67 results about "Nitrobenzoates" patented technology

The invention discloses a synthesis method of a Bcl-2 inhibitor ABT-199. The method comprises the following steps: by using methyl 2-fluoro-4-nitrobenzoate and 5-hydroxy-7-azaindole as raw materials, carrying out substitution, reduction, cyclization, substitution, hydrolysis, condensation and the like to synthesize the ABT-199. The method has the characteristics of mild reaction conditions, simple operating technique, low cost and high yield.

The invention relates to a method for synthesizing ridge sha tan, which uses the 2-tert-butyl ketonic oxygen amido-3-nitro benzoate (I) and N-(trityl )-5-(4'-morphine methylbiphenyll-2-group) tetrazolium (II) as raw material to do N-alkanisation reaction, protecting-released reaction, reduction reaction, ring-closed reaction and ester hydrolytic reaction. <0The protecting-released reaction can slough trityl and tert-butyl ketonic oxygen protect group in the lower aliphatic alcohol organic mixing solution.

Convenient method for obtaining carbapenem by hydrogenation with Raney Nickel, as an alternative to the known catalytic hydrogenation conducted under hydrogen overpressure in the presence of Palladium, starting from corresponding protected intermediates such as p-nitrobenzylesters and with optional suitable protections of any primary and secondary amino functions structurally present.

Relating to the field of chemical engineering, the invention in particular relates to a synthesis method of benzocaine. The method includes the steps of: synthesis of p-nitrobenzoic acid; synthesis of ethyl 4-nitrobenzoate; and synthesis of benzocaine. Through improvement of benzocaine synthetic experiment method, the invention specifically solves the problems of low yield, tedious reaction aftertreatment and the like in conventional preparation experiments, and the improved experimental operation method not only can achieve high yield preparation of benzocaine, enhance experimental efficiency, but also effectively improves the teaching effects of the experimental course, and is suitable for chemical experimental course teaching.

The invention discloses a fluorescent probe for detecting hydrogen persulfide, a synthetic method of the fluorescent probe and an application of the fluorescent probe, and belongs to the technical field of chemical analysis and detection. A benzothiazole phenothiazine fluorogen with green fluorescence emission reacts with 2-fluoride-5-nitrobenzoic acid to obtain the probe which has a general structural formula as shown in the specification. The fluorogen of the probe is benzothiazole phenothiazine, and a hydrogen persulfide response group is 2-fluoride-5-nitrobenzoate. Probe molecules have high selectivity and sensitivity to the hydrogen persulfide, detection range is 0-8 micromoles*L<-1>, and detection limit is 26 nanomoles*L<-1>. The probe can be used for detecting the hydrogen persulfide in water, soil and cells.

The present invention relates to the development of a novel assay for determining the activity of human histone deactylase 8 (HDAC8). As shown in FIG. 3, thioactyl-lysine-containing peptide is used as the substrate for the HDAC8-catalyzed dethioacetylation reaction. Thioacetate, which is formed during this reaction, is subsequently reacted with Ellman's reagent, 5,5′-dithiobis(2-nitrobenzoate), (DTNB) with a quantitative formation of 2-nitro-5-thiobenzoate (TNB). The concentration of thioacetate formed during the conversion reaction can be quantified by measuring the absorbance of TNB at 412 nm.

The invention relates to a method for preparing a tolvaptan intermediate. The method comprises the following steps of: reacting 2-methyl-4-nitrobenzoic acid used as an initial raw material and alcohols under the action of a catalyst to generate 2-methyl-4-nitrobenzoate, and reacting under the action of palladium-carbon catalyst by using ammonium formate as hydrogen donor to obtain 2-methyl-4-aminobenzoate compounds; and reacting the 2-methyl-4-aminobenzoate compounds and o-toluoyl chloride under the alkaline condition to generate 2-methyl-4-N-(2-methylbenzoyl)benzoate, adding alkali and a catalyst at presence of water to perform hydrolysis, extracting a water layer by using an organic reagent for one to two times, after layering, collecting a water-layer solution, adjusting the pH of the water-layer solution to be 5 to 6 to separate solid out, filtering an aqueous solution out to obtain solid remnant, and drying to obtain a target product. By the method, the quality and yield of a product are improved; a method for treating the intermediate is simplified; and a simple and feasible process method is provided for industrial production.

