185 results about "Ethoxidine" patented technology

The present invention relates to a process for the preparation of (4S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide of formula (I) and to the preparation and use of crystalline modification I of (4S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide of formula (I).

The invention discloses a molecular sieve catalyst for synthesizing methyl ethyl carbonate by a transesterification method and a regeneration method, and relates to the technical field of molecular sieve catalysts, the molecular sieve catalyst comprises a microporous double-active-center inner core and an amphoteric mesoporous shell; the microporous double-active-center core takes the X-type zeolite as a carrier to load potassium, cesium, lanthanum and barium; the amphoteric mesoporous shell is an MCM-41 and SBA-15 composite mesoporous silica layer coating the outer part of the inner core and has a double-mesoporous structure, amino propyl triethoxy silane and carboxyethyl triethoxy silane are grafted on the surface of the amphoteric mesoporous shell, and zirconium and titanium are co-doped. According to the invention, collaborative optimization of active centers and mass transfer channels is realized through a core-shell structure of a microporous double-active-center core and an amphoteric mesoporous shell. The activity and selectivity of catalytic transesterification are remarkably improved by the microporous core; due to the double-mesoporous structure and surface functional modification of the amphoteric mesoporous shell, the mass transfer efficiency of reactants and products is improved, and the adaptability of the catalyst to a reaction system is enhanced.

The application relates to the technical field of chemical synthesis, in particular to a synthesis method of a key intermediate of pentconazole, which comprises the following steps: S1, Witting-Horner reaction of 2,4-dichlorobenzophenone and (diethoxy) phosphoethyl acetate under the action of a strong base to generate 3-(2,4-dichlorophenyl)-2-en-hexanoic acid ethyl ester; S2, Prilezhaev epoxidation reaction of 3-(2,4-dichlorophenyl)-2-en-hexanoic acid ethyl ester and meta-chloro peroxybenzoic acid to generate 3-(2,4-dichlorophenyl)-2,3-epoxy-hexanoic acid ethyl ester; and S3, base hydrolysis and acidification of 3-(2,4-dichlorophenyl)-2,3-epoxy-hexanoic acid ethyl ester to obtain a key intermediate 2-(2,4-dichlorophenyl) pentanal of pentconazole. The application has the effects of higher reaction yield, lower toxicity of reaction raw materials and more gentle reaction conditions.

Disclosed in the present invention is a monodisperse nanocalcium carbonate-based foliar calcium fertilizer, comprising the following raw materials in parts by mass: 1-20 parts of a monodisperse nanocalcium carbonate filter cake, 0.05-0.9 parts of ethoxy-modified polytrisiloxane, 0.01-0.8 parts of modified casein, 0.01-0.8 parts of an enzyme, 0.05-0.9 parts of a sugar alcohol, and 10-180 parts of water. After being diluted by means of water such that the solid content of calcium carbonate is 0.5-2%, the foliar calcium fertilizer is used for foliar calcium supplementation of various crops and fruit and vegetable crops. The novel foliar calcium fertilizer is safe and non-toxic, can be directly sprayed onto foliar and fruit surfaces of crops and fruits and vegetables, effectively ensures calcium absorption and utilization in crops, achieves the effect of increasing yield and increasing income, and can also improve the yield of fruits and vegetables.

The application discloses a preparation method of a key intermediate of dapagliflozin, and belongs to the technical field of preparation of medical intermediates. The preparation method of the key intermediate of dapagliflozin comprises the following steps: 1, 1-ethoxy-4-methylbenzene is prepared by using p-cresol, sodium hydroxide and diethyl sulfate; 2, (4-ethoxybenzyl) phenyl sulfide is prepared by using 1-ethoxy-4-methylbenzene, thiophenol, a palladium catalyst, an alkali and an oxidant; 3, 1-benzyl-4-ethoxybenzene is prepared by using (4-ethoxybenzyl) phenyl sulfide under a hydrogen atmosphere; 4, 4-ethoxy-2'-chlorobenzhydrol is prepared by carrying out chlorination reaction on 1-benzyl-4-ethoxybenzene; and 5, 5-bromo-2-chloro-4'-ethoxybenzhydrol is prepared by carrying out bromination reaction on 4-ethoxy-2'-chlorobenzhydrol. The yield and purity of 5-bromo-2-chloro-4'-ethoxybenzhydrol prepared by the method are higher, the process is safer, and the production cost is reduced.

