129 results about "Para-toluene sulfonate" patented technology

The invention relates to novel AZD 9291 pharmaceutical salt. The chemical structural formula of AZD 9291 is shown in the specification. The pharmaceutical salt is sulfate or tosilate or tartrate or acetate or citrate. The AZD 9291 pharmaceutical salt has solubility equivalent to or higher than that of AZD 9291 mesylate, can meet bioavailability and efficacy requirements, is higher in bio-safety and lower in hygroscopicity, solves the problems that existing AZD 9291 mesylate is high in toxicity and prone to deliquescence, and is more suitable for drug development.

The invention belongs to the technical field of medicines and discloses cytarabine 5'-O-amino-acid ester, pharmaceutically acceptable salts thereof and a preparation method thereof. The preparation method comprises the following steps of: slowly dropping carbobenzoxy chloride into a solution formed by cytarabine, sodium bicarbonate and N,N-dimethylacetylamide, and obtaining a compound A after reacting at room temperature; using the compound A and N-butyloxy formoxyl-amino acid as raw materials; adding a reagent to the solution to carry out an esterification reaction to obtain the cytarabine 5'-O-amino-acid ester; and then adding acid to obtain a finished product. The pharmaceutically acceptable salts comprise hydrochlorides, sulfates, formates, acetates, mesylates, propionates, butyrates, p-toluene sulphonates, phosphates, bisulfates, maleates, lactates, carbonates, bicarbonates, malonates, and salts formed with acidic amino acids, and the like. The invention can obviously improve the membrane permeability of the cytarabine so as to improve the bioavailability of the cytarabine.

The invention discloses 4-alkyl-2-arylamino-5-(1,2,4-triazole-1-group) thiazole and salts thereof shown in a formula I, wherein R is selected from H, alkyl groups of C1-C2 and straight-chain alkyl groups or branched-chain alkyl groups of C3-C4; X1, X2, X3, X4 and X5 are selected from hydrogen, alkyl groups of C1-C2, hydroxide group, methoxy group, oxyethyl group, trifluoromethyl, fluorine, chlorine, bromine, nitryl, amino group, acetyl amino group, methanesulfamide, ethoxycarbonyl or carboxyl; and the salts of the 4-alkyl-2-arylamino-5-(1,2,4-triazole-1-group) thiazole are selected from hydrochloride, hydrobromide, nitrate, sulfate, phosphate, mesylate, p-toluene sulfonate, tartrate, lactate or malate. The 4-alkyl-2-arylamino-5-(1,2,4-triazole-1-group) thiazole is applied to preparation of medicaments for resisting cervical cancer or lung neoplasms.

The invention relates to a pressure reducing and injection increasing agent used for a flooding well, which is applicable to water injection of an oil well. The invention is characterized in that the pressure reducing and injection increasing agent comprises the following ingredients according to the parts by weight: 30-42 parts of lauric acid monoethanolamine, 2.5-4.5 parts of L-alinebenzylestertosilate, 5.5-7.5 parts of C8-C10 alkylglucoside, 0.5-1.0 part of sodium nitrite, 0.5-1 part of Vitamin A, 0.05-0.1 part of fluorocarbon surfactant FN-2, 25-35 parts of methanol, and 15-35 parts of water. The invention has the effects that the pressure reducing and injection increasing agent can reduce oil-water interface tension, change wettability of rocks and inhibit clay swelling, thereby reducing wellhead pressure of the flooding well by 5-15 percentage points, so as to improve the seepage ability of injected water; therefore, the pressure reducing and injection increasing agent realizes pressure reducing and injection increasing for a low-seepage oil well and can inhibit bacteria growth.