The invention discloses a method for preparing 5-methyl carboxylate-6-benzoltriazolylmethoxy. The method comprises the following steps of taking 2-methoxyl-4-aminobenzoate as a raw material, adding acetic anhydride and glacial acetic acid with a dissolved quantity and concentrated nitric acid with a nitration quantity in the raw material, performing a nitration reaction to prepare an intermediate of 2-methoxyl-4-amino-5-nitrobenzoate; taking 2-methoxyl-4-amino-5-nitrobenzoate as a raw material, adding methanol with a dissolved quantity and Raney nickel with a catalytic amount, controlling the pressure at 0.5-0.8 Mpa, putting hydrogen into the mixture, performing a hydrogenation reaction, pouring methanol aqueous solution containing sulfuric acid into the mixture, adding ices to separate out crystals, filtering and drying the crystal to obtain the intermediate 2-methoxyl-4,5-diaminobenzoate; adding the 2-methoxyl-4,5-diaminobenzoate in concentrated hydrochloric acid, adding sodium nitrite solution in the mixture drop by drop at a temperature of 0-5 DEG C, after the adding of the sodium nitrite solution is finished, heating the mixture to 30-35 DEG C and agitating the mixture for 1-2 hours; cooling and filtering the mixture, obtaining solid; washing the solid with methylene dichloride and water in sequence, obtaining the 5-methyl carboxylate-6-benzoltriazolylmethoxy. According to the method provided by the invention, the raw materials are easy to get, the operation is simple, the cost is low, the industrialization production is easy to realize, the product yield is high and more than 80%, therefore, the method has a good practicability and can produce good economic benefit and social benefit.

Disclosed is a preparation method of nintedanib (I), comprising the following steps: carrying out a condensation reaction on 4-(R acetate-2-yl)-3-nitrobenzoate (II) and trimethyl orthobenzoate to obtain (E)-4-[(2-methoxybenzylidene) R acetate-2-yl]-3-nitrobenzoate (III); carrying out a substitution reaction on the compound (EI) and N-(4-aminophenyl)-N-methyl-2-(4-methyl piperazine-1-yl) acetamide (IV) under the action of an acid-binding agent to generate (Z)-4-{[2-(N-methyl-2-(4-methyl piperazine-1-yl) acetamido-aniline) benzylidene] R acetate-2-yl}-3-nitrobenzoate (V); and sequentially carrying out reduction reactions and cyc-lization reactions on the compound (V) to prepare the nintedanib (I). The preparation method has an easily obtained raw material and a simple process, is economical and environmentally friendly, and is suitable for industrial production.

The invention relates to a method for preparing a tolvaptan intermediate. The method comprises the following steps of: reacting 2-methyl-4-nitrobenzoic acid used as an initial raw material and alcohols under the action of a catalyst to generate 2-methyl-4-nitrobenzoate, and reacting under the action of palladium-carbon catalyst by using ammonium formate as hydrogen donor to obtain 2-methyl-4-aminobenzoate compounds; and reacting the 2-methyl-4-aminobenzoate compounds and o-toluoyl chloride under the alkaline condition to generate 2-methyl-4-N-(2-methylbenzoyl)benzoate, adding alkali and a catalyst at presence of water to perform hydrolysis, extracting a water layer by using an organic reagent for one to two times, after layering, collecting a water-layer solution, adjusting the pH of the water-layer solution to be 5 to 6 to separate solid out, filtering an aqueous solution out to obtain solid remnant, and drying to obtain a target product. By the method, the quality and yield of a product are improved; a method for treating the intermediate is simplified; and a simple and feasible process method is provided for industrial production.