The invention discloses a synthesis method of 4-bromo-3-(ethoxymethyl) benzoic acid, which comprises the following steps: (1) activating carboxyl of p-bromobenzoic acid serving as a raw material in the presence of an organic anhydride activator, and then performing chloromethylation reaction with paraformaldehyde in the presence of a chlorine-containing Lewis acid catalyst to obtain 4-bromo-3-(ethoxymethyl) benzoic acid; after the reaction is completed, carrying out post-treatment to obtain an intermediate 4-bromo-3-(chloromethyl) benzoic acid; and (2) carrying out nucleophilic substitution reaction on the intermediate obtained in the step (1) in ethanol under the action of inorganic alkali to prepare the target product 4-bromo-3-(ethoxymethyl) benzoic acid. According to the invention, through one-pot activation and chloromethylation of p-bromobenzoic acid, concise, efficient and highly economical synthesis from cheap raw materials to the sparsentan key intermediate is realized.

This invention discloses a yam oxylipoic acid compound with aromatase inhibitory activity, its application, and analytical identification methods, belonging to the field of medicinal chemistry. The yam oxylipoic acid compound is (Z)-9-ethoxy-6,10-dihydroxyoctadec-7-enoic acid, a novel compound. This compound can significantly inhibit aromatase activity and possesses the ability to inhibit excessive estrogen production, thus showing promising application prospects and value in diseases related to estrogen imbalance regulation.

Disclosed is a method for preparing oxetan-2-ylmethanamine, which belongs to the field of organic synthesis. [2-(1-ethoxyethoxy)methyl]propylene oxide is used as an initial raw material, and reacted in the presence of potassium tert-butoxide and trimethylsulfoxonium iodide; the resulting product is reacted with a sulfonyl compound and triethylamine; the resulting product is reacted with a compound of phthalimide; the resulting product is reacted with an amino group-containing compound, to obtain oxetan-2-ylmethanamine. The method according to the disclosure allows for an overall yield of not less than 30% in scale-up production (kilogram level), which is higher. Moreover, compared with the traditional method for preparing oxetan-2-ylmethanamine, a palladium-carbon catalytic hydrogenation step is not required, and dangerous chemical-sodium azide is not required in the method according to the disclosure. Thus, the method has high safety, low production cost, simple operations, and thereby is suitable for industrial production.

The invention relates to the technical field of chemical synthesis, and particularly discloses a compound with a peculiar smell removing function as well as a preparation method and application thereof. The chemical name of the compound is 2-ethoxy-3-((E)-methoxy-3-oxopropyl-1-alkene-1-yl) phenyl cinnamate, the smell of the compound is extremely light, sulfur-containing and nitrogen-containing compounds causing stink can be captured through a Michael addition reaction, and efficient peculiar smell removal is achieved. The preparation method comprises the following steps: (1) taking cinnamic acid as an initial raw material, and reacting with diethylamino sulfur trifluoride to prepare cinnamic acid acyl fluoride; (2) carrying out an esterification reaction on the cinnamic acid acyl fluoride and 2-methoxy-3-hydroxybenzaldehyde in the presence of 4-dimethylaminopyridine, so as to obtain 2-methoxy-3-formyl phenyl cinnamate; and (3) carrying out Wittig reaction on the 2-methoxy-3-formyl phenyl cinnamate and a phosphorus ylide reagent, so as to obtain the target compound.