The invention relates to two regorafenib organic acid salt as shown in formulas (I, II), namely 2-isethionate(isethionate) and esilate of regorafenib, and relates to two regorafenib isethionate (formula I) crystals named as a crystal A and a crystal B, two regorafenib esilate (formula II) crystals named as a crystal alpha and a crystal Beta and a novel regorafenib tosilate crystal named as a crystal N-1. The invention also relates to preparation methods of the regorafenib isethionate crystals A, B, the regorafenib esilate crystals alpha and beta and the novel regorafenib tosilate crystal N-1. The regorafenib isethionate crystals A, B, the regorafenib esilate crystals alpha and beta and the novel regorafenib tosilate crystal N-1 which are disclosed by the invention have X-ray powder diffraction characteristic absorption peaks and DSC (Differential Scanning Calorimeter) characteristic absorption peaks; and the regorafenib isethionate crystal A, the regorafenib esilate crystal beta and the novel regorafenib tosilate crystal N-1 which are disclosed by the invention have the advantages of stability, difficulty in moisture absorption and good solubility.

The invention relates to a soldering assistant chemical used for electronic assembly, in particular to an unleaded halogen-free soldering paste in the field of brazing material used for electronic surface assembly, which consists of 80-93 percent by weight of solder alloy powder and 7-20 percent by weight of flux, wherein the solder alloy powder is unleaded alloy, and the flux comprises 30-55 percent by weight of resin, 20-50 percent by weight of solvent, 1-8 percent by weight of thixotropic agent and 0.01-20 percent by weight of active agent, and the active agent comprises amino acid p-toluenesulfonic acid salt and / or amino-acid ester p-toluenesulfonic acid salt. The soldering paste has higher wettability, reduces corrosivity, has good storage stability, is unleaded and halogen-free, meets the requirement of environmental protection, and can be applied to the electronic industry.

The present invention relates to a method of synthesizing trioxymethylene from formaldehyde by the catalytic action of an acidic ionic liquid. In the method, formaldehyde solution with a concentration of 30˜80 wt % is used as reactant, and an ionic liquid is used as catalyst. The cation moiety of the catalyst is selected from either imidazoles cation or pyridines cation, and the anion moiety of the catalyst is selected from one of p-tolyl benzene sulfonate, trifluoromethyl sulfonate, and hydrogen sulfate. In the present invention, ionic liquid is used, for the first time, as a catalyst to synthesize trioxymethylene from formaldehyde. The catalyst can be circularly used for continuous sampling.

The invention discloses a compound extender for urea-formaldehyde resin, which is prepared by mixing the following raw materials in parts by weight: 30-40 parts of bean flour, 20-30 parts of wood flour, 10-15 parts of walnut shell flour, 5-10 parts of corn flour, 20-30 parts of modified attapulgite, 10-15 parts of ammonium chloride, 3-6 parts of para toluene sulfonate and 5-10 parts of desugared sodium lignosulfonate. According to the invention, the modified attapulgite contains carboxyl, so that condensation crosslinking with hydroxymethyl of urea-formaldehyde resin is greatly improved, and the dispersion property in the urea-formaldehyde resin is good, thereby reducing the number of hydrophilic groups and improving the water resistance of adhesion. The extender disclosed by the invention is convenient in adhesive mixing method, can reduce or replace extenders such as flour and the like for use and lower the cost, and has high adhesion strength, good shock strength and large elastic modulus. Through chemical bond combination and adsorption of the modified attapulgite, release of free formaldehyde is reduced.

The invention discloses a new medicinal salt of (E)-1-{4-[(3',4',5'-trimethoxy cinnamon acyl]-1-piperazidine} acetopyrrole as cinprazole, which comprises the following parts: mesilate, phosphate, nitrate, sulfate, hydrobromide, p-toluenesulfonic acid salt, tartrate, fumarate, citrate, succinate, malonate, optimizing the mesilate, nitrate, phosphate and sulfate, for mesilate at best. The drug can be used to treat and / or prevent cardiovascular and cerebrovascular disease and peripheral vessel disease. The drug possesses good stability and superior solubility, which can be made into acceptable pharmacy agent.

