqueous solution reaction, reaction solution obtains target product through water and ethanol crystallization treatment, process of the present invention Simple, low cost, high product purity, and basically zero pollution in chemical reactions.

The invention discloses a method for preparing N-(5-chloro-8-quinolyl) benzamide compounds by using an electrochemical microchannel reaction device. The 8-(benzoylamino) quinoline compounds are dissolved in The first organic solvent is made into reaction solution A; dichloromethane and copper acetate are dissolved in the second organic solvent to make reaction solution B; reaction solution A and reaction solution B are pumped into the electrochemical microchannel reaction device simultaneously respectively Mix in a micro-mixer, then flow into a micro-reactor for reaction, and obtain the product. Compared with the prior art, the present invention does not need traditional oxidants, and creatively develops a new method for the electrocatalytic selective preparation of chloroquinolines using dichloromethane as a chlorination reagent microflow field; at the same time, the present invention utilizes The microchannel reaction device greatly shortens the reaction time, improves the reaction conversion rate, and significantly increases the yield to 85%.

Selective enrichment media and methods for selectively growing and detecting Salmonella spp. and / or Shiga toxin-producing E. coli. The media may comprise a carbon and nitrogen source, an inorganic salt, a fermentable sugar, one or more selective agents, and an efflux pump inhibitor. Various selective agents include sulfa drugs, surfactants, aminocoumarins, cycloheximide, supravital stains, ascorbic acid, bromobenzoic acid, myricetin, nitrofurantoin, rifamycins, polyketides, and oxazolidinones. Various efflux pump inhibitors include arylpiperazines, such as 1-(1-naphthylmethyl)piperazine, and quinoline derivatives, such as 4-chloroquinoline. Methods of selectively growing and detecting Salmonella and / or Shiga toxin-producing E. coli are provided.

The invention relates to the technical field of organic chemistry, in particular to a chloroquine photoaffinity molecular probe and a preparation method and application thereof. The provided preparation method takes 1,4-dibromopentane as a raw material, and obtains N-(4-((7-chloroquine through a series of nucleophilic substitution, hydrogenation reaction, reduction reaction, amidation reaction, click reaction and the like. olin-4-yl)amino)pentyl)-N-ethyl-5-(4-((2-(3-(2-(prop-2-alkyn-1-propoxy)ethyl)-3H -Diazine-3-yl)ethoxy)methyl)-1H-1,2,3-triazol-1-yl)pentanediamine, i.e. chloroquine photoaffinity molecular probe; On the basis of , the structure was modified, and the photo-affinity diazide and alkynyl groups were introduced to obtain the probe. To achieve the purpose of visualization, enrichment and identification of target proteins, the obtained chloroquine photoaffinity molecular probe has a wide range of applications.

The invention discloses a quinoline formamide compound and a preparation method thereof and an application of an anti-enterovirus type 71 (EV71), and belongs to the technical field of medicine. Specifically, 2-chloroquinoline-4-formamide derivative and an alcohol compound are subjected to a substitution reaction, so that a series of quinoline formamide compounds are prepared. The quinoline formamide compounds have the activity of resisting enterovirus type 71, have small toxicity to cells, can be developed as a new anti-EV 71 drug, and have a wide application prospect.

The invention relates to a preparation method of 4,7-dichloroquinoline in the technical field of medicine, which uses 2-amino-6-chlorobenzoic acid (I) as a starting material, and ethoxymethine in an organic solvent Diethyl malonate (II) undergoes condensation reaction to obtain (Ⅲ), III undergoes cyclization, hydrolysis, and acidification to obtain hydroxyquinoline dicarboxylic acid (V), V undergoes high-temperature decarboxylation to obtain hydroxyquinoline (VI), and VI undergoes Chlorination of phosphorus oxychloride gives 4,7-dichloroquinoline. The 4,7-dichloroquinoline prepared by the method of the present invention does not have the isomer 4,5-dichloroquinoline, and the temperature of the condensation reaction under the catalysis of the catalyst is low, which improves the yield of the reaction and avoids the generation of impurities , and reduce energy consumption, improve the economic benefits of the product.