This invention relates to a method for preparing the fenelone intermediate 2-cyanoethyl(4S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthidine-3-carboxylic acid ester, and also relates to diastereomeric salts (Va), (Vb), (Vc), and / or (Vd). This method is simple to operate, and the diastereomeric salts can be obtained with very high chemical and enantiomeric purity (tartrate ester content <0.05%) through a single dissociation, avoiding the raw material loss and waste problems caused by multiple dissociations. It also has low production costs and meets the requirements of green production.

The invention discloses a hydrophobic Zr-doped SiO2 (at) APTES-T composite aerogel desulfurization adsorbent as well as a preparation method and application of the hydrophobic Zr-doped SiO2 (at) APTES-T composite aerogel desulfurization adsorbent. The preparation method comprises the following specific steps: dissolving thiophene in n-heptane to form a non-polar template solution, and adding the non-polar template solution into a polar mixed solution of ZrOCl2, methyltriethoxysilane and 3-aminopropyltriethoxysilane, wherein water and ethanol serve as solvents of the ZrOCl2, the methyltriethoxysilane and the 3-aminopropyltriethoxysilane; the non-polar template solution is stirred in the polar solution to form uniform tiny liquid drops. The preparation method comprises the following steps: carrying out a hydrolysis-polymerization reaction on a mixed solution to form hydrophobic Zr-doped SiO2 (at) APTES-T alcogel, carrying out aging, replacement and drying steps to obtain the hydrophobic Zr-doped SiO2 (at) APTES-T composite aerogel desulfurization adsorbent, and applying the hydrophobic Zr-doped SiO2 (at) APTES-T composite aerogel desulfurization adsorbent to adsorption removal of thiophene compounds in simulated aromatic hydrocarbons. Results show that the desulfurization adsorbent disclosed by the invention has good adsorption performance on thiophene sulfides in aromatic hydrocarbons, has excellent performance of resisting competitive adsorption of polar impurities, and has good application prospects in the field of deep desulfurization.

The invention belongs to the technical field of medicine synthesis, and particularly relates to a method for efficiently preparing cyclobutane derivatives. Comprising the following steps: dissolving 4-chloro-7H-pyrrolo [2, 3-d] pyrimidine and chloromethyl pivalate in 1, 4-dioxane, and adding an acid binding agent for reaction to obtain a reaction solution; the preparation method comprises the following steps: adding 1-(1-ethoxyethyl)-4-pyrazol boronic acid pinacol ester, purified water, a catalyst and an acid-binding agent into a reaction kettle, carrying out Suzuki reaction, separating liquid, adding activated carbon into an upper organic phase for decoloration, adding an organic solution containing hydrogen chloride for crystallization, and filtering to obtain a wet product; and dissolving the wet product and 2-[1-(ethylsulfonyl)-3-azacyclobutane] acetonitrile in 1, 4-dioxane, and reacting under an alkaline condition to obtain the cyclobutane derivative. According to the preparation method, synthesis is performed through a one-pot four-step reaction, a solvent only relates to 1, 4-dioxane and water, and post-treatment is simple, convenient and efficient.

The present invention relates to an isoindoline compound containing a phenylethoxyalkyleneamine structure, a conjugate thereof, and use thereof. The isoindoline compound containing a phenylethoxyalkyleneamine structure has a structure represented by formula (I). The conjugate thereof has a structure represented by formula (B). The compound of the present invention exhibits increased proliferation inhibition activity for cancer cells and a degradation effect on proteins such as GSPT1, demonstrating practical values.

The invention provides a novel economical and practical method for preparing the quetiapine key intermediate 1-[2-((2-hydroxy ethyoxyl) ethyoxyl) ethyl] piperazine hydrochloride.