The present invention relates to the fracturing field, and discloses a water solution, a clean fracturing fluid, and a method for fracturing reservoir. The water solution contains organic acid amidopropyl dimethylamine, an additive, and water, wherein, the additive is at least one of salicylate, cis-butenedioic acid, o-phthalic acid, dodecyl sulfonate, p-toluene sulfonate, and benzoate. The water solution has high carbon dioxide response performance, a clean fracturing fluid that contains the water solution has superior cyclic utilization performance, and the fracturing fluid can solve the problems of conventional fracturing fluids used in fracturing stimulation of oil and gas reservoirs, including incomplete gel breaking, severe damages to the reservoir, and severe contamination of flow-back fluid, etc.

The invention discloses quaternary phosphonium salts with p-toluenesulfonate as anions as well as a synthesis method, a preparation method and an application of the quaternary phosphonium salts. The synthesis method adopts a simple two-step synthesis route, that is, diethylene glycol monomethyl ether / methoxypolyethylene glycols reacts with p-methyl benzene sulfonic chloride to prepare diethylene glycol monomethyl ether / methoxypolyethylene glycol p-toluenesulfonate, then, diethylene glycol monomethyl ether / methoxypolyethylene glycol p-toluenesulfonate further reacts with triphenylphosphonium toobtain diethylene glycol monomethyl ether / methoxypolyethylene glycol-triphenyl phosphine p-toluenesulfonate. Through the simple synthesis route, the product has good dissolution property and cell penetrability, better antibacterial and killing performance for microbes and an anti-tumor function.

The invention relates to a preparation method of racecadotril. The method comprises the following steps: (1) enabling thioacetic acid to react with 2-benzylacrylic acid to prepare an intermediate 3-acetyl mercapto-2-benzyl propanoic acid; (2) carrying out amidation on the intermediate 3-acetyl thiol-2-glycin benzyl propionic acid and glycine benzyl ester p-toluenesulfonate salt under existence of a catalyst to generate the racecadotril. By adopting the method, the racecadotril with high yield and purity can be obtained, the defect of the original technology is compensated, pollution is reduced, and the cost is reduced. Thioacetic acid is used as a solvent and is also used as a reaction reagent, reaction process is simple and rapid, few reagents are used, and the purity and the yield are greater than or equal to 95%; EDCI or DCC is selected as a condensation reagent; a mixed solvent is used for crystallization, the influence on product yield is small, and impurity removal effect is good; the overall technology adopts a one-step to synthetize, simple, efficient, high in atom economy, more green and environment-friendly, and the racecadotril product which is high in yield, and accords with the EP quality standard can be obtained.

The invention relates to foaming printing ink which comprises the following components in parts by mass: 5-30 parts of para toluene sulfonate, 10-25 parts of azodicarbonamide, 0.1-0.2 parts of defoaming agent, 15-30 parts of ethanol amine, 1-2 parts of cross-linking agent, 50-60 parts of polyvinyl chloride, 60-80 parts of polyvinylidene chloride emulsion, 5-10 parts of epoxy glycol, 0.5-1 part of thickener, 10-20 parts of ethylene glycol, and 1-3 parts of water dispersing pigment. The foaming printing ink is stable to store, nontoxic, odorless, difficult to damage and low in cost, has a three-dimensional effect, improves a decorative art effect, can shorten a technological flow, can lower the printing cost, and can be printed in quantity quickly.

The invention belongs to the field of organic chemical synthesis, and discloses cyclic pentapeptide with a novel structure, as well as a synthetic method and application thereof. The cyclic pentapeptide with the novel structure is cyclo-(N-Me-D-Phe-D-Leu-N-Me-D-Leu-D-Leu-L-Leu), the molecular formula is C35H57N5O5, and the structural formula is shown in the description. The cyclic pentapeptide adopts D-Leu, L-Leu, D-Phe and D-Leu benzyl ester tosilate as raw materials, a tripeptide midbody and a dipeptide midbody are respectively prepared through a proper technology, and a cyclization locus is selected at the amido linkage position adjacent to D and L configurations, so that the cyclization efficiency is effectively increased. The cyclic pentapeptide has the advantages of simple synthetic process, low raw material cost, mild reaction conditions, high purity and easy industrial production, and can fully meet the requirements of medical experiments and clinical application.