The invention discloses a process for preparing Quinclorac artificial semiantigen, artificial antigen, specific antibody and use thereof, wherein the preparation comprises, subjecting the dichloroquine (3,7-dichlorine-8-quinoline carboxylic acid) to sulfoxide chlorinated acylation, reacting with reanal and aminocaproic acid, thus obtaining semiantigen 4-(3,7-dichlorine-8-quinolineformyl) reanal or 6-(3,7-dichlorine-8-quinolineformyl) aminocaproic acid (QB or QC).

The invention provides a preparation method of a disubstituted 4-chloroquinoline-3-carbonitrile derivative and a preparation method of bosutinib. The preparation method of the disubstituted 4-chloroquinoline-3-carbonitrile derivative comprises the following steps: disubstituted o-nitrobenzoate (II) used as a raw material and acetonitrile are condensed under the action of an alkali to obtain a compound of formula III; the compound of formula III and a chloroformylating reagent undergo a chloroformylating reaction to obtain a compound of formula IV1 or formula IV2; and the compound of formula IV1 undergoes catalytic hydrogenation cyclization in the presence of a hydrogenation catalyst to prepare 7-[3-(4-methyl-1-piperazinyl)propoxy]-6-methoxy-4-chloroquinoline-3-carbonitrile (Ia), or the compound of formula IV2 is subjected to catalytic hydrogenation cyclization and anhydride amidation to prepare 6-acetamido-7-ethoxy-4-chloroquinolin-3-carbonitrile (Ib). The compound of formula Ia or Ibis used to prepare bosutinib, neratinib or pelitinib. The method of the invention has the advantages of short process flow, simplicity in operation, easiness in realization, low cost, few three wastes, high yield, high purity, and easiness in industrial production.

The present invention relates to a kind of 3-[(7-chloroquinoline-4-amino)butylamino]-7-substituted-benzo[e][1,2,4]triazine- 1‑Oxygen derivatives, their pharmaceutically acceptable salts, esters, solvates: R 1 selected from hydrogen, hydroxyl, C 1 -C 6 Alkyl, fluorine, chlorine and bromine; R 2 selected from hydrogen, C 1 -C 12 Alkyl or hydroxyl; R 3 selected from hydrogen, C 1 -C 12 Alkyl or hydroxyl. The present invention also provides a composition comprising 3-[(7-chloroquinoline-4-amino)butylamino]-7-substituted-benzo[e][1,2, 4] Triazine‑1‑oxygen derivatives, their pharmaceutically acceptable salts, esters, solvates and pharmaceutically acceptable excipients: wherein, R 1 selected from hydrogen, hydroxyl, C 1 -C 6 Alkyl, fluorine, chlorine or bromine; R 2 selected from hydrogen, C 1 -C 12 Alkyl or hydroxyl; R 3 selected from hydrogen, C 1 -C 12 Alkyl or hydroxyl. The present invention also claims protection of 3-[(7-chloroquinoline-4-amino)butylamino]-7-substituted-benzo[e][1,2,4]triazine-1-oxygen derivatives, and its pharmaceutical The application of acceptable salts, esters and solvates in the preparation of tumor therapeutic drugs.

The object of the present invention is to provide a more efficient method for synthesizing cabozantinib, which uses 6-nitroveratraldehyde as a starting material, and completes reduction, cyclization, and hydrolysis reactions in one pot to obtain 6,7- Dimethoxy-2-carboxy-quinoline, then treated with thionyl chloride to obtain 6,7-dimethoxy-2-carboxy-4-chloro-quinoline, and finally again under copper catalyst system conditions The kettle method completes the condensation and decarboxylation reactions to obtain the target product cabozantinib.