The application discloses a method for preparing N-ethoxyl oxalyl alanine ester by using a dynamic tubular reactor, which comprises the following steps: (1) reacting L-alanine, diethyl oxalate and 4-dimethylaminopyridine in the dynamic tubular reactor; (2) removing light components from the reaction solution; (3) reacting the reaction solution after removing the light components and ethanol in the dynamic tubular reactor; and (4) obtaining N-ethoxyl oxalyl alanine ester after removing the light components. Compared with traditional kettle reactors and tubular reactors, the method adopts the dynamic tubular reactor to prepare N-ethoxyl oxalyl alanine ester, and through the regulation of reaction parameters, the selectivity of key by-products N-oxamide and double N-oxamide can be effectively controlled below 2%. The process has the advantages of high reaction yield, high degree of continuous operation, significantly shortened reaction time and no use of high-toxicity materials such as benzene.

This invention discloses a green synthesis process for 2-chloropyranose-1-yl)-4'-ethoxydiphenylmethane, belonging to the field of pharmaceutical intermediate preparation. The method involves forming a mixture of a substrate in the protected state of Formula I and a reducing agent containing siloxane bonds, which is continuously fed into a microreactor loaded with a confined-domain MOF (Metal-Oxide-Fractions) supported catalyst for room-temperature reduction. The MOF catalyst has a rigid pore size of 1.2~2.5 nm and internally coordinates and anchors metal trifluoromethanesulfonate. This invention utilizes the limiting confinement effect of rigid channels to lock the substrate conformation, blocking the surface attack of reactants and achieving extremely high configuration selectivity. Simultaneously, the efficient mass transfer of the continuous flow microchannel and the online infrared spectroscopy closed-loop control system completely eliminate the need for traditional cryogenic conditions, remove highly corrosive fluorine-containing waste liquid, significantly reduce synthesis costs, and achieve efficient, green, and stable continuous industrial production of this core intermediate.

The invention discloses a glyphosate soluble concentrate and a preparation method, and the glyphosate soluble concentrate comprises the following raw material components in parts by weight: 30-40 parts of glyphosate, 10-15 parts of isopropylamine, 8-12 parts of a composite synergist, 2-3 parts of an anti-freezing agent, 0.05-0.1 part of a pH regulator, 2-3 parts of an additive, 0.1-0.5 part of a defoaming agent, 1-2 parts of a loading agent and 40-50 parts of water. Compared with the prior art, the glyphosate soluble concentrate prepared by the invention has the advantages that the propoxylated quaternary ammonium salt and the ethyoxyl alkyl phosphate are mixed according to a certain mass ratio to form the synergist, so that the pesticide effect of glyphosate is remarkably improved. Meanwhile, the aluminum pillared clay is introduced to load the glyphosate and is cooperatively used with the polydopamine-sodium alginate compound, so that the prepared glyphosate soluble concentrate has relatively high leaf deposition rate and rain wash resistance and also has excellent ultraviolet resistance.

The invention relates to a synthesis method of 4-(4-cyano-2-methoxyphenyl)-5-ethoxy-1, 4-dihydro-2, 8-dimethyl-1, 6-naphthyridine-3-formamide, which comprises the following four steps: carrying out a Knoevenagel condensation reaction, carrying out a Hantzsch dihydropyridine synthesis method, carrying out an O-ethylation reaction and carrying out a deprotection reaction to synthesize the 4-(4-cyano-2-methoxyphenyl)-5-ethoxy-1, 4-dihydro-2, 8-dimethyl-1, 6-naphthyridine-3-formamide, and carrying out a reaction to obtain the 4-(4-cyano-2-methoxyphenyl)-5-ethoxy-1, 4-dihydro-2, 8-dimethyl-1, 6-naphthyridine-3-formamide. The preparation method of the 4-(4-cyano-2-methoxyphenyl)-5-ethoxy-1, 4-dihydro-2, 8-dimethyl-1, 6-naphthyridine-3-formamide has the advantages that the selectivity is high, the post-treatment is simple, the yield and the purity of the product are high, a new synthesis route and method are developed for synthesizing the 4-(4-cyano-2-methoxyphenyl)-5-ethoxy-1, 4-dihydro-2, 8-dimethyl-1, 6-naphthyridine-3-formamide, the amplified production is conveniently realized, and the method is suitable for industrial production. The method has good application potential and research value.

