558results about How to "Short route" patented technology

A process for preparing the non-chiral non-peptide antithrombase depressants BIBR-953, BIBR-1048, etc from 3-nitro-4-chlorophenyl formic acid is disclosed. Said depressant contains 1,2,5-trisubstituted benzimdazole as central skeleton or a F atom.

The invention discloses azepine argireline or pharmaceutically acceptable salt thereof and a preparation method and application thereof. The structure of the azepine argireline is shown in formula 4.

The invention discloses a c-di-GMP and analogues thereof which have structures of a general formula I. The invention also discloses a novel preparation method-a kettle phosphoramidite method which can be used for rapidly, simply and conveniently preparing c-di-GMP compounds with high yield and low cost on a large scale and at mild conditions. The c-di-GMP is prevalent in bacteria and is a novel second messenger molecular which takes part in regulating multiple physiological functions. The research shows that the c-di-GMP and the analogues thereof can inhibit the formation of bacterium biological membranes and the multiplication of eukaryotic cells; and thereof the c-di-GMP and the analogues thereof have good medicine development prospect.

The invention relates to the field of vehicle welding in a vehicle production line, in particular to a storage switching mechanism for multi-vehicle-type vehicle body mixed line forming station clamps. The storage switching mechanism comprises four sets of clamp storage banks, and a clamp conveying device is installed below the clamp storage banks. The storage switching mechanism further comprises a clamp transfer device and a clamp in-place device. The clamp transfer device and the clamp in-place device are fixed between two sets of clamp storage banks located on the same side of a welding production line. The two ends of the clamp in-place device and the two ends of the clamp transfer device are connected with the clamp conveying device in the two sets of clamp storage banks on the same side respectively to form an annular clamp conveying system. The clamp storage banks are reasonable in arrangement structure, the occupied area of a factory is saved, the whole arrangement structure is more reasonable, the clamps can be well conveyed to designated positions through the cooperation of three-dimensional conveying mechanisms, the transfer device and the in-place device, the transfer efficiency of the clamps on the welding production line is improved, and high promotional value is achieved.

The invention relates to a method for synthesizing glabridin. The method comprises the following steps: using acetophenone protected by phenol hydroxy as a raw material, carrying out a Willgerodt-Kindler reaction to obtain aryl phenylacetic acid, and carrying out a Friedel-Crafts reaction to obtain an isoflavones compound; causing the isoflavones compound to carry out Pd / C catalytic hydrogenation to obtain a isoflavanone compound; and causing the isoflavanone compound to carrying out a crclizationreaction, a conyl reduction reaction and a removing phenolic hydroxyl group protection group reaction to obtain the glabridin. The operation and the serparation of the steps of the method are simple, the yield is higher, the used reagents are common reagents, are cheap and are easily obtained, the path is shorter, and the tptal yield is not lower than 20 percent.

A process for preparing dichroine and (2R, 3S)-1-benzyloxy-2-allyl-3-alkoxy piperidine as the intermediate of RU-19110 includes such steps as the reaction of imide on protecting agent to obtain compound E, reacting on allyl magnesium to obtain compound F, reacting on lewis acid and silane to obtain compound G, reacting on cerium ammonium nitrate to obtain compound H, reacting on litium aluminium hybrid to obtain protected (2R, 3S)-9, and reacting on meta-chloroperoxy benzoic acid to obtain compound J.

The invention discloses a mercury ion fluorescence sensor shown in a formula (I). The sensor comprises a rhodamine b framework, anion bonding unit urea or thiourea and a signal element fluorescent molecular radical sensed. The invention further discloses a synthetic method of the mercury ion fluorescence sensor. The invention further provides an application of the mercury ion fluorescence sensor show in the formula (I) in mercury ion detection. Compared with the prior art, the raw materials used by the invention are available, the synthetic steps are simple and the post-treatment is convenient, and industrialized production is easy to realize.