Provided is a novel preparation method of lapatinib and two pairs of tosylate monohydrate and compounding of relevant midbody N-[3-chlorine-4[(3-fluorine benzyl group) oxygen] phenyl group]-6-halogen-quinazoline-4-amine and 5-[(2'-methylsulfonyl ethyl amino) methyl-2-furanboric acid. The synthetic method comprises reaction steps of amidining, condensation, reduction amination, suzuki coupling, salify purification and the like. The method avoids preparation of an unstable midbody and using of chlorinated reagent with large pollution and danger, and has the advantages of being high in product purity, simple in operation, less in liquid and gas waste generated by reaction, convenient in aftertreatment and the like.

The invention provides pharmaceutical salt of an EGFR inhibitor and a crystal form, preparation method and application of the pharmaceutical salt. The structural formula of the EGFR inhibitor is as shown in formula I. The pharmaceutical salt is the mesylate, the tosilate, the phosphate, the hydrochloride or the citrate of the EGFR inhibitor. The pharmaceutical salt has the advantages that the pharmaceutical salt has the specific crystal form, the solubility and the stability of the pharmaceutical salt are higher than those of corresponding free alkali, the pharmaceutical salt is suitable for being used to prepare drugs for treating cancer (especially non-small-cell lung cancer), and the bioavailability and drug effect requirements are satisfied.

The invention provides a preparation method of metacycline. The metacycline is prepared by carrying out dechlorination reaction on 11alpha-chloro-6-methyleneoxytetracycline p-toluenesulfonate under the action of a dechlorinating agent. The product prepared by the method is high in selectivity and yield, the yield of the metacycline is 90.8-98.6 percent, reaction conditions are very mild and safe,and reaction equipment model selection is relatively simple; on the other hand, the preparation of the dechlorination reagent is relatively simple, the reaction process is relatively simple, and the production cost is greatly reduced.

The invention provides a preparation method of edoxaban p-toluenesulfonate monohydrate. According to the preparation method, an appropriate amount of a specific ionic liquid is added, a specific ratioof a combination of triethylamine and pyridine is selected as a base, the rapid progress of a reaction is facilitated, and improvements on the production rate and the product purity are facilitated.

The invention provides a method for synthesizing a novel beta-cyclodextrin derivative modified by radicals containing oxazoline by using beta-cyclodextrin, and also provides a method for modifying the surface of common silica gel into hydrogenated silica gel and bonding the cyclodextrin derivative to the hydrogenated silica gel by using appropriate small molecules. An oxazoline derivative ligand used in the method provided by the invention has a very good rigid structure and a chiral recognition site, and is beneficial for improving the separation selectivity of a chiral selector to an enantiomer, and expanding the separation range of chiral compounds. According to the methods provided by the invention, 6-deoxy-6-R,S-(4-phenyl)-4,5-dihydrogen oxazoline-beta-cyclodextrin and 6-deoxy-6-R,S-(4-pyridine p-toluene sulfonate methyl)-4,5-dihydrogen oxazoline-beta-cyclodextrin are synthesized respectively by virtue of simple and easy operation steps, and are bonded to the hydrogenated silica gel to prepare a hydrogenated silica gel stationary phase. The whole synthetic route is simple in operation and mild in reaction condition, and the product is easy to purify and high in yield. The methods provided by the invention are applied to chiral separation, and are used for performing qualitative researches on certain chiral aromatic alcohols, ferrocene derivatives, amino acid and mandelic acid derivatives and chiral drugs in a polar organic mode and a reversed phase mode.