This invention discloses a yam component with α-glucosidase inhibitory activity, its application, and analytical identification methods, belonging to the field of medicinal chemistry. The yam component is (Z)-6-ethoxy-9,10-dihydroxyoctadecano-7-enoic acid, a novel compound extracted from yam, exhibiting excellent α-glucosidase inhibitory activity, thus showing promising application prospects and value in lowering blood sugar.

The present application relates to a preparation method of cyprosulfamide, and the cyprosulfamide is prepared by using a one-pot method, and the method specifically comprises the following steps: adding an organic base, a reaction solvent, 2-chloro-3-(2,2,2-trifluoroethoxy)methyl-4-methylsulfonylbenzoic acid and a Curtius condensing agent into a reaction container, heating and refluxing for 3-5 h to generate an active ester intermediate; after the reaction solution containing the active ester intermediate is cooled, 1,3-cyclohexanedione and acetone cyanohydrin are added to perform a condensation rearrangement reaction, and cyprosulfamide is generated. The one-pot synthesis process is adopted, the use of dimethyl sulfoxide is avoided, compared with a traditional process, the method is green, environmentally friendly, has low safety risks, has high yield and good purity, and is more suitable for industrialized production.

The presently claimed invention relates to an alkaline composition for cleaning a substrate comprising i) copper or copper alloy and ii) cobalt or cobalt alloy, the composition comprising: a) at least one pH adjustor selected from diglycolamine, 4,4-diethoxy-N,N-dimethyl-1-butanamine, 3-dimethylaminopropan-1-ol, dimethylaminoethoxyethanol, N,N-dimethylisopropanolamine, ethylethanolamine, N-methyldiethanolamine, 2-(2-(methylamino)ethoxy)ethanol, 3-(methylamino)propane-1,2-diol, 2-[2-[2-(2-methoxy- ethoxy)ethoxy]ethoxy]ethylamine, 2-[2-(2-aminoethoxy)-ethoxy]-ethanol, N-butyldiethanolamine, diisopropanolamine, N-methyldiisopropanolamine, monoethanolamine, 3-dimethylamino-1,2-propandiol, 2- amino-1-butanol, 2-(2-(2-(2-aminoethoxy)ethoxy)ethoxy)ethanol, prolinol, 1-methyl-2-pyrrolidinemethanol, 1-methyl-2-pyrrolidinemethanol, 1-methyl-3-pyrrolidinol, 2-amino-2-methyl-1-propanol, N,N-dimethylethanolamine, butylethanolamine, diethylethanolamine, 3-methoxypropylamine, 4-(2-hydroxyethyl)morpholine, 4-(dimethylamino)cyclohexanol, 2-amino-2-methyl-1, 3-propanediol, or diisopropylamine; b) at least one complexing agent selected from C2 to C12 hydrocarbon having at least two sulfonic acid or carboxylic acid groups; c) at least one polymeric dispersing agent having a weight average molecular weight ≥ 1000 g / mol; and d) a solvent comprising water.

The present application provides methods for preparing (R)-4-(3-((S)-1-(4-amino-3-methyl-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-5-chloro-2-ethoxy-6-fluorophenyl)pyrrolidin-2-one, which is useful as a phosphoinositide 3-kinase-delta (PI3Ks) inhibitor, as well as salt forms and intermediates related thereto.