The invention discloses a preparation method of a ribofuranose phosphate derivative. The preparation method comprises preparation steps as follows: L-alanine isopropyl ester hydrochloride, phenol dichlorophosphate and substituted phenol are taken as starting materials and have a docking reaction under the action of alkali; (2R)-2-deoxy-2-difluoro-2-methyl-D-erythropentonic acid GAMMA-lactone and 3,5-dibenzoate reduce carbonyl in a dichloromethane or ether solvent into an alcoholic hydroxyl group under the action of a strong reducing agent; an intermediate with a formula 2-1 has a reaction with paratoluensulfonyl chloride under the action of alkali to obtain p-toluenesulfonates; an intermediate with a formula 2-2 and a benzoyl cytosine derivative have a docking reaction under the action of a condensing agent; an intermediate with a formula 2-3 converts cytosine into uracil under the action of organic acid; benzoyl protection for an intermediate with a formula 2-4 is released under the action of an alkaline agent; an intermediate with a formula 2-5 and an intermediate with a formula 1 are docked under the action of a Grignard reagent to obtain Sofosbuvir.

The invention discloses a process for preparing bosutinib, which simplifies reaction steps, optimizes reaction conditions, improves yield and paves the way for industrial production. The bosutinib is prepared from 4-hydroxy-3-methoxybenzoic acid serving as a raw material and the raw materials required in the reaction process have already been industrially produced, so the cost is low and can be saved; the process flow is relatively short and the yield is relatively high; and the cyclization conditions are mild and cyclization is only carried out at room temperature, so the process is suitable for industrial production.

The present invention discloses a process for producing light olefins, comprising the steps of: i) contacting a feed comprising a monohalo-methane with a molecular sieve catalyst under the conditions: a reaction temperature in the range of from 350° C. to 600° C., a reaction pressure in the range of from 0.05 to 1.1 MPa (absolute), and a weight hourly space velocity of the monohalo-methane in the range of from 0.1 to 100 hour−1, to give an effluent comprising ethylene, propylene, and hydrogen halide; and ii) isolating ethylene, propylene and hydrogen halide from the effluent.

The present invention publicly discloses a synthetic method and intermediates of rosuvastatin calcium and synthetic methods of the intermediates. The synthetic method uses 4-4′-fluorophenyl-6-isopropyl-2-(N-methyl-N-methylsulfonylamino)pyridine-5-formaldehyde as the raw material, includes 4-4′-fluorophenyl-6-isopropyl-2-(N-methyl-N-methylsulfonylamino)pyridine-5-acrylonitrile (intermediate I) from a nitrilized reaction, and 4-4′-fluorophenyl-6-isopropyl-2-(N-methyl-N-methylsulfonylamino)pyridine-5-acraldehyde (intermediate II) from an aldehydized reaction of the intermediate I, and further goes through such unit processes as side-chain extension, ketone-group reduction, ethyl-group hydrolysis and neutralization reaction or decomposition reaction to obtain rosuvastatin calcium. The nitrilized reagent can be phosphate diethylacetonitrile, acetonitrile, etc.; the aldehyde reductant can be diisobutyl aluminum hydride, red aluminum, etc.; and the ketone-group reductant can be diethylmethoxyborane, NaBH4, KBH4, etc.

The invention discloses a one-step synthesis method of N, N-diethyl-3-methyl-benzamide with a fixed bed, which comprises the steps that: 3-methyl benzoic acid and diethylamine are stirred under a solvent system for reaction to generate a complex salt compound of the 3-methyl benzoic acid and diethylamine, and then materials are fed to the catalyzing fixed bed continuously under constant temperature and constant pressure, then dehydrated continuously to obtain a crude product; the solvent is recovered by distillation under ordinary pressure; finally the pure product of the N, N-diethyl-3-methyl-benzamide is obtained after rectification under vacuum. The molar ratio of the 3-methyl benzoic acid to the diethylamine to the solvent is 1.0: (1.0-15.0): (0-25.0), the mass velocity is 0.1 h<-1> to 20.0 h<-1>, the reaction temperature of the fixed bed is 60 DEG C to 550 DEG C and the reaction pressure of the fixed bed is 0.1 MPa to 5.0 MPa. The synthesis technology has the advantages of short technological process, high conversion ratio, good selectivity, high yield rate, small amount of waste gas, waste water and waste residues, reproducible and recyclable catalyst and low cost.