Polypyrrole / carbon (PPy / C) composite doped with organic anion p-toluenesulfonate (pTS) is utilized as an electrode in supercapacitor for energy storage application. The surface initiated in-situ chemical oxidative polymerization yields a composite material PPy / C in the presence of varying concentrations of pTS. The novelty of the present invention lies in the doping of PPy / C composite with organic anion pTS and consequent enhancement of its electrochemical activity and stability. The conjugation length and electrical conductivity of pTS doped PPy / C composites increase with the increase in dopant concentration. The pTS doped PPy / C composite synthesized using equimolar concentration (0.1 M) of pTS to pyrrole shows the maximum specific capacitance of ˜395 F / g in 0.5 M Na2SO4 aqueous solution with significant stability ˜95% capacitance retention after ˜500 cycles.

The invention provides a preparation method of ubenimex. The preparation method comprises that L-leucine benzyl ester p-toluenesulfonate and HOBt undergo a condensation reaction to produce an activated ester solution, (2S, 3R)-3-benzyloxyformamido-2-hydroxy-4- phenylbutyric acid and a weak acid strong alkali inorganic salt are mixed, the activated ester solution is added into the mixture drop by drop and undergoes a reaction to produce N-[(2S, 3R)-3-benzoylformamido-2-hydroxy-4-phenylbutyryl]-L-leucine, and N-[(2S, 3R)-3-benzoylformamido-2-hydroxy-4-phenylbutyryl]-L-leucine is reduced into ubenimex through hydrogen gas. The preparation method utilizes ethyl acetate as an organic solvent, saves tetrahydrofuran-caused potential safety hazard, utilizes the weak acid strong alkali inorganic salt as a base catalyst, saves a cost, is free of an organic solvent and is easy to operate.

The present disclosure relates to p-toluene sulfonic acid salt of 5-amino-3-(2′-O-acetyl-3′-deoxy-beta-D-ribofuranosyl)-3H-thiazolo[4,5-d]pyrimidin-2-one and to its use in treating conditions such as viral infections, tumors, and cancer.Also disclosed is a method of preparing the p-toluene sulfonic acid salt of 5-amino-3-(2′-O-acetyl-3′-deoxy-β-D-ribofuranosyl)-3H-thiazolo[4,5-d]pyrimidin-2-one and methods for producing furanose compounds which are useful intermediates in the preparation of pharmaceutical compounds such as p-toluene sulfonic acid salt of 5-amino-3-(2′-O-acetyl-3′-deoxy-β-D-ribofuranosyl)-3H-thiazolo[4,5-d]pyrimidin-2-one and the like.

The present disclosure relates to p-toluene sulfonic acid salt of 5-amino-3-(2′-O-acetyl-3′-deoxy-beta-D-ribofuranosyl)-3H-thiazolo[4,5-d]pyrimidin-2-one and to its use in treating conditions such as viral infections, tumors, and cancer.Also disclosed is a method of preparing the p-toluene sulfonic acid salt of 5-amino-3-(2′-O-acetyl-3′-deoxy-β-D-ribofuranosyl)-3H-thiazolo[4,5-d]pyrimidin-2-one and methods for producing furanose compounds which are useful intermediates in the preparation of pharmaceutical compounds such as p-toluene sulfonic acid salt of 5-amino-3-(2′-O-acetyl-3′-deoxy-β-D-ribofuranosyl)-3H-thiazolo[4,5-d]pyrimidin-2-one and the like.

The invention discloses a preparation method of methacycline. The method includes: firstly taking water as a solvent, adding a ruthenium precursor into a carrier activated carbon, carrying out hydrogenation activation to obtain a ruthenium-carbon catalyst, and hydrogenating the ruthenium-carbon catalyst for reaction with 11alpha-chloro-6-methenyl oxytetracycline p-toluenesulfonate to obtain methacycline. The method has the advantages of simple process, mild reaction conditions and high total yield, enhances the product selectivity, lowers the production cost, and avoids the generation of threewastes, thus having favorable industrial prospects.

