34 results about "Tosyl" patented technology

An N-heterocycle-containing boric acid compound and a preparation method and application thereof are provided. The preparation method adopts 3-bromo-1-p-tosyl-1H-pyrrolo[2, 3-b]pyrimidine as a raw material to generate (3-((5-chloro-4-(1H-pyrrolo[2,3-b]pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)boric acid by three steps of reaction. The (3-((5-chloro-4 (1H-pyrrolo[2,3-b]pyridin-3-yl)pyrimidin-2-yl)amino)phenyl)boric acid has good inhibition effect on the proliferation activity of brain glioma, which is proven by cell experiments.

The invention belongs to the technical field of pharmacy, and particularly relates to application of polycyclic alkaloid in preparation of an anti-breast cancer drug, and the polycyclic alkaloid is 1, 2a, 7-trimethyl-5-tosyl-1, 2, 2a, 3, 4, 5-hexahydropyrrolo [4, 3, 2-de] quinoline. The polycyclic alkaloid compound is applied to preparation of anti-breast cancer drugs, the effect of inhibiting growth of breast cancer cells is remarkable, and the efficacy of the polycyclic alkaloid compound is far better than that of a positive drug ML162 aiming at EC50 (mu M) + / -S.D = 9.04 + / -0.37 of HCC1937 human breast cancer cells.

The invention discloses a preparation method of a 3-substituted-2, 3 '-bisindole compound, and belongs to the field of organic synthesis. According to the method, 3-iodoindole with indole N-H protected by p-toluenesulfonyl and olefin are used as initial raw materials and are stirred to react in an organic solvent at 60-120 DEG C under the action of a palladium catalyst, norbornene, a phosphine ligand, an accelerant and alkali, and the 3-substituted-2, 3 '-bisindole compound can be obtained. The raw materials used in the method are cheap and easy to obtain, the reaction process is mild, the substrate universality is good, and the method has high step economy and practicability.

The invention discloses a novel bismuth-based chelate CT contrast agent and a preparation method and application thereof. The synthesis method comprises the following steps: reacting 2, 6-pyridine dimethyl carbinol with thionyl chloride to obtain 2, 6-bis (chloromethyl) pyridine; the preparation method comprises the following steps: carrying out a heating reaction on 2-(4-methylphenyl)-1, 2, 4-triazine-2-ketone, N, N ', N'-tri (p-toluenesulfonyl) diethylenetriamine and an inorganic base in a solvent, and carrying out concentrated sulfuric acid deprotection to obtain an intermediate pyclen; the preparation method comprises the following steps: heating and reacting pyrene and halogenated carboxylic ester in a polar organic solvent under an alkaline condition, and hydrolyzing to obtain a ligand product; and heating and chelating the ligand product and a bismuth agent to prepare the target bismuth-based chelate. Laboratory large-scale preparation of the small-molecule bismuth-based chelate CT contrast agent is achieved, and the prepared nonionic contrast agent has low osmotic pressure, high stability, high water solubility and good biological safety and is used for CT imaging of digestion, urinary and circulatory systems.

The application discloses a new method for synthesizing 3-acyl imidazo[1,5-a]pyridine compounds. The method comprises the following steps: adding 2-pyridyl-p-methanequinone (2-Py-p-QMs), terminal alkyne and p-toluenesulfonyl azide (TsN3), catalyst CuI, organic solvent and alkali into a reaction container under the condition of RT and O2 atmosphere, stirring the reaction for 4 hours, and then separating and purifying 3-acyl imidazo[1,5-a]pyridine compounds after the reaction is completed. The method expands the structure range of 3-acyl imidazo[1,5-a]pyridine products, and more compounds with rich structures can be obtained. Compared with the previous method for synthesizing the target product, the method is efficient, the reaction reagent is non-corrosive, the method design is novel, the raw material is cheap, the operation method is simple, and the product can be directly obtained under mild conditions.