The invention discloses a preparation method of intermediate of rivaroxaban of formula 6, which comprises the following steps of: carrying out reaction of removing benzyl protecting group of amino to the compound 5 in a solvent. The invention also discloses a preparation method of rivaroxaban and an intermediate compound thereof. The preparation method disclosed by the invention has the advantages of shorter process, lower cost, easily acquired material and high production rate, and the prepared product is suitable for industrial production.

The invention discloses 1, 2-anti form glucoside derivative of oxazole compound. During the preparation, 4-(3, 4, 5-trimethoxy phenyl)-5-(3-hydroxyl-4-methoxy phenyl oxazole is used as the acceptor of glycosyl, bromo sugar of D-glucose, D-galactose, L-arabinose, D-xylose, L-fucose or lactose with full acetyl protection, or trichlorine imine ester of L-rhamnose or D-mannose with full acetyl protection is adopted as the donator of glycosyl, glycosylation is performed with the catalysis of alkali and tetrabutyl ammonium bromide or lewis acid, to obtain glucoside derivative containing acetyl protecting group; and then the acetyl protecting group is removed by utilizing methyl alcohol and sodium methoxide, to obtain 1,2 anti-form glucoside derivative of oxazole compound. The preparation method is simple, highly effective and universal, the route is short, the water-solubility of the product is good, the bioavailability is high, thereby the glucoside derivative can be applied as antineoplastic medicine inhibiting microtubule assembly and selectively targeting tumor blood vessels.

The invention discloses a preparation method of 2,5-dichlorophenol and relates to the technical field of pesticide intermediate synthesis. The preparation method comprises the following steps: with p-dichlorobenzene as a start raw material, performing a Friedel-Crafts acylation reaction between the p-dichlorobenzene and acetyl chloride in the presence of aluminum trichloride to obtain 2,5-dichloroacetophenone; performing a Baeyer-Villiger oxidation reaction between the 2,5-dichloroacetophenone and a peroxide in the presence of a catalyst at room temperature to obtain 2,5-dichlorobenzene acetate; and performing a hydrolysis reaction between the 2,5-dichlorobenzene acetate and inorganic aqueous alkali in a reflux condition to obtain 2,5-dichlorophenol. The preparation method disclosed by the invention has the characteristics of simple synthesis process, short line, low production cost and high yield; and moreover, with less quantity of generated three wastes and high environmental protection property, the preparation method is more suitable for large-scale industrial production.

The invention discloses a novel single phosphorus ligand PC-Phos of a xanthene framework. The ligand is a compound as shown in a formula (1) or an enantiomer, racemate or diastereoisomer of the compound as shown in the specification. The invention further discloses a preparation method of the ligand. A formula 2 and a formula 4 as shown in the specification serve as raw materials, and substitution reaction, addition reaction, condensation reaction and reduction reaction are performed to prepare the ligand. Alternatively, a formula 6 and the formula 4 as shown in the specification serve as raw materials, are subjected to condensation reaction and subjected to addition reaction with a formula as shown in the specification to prepare the ligand. Chiral sulfonamide 4 with two structures and different types of metallic reagents are subjected to addition reaction, and optical voidness of four full structures 1 (S, Rs), 1 (R, Rs), 1 (S, Ss) and 1 (R, Ss) of the chiral single phosphorus ligand can be obtained. The invention further discloses an application of the ligand to asymmetric cyclization reaction in catalytic allene amine molecules. The ligand has quite high reaction activity, stereo-selectivity and wide application values.

The present invention relates to an accumulator-type injection system for injecting fuel from an accumulator into a combustion chamber of an internal combustion engine by means of injectors, the injectors being arranged completely within the cylinder head of the internal combustion engine.