The invention belongs to the field of chemical pharmaceuticals and particularly relates to the crystal form A of niraparib (2-[4-((3S)-3-piperidyl)phenyl]-2H-indazole-7-formamide) p-toluene sulfonateand a preparation method of the crystal form A. The X-ray powder diffraction diagram of the crystal form A has feature peaks at the 2theta values of 9.5+ / -0.2 degrees, 15.1+ / -0.2 degrees, 18.4+ / -0.2 degrees, 19.4+ / -0.2 degrees, 21.0+ / -0.2 degrees, 24.6+ / -0.2 degrees and 30.0+ / -0.2 degrees. The crystal form A which is free of or hardly has hygroscopicity is extremely high in stability, stable in properties, less prone to deterioration and beneficial to medicine effect maintaining.

The present application belongs to the technical field of inorganic chemistry, and particularly relates to a preparation method for perfluoroisobutyronitrile. The method includes the following steps:step 1, in the presence of an organic solvent and an alkaline solution, performing condensation on heptafluoroisobutyramide and p-toluenesulfonyl chloride to obtain heptafluoroisobutyryl p-toluenesulfonate; and step 2, performing a reaction on the heptafluoroisobutyryl p-toluenesulfonate at the temperature of -30 DEG C to 20 DEG C to produce the perfluoroisobutyronitrile and p-toluenesulfonate. The preparation method for the perfluoroisobutyronitrile disclosed by the present application can effectively solve the technical defects that a current method for preparing perfluoroisobutyronitrile has a low yield and high costs, and the generated perfluoroisobutyronitrile is difficult to store in the system.

The invention provides glycyrrhetinic acid derivatives and medically acceptable salt thereof in a general formula (I) and a general formula (II). In the general formulas (I) and (II), R1 represents H, substituted or unsubstituted C1-C4 alkyl, C1-C4 alkenyl, alcyl alkyl, heterocycle alkyl, aryl, ceteroary, monosaccharide or polysaccharide, amino acid and polypeptide residue; R2 represents H, CH3, CH2CH3 or CH(CH3)2; R3 represents H, CH3CO, C2H5CO, C3H7CO, CF3CO and C6H5CO; and the salt comprises hydrochloride, hydrobromide, phosphate, lactate, tartrate, salicylate, sulfate, oxalate, acetate, succinate, maleate, malate, gluconate, toluenesulfonate, citrate, fumarate, formate and phenpropionate. The invention also provides a preparation method, a medicinal composition and application of the glycyrrhetinic acid derivatives. The glycyrrhetinic acid derivatives have a good anticancer effect.

The invention discloses a high-efficiency antibacterial powder paint which is prepared from the following raw materials in parts by weight: 60-70 parts of 191 unsaturated polyester resin, 5-10 parts of triglycidyl isocyanurate, 2-3 parts of barium stearate, 1-2 parts of nano silver inorganic antimicrobial agent RHA-1, 3-4 parts of aluminum silicate, 1-2 parts of N-ethyl-ortho-para toluene sulfonate, 2-3 parts of hexabromocyclododecane, 1-2 parts of sodium fluosilicate, 0.6-1 part of 1-hydroxycyclohexylphenyl ketone, 1-2 parts of benzotriazole and 5-10 parts of composite filler. The powder paint has the advantages of short curing time, low temperature, production cost saving, favorable antibacterial effect, favorable microbial corrosion resistance, favorable acid / alkali resistance and wide application range, and is especially suitable for application of furniture and home appliances.

The method for preparing polyvetone by means of copolymerization of carbon monoxide and olefin hydrocarbon uses the carbon monoxide and olefin hydrocarbon including ethylene, styrene and its derivative as raw material, and make them produce copolymerization reaction in the presence of catalyst, the composition of said catalyst contains palladium acetate, 2,2'-bipyridine and p-benzoquinone. The catalyst also contains the following components: acetates of yttrium, neodymium, praseodymium, lanthanum and cerium, p-toluenesulfonate, phosphate salt or their mixture and p-toluenesulfonic acid or aminosulfonic acid of fluoboric acid or their mixture.