45 results about "Chloroquinocin" patented technology

The invention discloses a carbonyl reductase derived from Rhodosporidium toruloides ZJB14212, a gene, a vector, a strain and an application of the carbonyl reductase in the preparation of chiral drug intermediates. The above carbonyl reductase can biologically catalyze preparation of highly optically pure (S)-N,N-dimethyl-3-hydroxy-3-(2-thienyl)propionamide, (S)-N-methyl-3-hydroxy-3-(2-thienyl)propionamide, (R)-3-chloro-1-(2-thienyl)1-propanol, ethyl (S)-3-hydroxy-3-(2-thienyl)propanoate, (S)-3-hydroxy-3-(2-thienyl)propionitrile, tert-butyl 6-chloro-(3R,5S)-dihydroxyhexanoate, (4S)-3-[(5S)-5-(4-fluorophenyl)-5-hydroxyvaleryl]-4-phenyl-1,3-oxazolidine-2-one and methyl [S-(E)]-2-[3-[3-[2-(7-chloro-2-quinolyl)vinyl]phenyl]-3-hydroxypropyl]benzoate.

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.

Organometallic compounds comprising a chloroquinoline moiety and uses the compounds. The compounds are, for example, manganese or rhenium complexes of a ligand comprising a chloroquinoline moiety. The compounds can be used in, for example, methods of inhibiting cell growth.

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 the field of herbicides, in particular to a preparation method of 7-chloro-8-quinoline carboxylic acid, the method comprising the following steps: 1) dissolving N-hydroxyphthalimides as a catalyst In the reaction liquid of compound and azobisisobutyronitrile, with oxygen as oxidant, 7-chloro-8-methylquinoline is oxidized to obtain 7-chloro-8-quinoline carboxylic acid; 2) the oxidation of step 1) The product is separated into solid and liquid to obtain a solid phase and a reaction liquid phase. Through the method of the invention, the production of a large amount of waste acid and waste water in the synthesis process can be avoided, and the reaction liquid phase can be recovered and used mechanically.

The present invention relates to the technical field of compound synthesis, and discloses a 4, 7-dichloroquinoline synthesis purification method, which comprises: S1, primary reaction: adding 7-chloro-4-hydroxyquinoline into 300 g of toluene, sequentially adding DMF and triphenylphosphine oxide, starting stirring, internally heating to a temperature of 79-90 DEG C, slowly adding phosphorus oxychloride or a toluene solution of phosphorus oxychloride in a dropwise manner, after the dropwise adding is completed, carrying out a reaction for 2-3 h, and cooling to a room temperature to obtain the 4, 7-dichloroquinoline. Continuously reacting until the TLC monitoring reaction is finished; s2, performing reduced pressure distillation, namely performing reduced pressure distillation on the reaction liquid in the S1. The method has the advantages of simple operation, high yield, no use of any reagent in the purification process, no introduction of new impurities, no special requirements on equipment, no environmental pollution, no introduction of an organic solvent, no pollution, and easy 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 invention relates to a method for synthesizing 3,7-dichloro-8-quinolineformyl chloride. Under the condition that no solvent exists, 3,7-dichloro-8-quinolinic acid, monochloroacetyl chloride and a catalyst The acylation reaction is carried out at 95°C-120°C, after filtration, washing and distillation under reduced pressure, the compound represented by formula I is obtained, and the specific synthetic route is as follows. In the process of the reaction, a catalyst is used, no solvent needs to be added, the source of raw materials is easily available, the cost is low, the process steps are few, the reaction conditions are mild, no special equipment is required, the product quality is good, the purity is high, and the yield is higher than 95%, No waste water and waste gas, relatively safe and environmentally friendly.

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.