The invention provides a novel method for obtaining (4)-(4-cyano-2-methoxyphenyl)-5-ethoxy-2, 8-dimethyl-1, 4-dihydro-1, 6-naphthyridine-3-carboxylic acid (intermediate 5) and an optical isomer (intermediate 5a) thereof through hydrolysis of a fenerenone intermediate III or an optical isomer IIIa thereof, the method does not need to use CuCl2, and the method is simple in operation, easy to implement and low in cost. By controlling the dosage ratio of acid to the initial raw material, or the dosage ratio of Zn powder to the initial raw material, or optimizing reaction conditions, the conversion rate of the intermediate III or intermediate IIIa is unexpectedly improved (not less than 90%), the generation amount of intermediate impurity X is reduced (not more than 5%), the generation of experimental waste acid is reduced from the source, the product purity is also improved, and the production cost is reduced. The method is suitable for industrial large-scale production.

This invention discloses a phenylnaphthic acid derivative and its application in phosphorescent information encryption. The preparation method involves using 3,5-bis(ethoxycarbonyl)phenylboronic acid and methyl 6-bromo-2-naphthylcarboxylate as raw materials, and then performing a Suzuki coupling reaction under tetra(triphenylphosphine)palladium(O) catalysis to obtain the intermediate ethyl 2-(3,5-bis(ethoxycarbonyl)phenyl)-6-naphthylcarboxylate. This intermediate is then subjected to alkaline hydrolysis and acidification to obtain the target product, 2-(3,5-dicarboxyphenyl)-6-naphthylcarboxylic acid. This phosphorescent material has a simple preparation method, lower cost compared to noble metal phosphorescence systems, a simple guest synthesis method with high yield, and exhibits significant and stable phosphorescence effects. Furthermore, precise emission color control of high-performance doped thin films is achieved through the triplet-to-singlet Förster fluorescence resonance energy transfer (TS-FRET) mechanism, establishing a multicolor long-lifetime emission system. In addition, the material has multi-color adjustable properties and excellent long afterglow emission performance, showing great application potential in cutting-edge application fields such as multi-dimensional information encryption and high-end anti-counterfeiting.

The application discloses a synthesis process of (-)-alpha-lycorane alkaloid and belongs to the technical field of organic synthesis chemistry. (2Z,4E)-7,7-diethoxy-3-hydroxyhepta-2,4-dienoic acid methyl ester and 3,4-methylenedioxy-beta-nitrostyrene are used as starting materials, and (-)-alpha-lycorane is obtained through catalytic asymmetric tandem Michael addition reaction, nitro reduction amination reaction, Boc amidation reaction, Bischler-Napieralski cyclization reaction, ketone enolization tandem esterification reaction, enol triflate reductive hydrogenolysis reaction and amide reduction reaction in sequence. (-)-Alpha-lycorane has a four-membered ring core skeleton of pyrrole-phenanthridine ring, has good in-vitro tumor inhibition activity and cell proliferation growth inhibition activity. The synthesis process can realize efficient, simple and full synthesis of (-)-alpha-lycorane.

The invention relates to an imidazole bromide azobenzene ionic liquid catalyst as well as a synthesis method and application thereof. According to the technical scheme, the preparation method comprises the following steps: diazotizing 2, 6-diethylaniline at 0-5 DEG C, and then carrying out coupled reaction on the diazotized 2, 6-diethylaniline and 3, 5-dimethyl sodium phenolate to obtain 4-hydroxy-2, 6-dimethyl-2 ', 6'-diethylazobenzene; the preparation method comprises the following steps: carrying out a nucleophilic substitution reaction on 4-bromoethoxy-2, 6-dimethyl-2 ', 6'-diethylazobenzene and 1, 2-dibromoethane to obtain an intermediate 4-bromoethoxy-2, 6-dimethyl-2 ', 6'-diethylazobenzene; and finally, reacting the intermediate with excessive N-methylimidazole to synthesize the imidazole bromide azobenzene ionic liquid catalyst, namely 4-(N-methylimidazole bromide)-ethoxy-2, 6-dimethyl-2 ', 6'-diethyl azobenzene. The method has the characteristics of simple synthesis method, good water solubility of the catalyst, short reaction time at room temperature, high catalytic efficiency, green and environment-friendly catalytic reaction with water as a solvent, easy separation of products, recyclability of the catalyst and the like.