The invention provides a preparation method of capicotib, which comprises the following steps: carrying out aromatic nucleophilic substitution (SNAr) on 4-aminopiperidine-4-carboxylic acid and 4-chloro-7-toluenesulfonyl-7H-pyrrole [2, 3-d] pyrimidine to obtain a compound as shown in a formula II, then esterifying under the action of trifluoroacetic anhydride to form a ring to form a compound as shown in a formula III, and carrying out cyclization on the compound as shown in the formula III to obtain the capicotib. The preparation method comprises the following steps: carrying out ring-opening reaction with (S)-3-amino-3-(4-chlorphenyl) propan-1-alcohol without separation under an alkali condition to obtain a compound as shown in a formula IV, and finally removing a toluenesulfonyl protecting group to obtain the carpatinib. The preparation method has the advantages of few reaction steps, mild conditions and short SNAr reaction time, the obtained intermediate compound is easy to purify, the purity and the total yield of the cappitatide can be improved, and the preparation method is suitable for industrial large-scale production.

Disclosed is a phenol-free heat-sensitive recording material comprising: (a) a base material; from one side close to the base material, the coating sequentially comprises: (b) a bottom coating; and (c) a heat-sensitive layer; wherein the heat-sensitive layer includes: a first developer containing a sulfonamide compound represented by the following formula (1): wherein R1 and R2 may be the same or different and each independently represents a hydrogen atom, an alkyl group having 1-4 carbons, an alkoxy group having 1-4 carbons, or a halogen atom; one or more second color developing agents containing at least one phenyl ureide compound represented by the following formula (2): wherein R3 and R4 may be the same or different; and each independently represents a hydrogen atom, a halogen atom, a nitro group, an amino group, an alkyl group, an aryl group, an alkoxy group, an aryloxy group, an alkylcarbonyloxy group, an arylcarbonyloxy group, an alkylcarbonylamino group, an arylcarbonylamino group, an alkylsulfonylamino group, an arsulfonylamino group, a toluenesulfonyl group, a toluenesulfonyloxy phenyl group, a monoalkylamino group, a dialkylamino group, or an arylamino group; and one or more stabilizers selected from the group consisting of compounds represented by formulae (3) and (4) and derivatives thereof.

This invention provides the application of trifluoromethanesulfonyl magnetic nanospheres in chemiluminescent immunoassay. The trifluoromethanesulfonyl magnetic nanospheres are used for direct covalent coupling with antigens or antibodies. The specific preparation method includes first forming epoxy magnetic nanobead micelles, then adding trifluoromethanesulfonyl chloride as a modifier in batches under conditions of 0-25°C to obtain a crude product of trifluoromethanesulfonyl magnetic nanospheres. Then, the particles are screened by column chromatography and centrifugation to obtain the final product of trifluoromethanesulfonyl magnetic nanospheres. The trifluoromethanesulfonyl magnetic nanospheres have stronger thermal stability than p-toluenesulfonyl magnetic nanobeads, eliminating the need for an activation step. Under the action of ammonium sulfate catalyst, they are directly covalently coupled with amino-containing biomacromolecules, reducing antibody cross-linking and magnetic bead aggregation caused by activators such as EDC or glutaraldehyde.

A mild and general method for tosyl protecting group removal from a protected organic nitrogen compound that is additionally suitable for use at commercial scale. A method for the removal of a tosyl protecting group from a protected organic nitrogen compound to form an unprotected nitrogen compound, including azabicyclo[3.1.0]hexane-6-carboxamide derivatives.

The present invention provides a heat-sensitive recording material which has improved thermal responsiveness and improved stability of the print part and the background in comparison to conventional heat-sensitive recording materials that contain a non-phenolic compound as a color developer. The present invention provides a heat-sensitive recording composition which contains a color former, a color developer and a stabilizer, wherein: N-[2-(3-phenylureido)phenyl] benzenesulfonamide or N-(p-toluenesulfonyl)-N′-(3-p-toluenesulfonyloxyphenyl) urea is contained as the color developer, and 1,3-diphenyl urea is contained as the stabilizer.