The invention relates to quinoline compound, a synthesis method and the application for preparing medicines of camptothecin alkaloid. The syntheticroute is concise, high-efficient and economical, and can play a great role in promoting the later industrialized production of camptothecin alkaloid.

The present invention belongs to the field of medicine chemical technology. The preparation process of glycyl glutamine includes: dissolving carbobenzoxy Gly and N-maloylimine in organic solvent, adding solution of dicyclohexylcarbodiimide to obtain activated N-carbobenzoxy Gly-N-maloylimine solution, reacting the activated ester solution with glutamine under alkali condition to obtain carbobenzoxy glycyl glutamine; hydrogenolyzing the obtained carbobenzoxy glycyl glutamine in mixed water-alcohol solvent and under the catalysis of Pd catalyst, and re-crystallization to obtain glycyl glutamine product. The advantages includes short path, simple technological process, strong operability, low cost and less environmental pollution.

The invention discloses a method for preparing adipate, comprising the following steps of: (1) adding cyclohexane, solvent, an initiator and a solid catalyst into a reactor and mixing to form a mixed suspension; (2) introducing enough amount of oxygen into the mixed suspension to be used as an oxidant; and reacting under the conditions that the pressure is 0.5-5MPa and the temperature is 100-200DEG C for 1-20h; (3) separating the reaction mixture in the step (2) to obtain the solid catalyst and a liquid phase mixture; and (4) separating the adipate from the liquid phase mixture in the step (3). The invention prevents nitric acid from corroding the environment and the equipment, can solve the problems that a homogeneous catalyst is difficult to recover and is deactivated in the oxidation process of the cyclohexane, is free from using noble metals and has high reaction selectivity and favorable activity. The used catalyst can be recycled.

The invention discloses an ursodesoxycholic acid preparation method. The method comprises the following steps: 1, adding chenodeoxycholic acid and a solvent A to a reaction container, stirring for dissolving, adding 7-alphaHSDH, 7-betaHSDH and a coenzyme II, and carrying out a reaction at a controlled temperature at a controlled pH value to convert chenodeoxycholic acid into ursodesoxycholic acid in order to obtain a conversion liquid; 2, heating the conversion liquid obtained in step 1 to denaturalize the 7-alphaHSDH and the 7-betaHSDH, centrifuging through a high speed centrifuge, removing proteins, adding a sodium hydroxide solution to the above obtained solution, distilling to remove the solvent A, adding water to dissolve obtained distillation residues, adding an acid, and crystallizing to obtain crude ursodesoxycholic acid; and 3, adding the crude ursodesoxycholic acid obtained in step 2 and a solvent B to the reaction container, heating and refluxing the crude ursodesoxycholic acid and the solvent B for 1h, cooling the obtained reaction product to normal temperature, and filtering the cooled product to obtain ursodesoxycholic acid with the purity being greater than 99%. The ursodesoxycholic acid preparation method has the advantages of simple technology, short synthesis route, high conversion rate, easy post-treatment and environmental protection.

The invention discloses a c-di-GMP and analogues thereof which have structures of a general formula I. The invention also discloses a novel preparation method-a kettle phosphoramidite method which can be used for rapidly, simply and conveniently preparing c-di-GMP compounds with high yield and low cost on a large scale and at mild conditions. The c-di-GMP is prevalent in bacteria and is a novel second messenger molecular which takes part in regulating multiple physiological functions. The research shows that the c-di-GMP and the analogues thereof can inhibit the formation of bacterium biological membranes and the multiplication of eukaryotic cells; and thereof the c-di-GMP and the analogues thereof have good medicine development prospect.