The application discloses a hydroxyl chalcone carboxyl derivative and a preparation method thereof, and provides use of the compound, a pharmaceutically acceptable salt thereof or a mixture thereof in preparation of a medicine for preventing and / or treating diabetes and complications thereof. The compound is used as an aldose reductase selective inhibitor, an alpha-glucosidase inhibitor, a hypoglycemic agent, an antioxidant and a lipid metabolism improver, and has the effects of preventing and / or treating diabetes and complications thereof. The application further provides a pharmaceutical composition containing the compound and having the effects of preventing and / or treating diabetes and complications thereof. In the application, R1 is a hydroxyl group or an alkoxy group, the alkoxy group is preferably a methoxy group or an ethoxy group; R2, R3, R4, R5 and R6 are independently selected from hydrogen, halogen, a hydroxyl group, a methoxy group or a trifluoromethyl group, and at least one of R2, R3, R4, R5 and R6 is a hydroxyl group; and the halogen is preferably fluorine.

This invention relates to a method for preparing (4S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthidine-3-carboxylic acid, and also to diastereomeric salts (Va), (Vb), (Vc), and / or (Vd). This method is simple to operate, and the diastereomeric salts can be obtained with very high chemical and enantiomeric purity (tartrate ester content <0.05%) through a single dissociation, avoiding the raw material loss and waste problems caused by multiple dissociations. It also has low production costs and meets the requirements of green production.

The invention belongs to the technical field of biological medicines, and relates to phenyl naphthalene derivatives and application thereof in preparation of medicines for preventing and treating tumors or medicines for neuroprotection. The compound is a compound shown in a formula I or a formula II or a pharmaceutically acceptable salt thereof. In the formula I, A is not present or is carbonyl, A'is carbonyl, sulfuryl, oximido and imino, R1 is amino, nitryl, acylamino, sulfonamide, aryl methoxy, aryl ethyoxyl, fluorine atom, trifluoromethyl, ureido, amidoxime, amidino and N-methyl sulfonamide, and R2 is hydrogen atom, methoxy, amino, nitryl, acylamino, amidoxime, amidino or fluorine atom; r2 and H2N-A'are located at the adjacent position of a benzene ring, R2 or H2N-A 'is located at the para-position of phenyl, and X1 and X2 are independently selected from CH or N. The phenyl naphthalene derivative provided by the invention has relatively high NQO2 inhibitory activity, and can be used as a chemical drug for tumor treatment and a neuroprotective agent for neurological diseases.

The invention provides a method for preparing 1-methyl-3-difluoromethyl-1H-pyrazole-4-carboxylic acid with high selectivity, which comprises the following steps: reacting methylhydrazine with a protective agent in an inert solvent to obtain single-protection methylhydrazine (IV); in the presence of alkali, carrying out condensation reaction on the single protection methylhydrazine (IV) and 2-ethoxymethylene-4, 4-difluoro-3-oxobutyric acid ethyl ester (I) to obtain an intermediate (V); adding acid into the reaction system obtained in the step S2 to synchronously remove the protecting group R and form a pyrazole ring, so as to obtain 1-methyl-3-difluoromethyl-1H-pyrazole-4-ethyl formate (II); alkali is added into the 1-methyl-3-difluoromethyl-1H-pyrazole-4-ethyl formate (II) for hydrolysis, then the hydrolysis product is acidified with acid, and suction filtration is performed to obtain the 1-methyl-3-difluoromethyl-1H-pyrazole-4-carboxylic acid (III). The content of regioisomers in the prepared product is less than or equal to 1%, the HPLC purity of the product is more than or equal to 98.0%, the content of single impurities is less than or equal to 0.15%, the moisture content is less than or equal to 0.1%, the residual acid content is less than or equal to 50 ppm, and the downstream reaction requirement can be met without secondary refining.