The invention discloses a high-efficiency and environment-friendly electrochemical method which is used for synthesizing a 4-(iodomethyl)-1-phenyl-3-toluenesulfonyl imidazolidine-2-ketone derivative. The invention further discloses a preparation method of the 4-(iodomethyl)-1-phenyl-3-toluenesulfonyl imidazolidine-2-ketone derivative. Aiming at the problems of tedious steps, harsh conditions, serious pollution and the like of the traditional synthesis method, the method disclosed by the invention takes an alkenyl urea compound which is easy to obtain as a raw material, and realizes efficient synthesis of a target product through a one-step electrochemical iodine cyclization reaction under a mild condition. According to the method, the active iodine species are generated in situ by utilizing an electrochemical means, expensive or toxic reagents are not needed, and the environmental pollution and the synthesis cost are remarkably reduced. The reaction is carried out at normal temperature and normal pressure, the operation is simple and easy to control, and the method has wide substrate applicability. By optimizing reaction conditions, efficient selective synthesis of a target product can be realized. The method has the remarkable advantages of no need of high temperature and high pressure, green and environment-friendly reagents, simple reaction steps and clear product structure. Experimental results show that the method can efficiently synthesize various 4-(iodomethyl)-1-phenyl-3-toluenesulfonyl imidazolidine-2-ketone derivatives, has a good application prospect, and provides a new way for development of related drugs and functional materials. In conclusion, the invention provides a novel strategy with great potential for green synthesis of the imidazolidine-2-ketone compound.

A fluorine-free carbon chain hydrophobic fabric, and its preparation method and application. A fabric is sequentially soaked in an alkali liquor and an acid liquor to obtain a pretreated fabric; the pretreated fabric then reacts with bromoacetyl bromide to obtain a treated fabric; the treated fabric then reacts with 1,2-bis(p-toluenesulfonyl) hydrazine to obtain a diazotized fabric; the diazotized fabric reacts with a diazoacetate monomer to obtain a fluorine-free carbon chain hydrophobic fabric; and the diazoacetate monomer is butyl diazoacetate, hexyl diazoacetate, octyl diazoacetate, dodecyl diazoacetate, tetradecyl diazoacetate or octadecyl diazoacetate. According to the scheme, diazoacetate is used as a monomer, and different fiber grafting modification processes are used, so as to form different structures on the fiber surface; and the comprehensive properties such as thermal stability, air permeability and breaking strength of the finished fabric are tested, the heat resistance and breaking strength of the finished fabric are reduced, and the air permeability is good.

The application discloses a multifunctional electrolyte and a lithium ion battery. The multifunctional electrolyte comprises a first additive and a second additive, the first additive comprises 3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1-p-tolylsulfonyl-1H-pyrrolo[2,3-b]pyridine-5-carbonitrile, and the chemical structure of the second additive is shown in formula I: wherein R1, R2 and R3 are each independently selected from any one of -CH2CF3, -CHCF3CF3 and -CH2CF2CHF2. The application has the advantages of improving the cycle performance and rate performance of the lithium battery and reducing the risk of thermal runaway.

The application discloses a novel bismuth-based chelate CT contrast agent and a preparation method and application thereof. The synthesis method comprises the following steps: 2,6-pyridine dimethyl alcohol is reacted with chlorosulfoxide to obtain 2,6-bis(chloromethyl)pyridine; the 2,6-bis(chloromethyl)pyridine is reacted with N,N',N''-tris(p-tolylsulfonyl)divinyltriamine and an inorganic base in a solvent and is heated, is deprotected by concentrated sulfuric acid to obtain an intermediate pyclen; the pyclen is heated and reacted with a halogenated carboxylic acid ester under alkaline conditions in a polar organic solvent, is hydrolyzed to obtain a ligand product; and the ligand product is heated and chelated with a bismuth agent to obtain the target bismuth-based chelate. The application realizes the laboratory scale preparation of the small-molecule bismuth-based chelate CT contrast agent, and a non-ionic contrast agent is prepared, which has low osmotic pressure, high stability, high water solubility and good biological safety and is used for CT imaging of the digestive system, the urinary system and the circulatory system.