The invention relates to a preparation method of triallyl phosphate, which comprises the following steps that allyl alcohol, an acid-binding agent and an ether solvent are mixed in an inert gas atmosphere; phosphorus oxychloride is dropwise added to a mixed liquid in the inert gas atmosphere; then stirring and reaction are performed; a liquid obtained after the reaction is filtered; a filtrate obtained after filtering is subjected to atmospheric distillation and solvent recovery; the residual filtrate after the solvent recovery is subjected to rectification under vacuum; and a fraction of triallyl phosphate is collected. The method has the following advantages that 1, the method is simple in technology, short in route, cheap in material and very small in toxic property, and is suitable for industrial production; 2, the method is few in byproduct and high in yield; and 3, the purity of a rectified and purified product is high, and can reach 99.5%, and the method is particularly suitable for the fields of lithium ion battery electrolyte additives and the like.

The invention discloses a novel polyhalogenated isoquinoline class derivate and a synthetic method thereof. The structure of the polyhalogenated isoquinoline class derivate is as a formula I, wherein Z=NH, NR', O, S; n=1,2,3; the R' is alkyl and aryl; R is the alkyl, the aryl, heteroaryl, condensed aryl, alkoxyl and alkylthio group; R1 is a halogen atom, a hydrogen atom, the alkyl, the aryl, alkylamino radical, arylamine, alkylthio group and arylthio; R2 is cyano-group, nitryl, ester group, the halogen atom, the hydrogen atom, the alkyl, the aryl, the alkylamino radical, the arylamine, the alkylthio group and the arylthio; X1 is the halogen atom; and the X2 is also the halogen atom. The synthetic method of the polyhalogenated isoquinoline class derivate including the steps of porphyrizing and heating polyhalogenated cyanobenzene and heterocyclic ketene aminals derivates in a mortar. When raw materials are basically completely disappeared, and the polyhalogenated cyanobenzene and the heterocyclic ketene aminals derivates are all transferred to a round bottom flask by menstruum and then reacted to synthesize the polyhalogenated isoquinoline class derivate with potential medicine activity in the formula I after a catalyst is added into the round bottom flask. The invention has simple synthesis technology, high productive rate, stable products, simple routes, rapidness, and the like, realizes a parallel high-efficiency heterocyclic compound library and really realizes the molecular diversity.

The invention relates to a method for preparing 3-amino-1-adamantane alcohol. The method comprises the following steps of: adding amantadine hydrochloride into a nitrating agent in batches, performing reaction for 1 to 2 hours in an ice-water bath and performing reaction for 1 to 30 hours at room temperature to obtain yellowish liquid; pouring the yellowish liquid into ice, continuously reacting for 0.5 to 2 hours with stirring to obtain blue-green liquid; and adding solid base into solution obtained by the step 2 with stirring, keeping temperature below 80 DEG C, regulating pH to be between 10 and 12, performing reaction for 30 minutes with stirring, leaching, extracting reaction liquid by using dichloromethane, drying the obtained product with anhydrous sodium sulfate, steaming off the dichloromethane and performing recrystallization by using ethyl acetate to obtain white solid. The preparation method has the advantages of readily available starting raw materials, simple reaction operation, short route, environmental friendliness, easy industrial production and good application prospect, and also reduces cost for the synthesis of Vildagliptin serving as a medicament for treatingdiabetes; and the yield of products reaches 75 percent.

The invention discloses an N-quinolyl substituted beta-lactam compound as shown in a general formula (I), wherein R<1> and R<2> refer to mutually independent H or C1-12 straight-chain or branched-chain hydrocarbonyl, aryl, alkoxy, acyloxy or amino; R<3> refers to H or C1-25 straight-chain or branched-chain hydrocarbonyl or aryl, or R<3> together with R<1> or R<2> forms a substituted or non-substituted five-eight-membered ring containing or without containing heteroatoms, and the heteroatoms can be N, O and S; R<4> and R<5> refer to mutually independent H or C1-12 straight-chain or branched-chain hydrocarbonyl, aryl, alkoxy, acyloxy or amino, nitryl, sulfonyl and halogen, and halogen refers to F, Cl, Br and I. The invention also provides a synthetic method of the N-quinolyl substituted beta-lactam compound, a pharmaceutical composition containing the compound, as well as application of the compound in medicine preparation of beta-lactamase inhibitors.