The present application relates to the technical fields of compound synthesis and catalysis, and particularly relates to a precursor compound for preparing a ruthenium catalyst with an oxygen-locked chain type semi-sandwich structure, an intermediate and a preparation method thereof, the precursor compound has the following general formula: wherein R1 is a p-toluenesulfonyl group or a methanesulfonyl group. The synthesis path of the precursor compound is shown as follows: The present application also provides application of the precursor compound in preparation of a key intermediate of a ruthenium catalyst. The method has mild reaction conditions (0-50 DEG C), simple operation, high yield, and the raw materials are easy to obtain, and the purification process is simple, and is suitable for industrialized production.

The invention discloses a heat-triggered in-situ reinforced polyolefin high polymer material and a preparation method thereof, and belongs to the technical field of high polymer materials. The preparation method comprises the following steps: carrying out a ring-opening metathesis polymerization reaction on 9-tosyl-9-azabicyclo [6.1. 0] nonyl-4-ene and cyclooctene under the catalysis of a ruthenium-based catalyst to obtain a ring-opening metathesis polymerization reaction product, mixing the ring-opening metathesis polymerization reaction product with elemental sulfur, and carrying out a cross-linking reaction under the catalysis of an organic alkali to obtain the thermal-trigger in-situ reinforced polyolefin polymer material. The heat-triggered in-situ reinforced polyolefin high polymer material provided by the invention has the characteristics of glass-like high polymers in an initial state, and can realize preliminary recycling of waste materials or precise molding of special-shaped parts; the thermosetting resin also has mechanical properties close to those of traditional thermosetting resin, and can be competent for high-load and high-temperature extreme service environments; the reinforcing process is spontaneously or inductively generated after the part is formed, and additional reinforcing fibers or fillers do not need to be added.

The present invention relates to fungicidal combinations comprising at least two components: (1) a polyphenol-based component and (2) 5-fluoro-4-imino-3-methyl-1-tosyl-3,4 dihydropyrimidin-2(1H)-one represented by the following structure,

The invention relates to a p-toluenesulfonyl functionalized fluorescent probe capable of being specifically combined with a histidine label and application of the p-toluenesulfonyl functionalized fluorescent probe in single-molecule FRET (Fluorescence Resonance Energy Transfer) research. The probe is based on a Cyanine 5 dye, and can realize covalent binding with a protein with a His-tag by performing chemical modification on toluenesulfonyl. Compared with a traditional Ni < 2 + >-NTA non-covalent fluorescent probe, the probe provides higher binding stability and site specificity, and is suitable for high-resolution single-molecule fluorescence imaging of protein. The invention further establishes a protein fluorescence labeling strategy which is suitable for smFRET analysis and is universal, simple and convenient to operate and stable in labeling, and a novel technical means is provided for exploring protein conformation change and a dynamic regulation and control mechanism.

The present invention provides a synthesis method for fezolinetant, comprising: using (R)-3-methylpiperazin-2-one compound 1 as a starting material, first using p-toluenesulfonyl chloride to protect amino groups, to obtain (R)-3-methyl-4-p-toluenesulfonylpiperazin-2-one compound 2, then performing an alkylation reaction to activate amides, to obtain compound 3; compound 3 producing (R)-3-methyl-5-(8-methyl-7-p-toluenesulfonyl-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]piperazin-3-yl)-1,2,4-thiadiazole compound 7 by means of two pathways; finally, deprotecting and salifying compound 7 to obtain compound 8, and compound 8 undergoing a condensation reaction with compound 9, to yield a final product of fezolinetant, compound 10. This route is simple in operation, provides a relatively high overall yield, obtains a product having high purity, and is suitable for scaled-up production.

This invention discloses a multifunctionalized pyridine compound, its preparation method, and its applications, belonging to the fields of pharmaceutical intermediates and organic synthesis. The invention uses α-allyl-p-toluenesulfonylmethylene isonitrile and substance A as raw materials, and a free radical cyclization reaction is carried out under the action of a catalyst to obtain a highly functionalized pyridine compound, as shown in formula (Ⅰ). Substance A is phenylboronic acid, cyclohexylboronic acid, [1,1'-biphenyl]-4-boronic acid, p-methylphenylboronic acid, m-methylphenylboronic acid, o-methylphenylboronic acid, p-cyanophenylboronic acid, thiophene-3-boronic acid, or cyclopropylboronic acid. The method of this invention not only has very broad substrate tolerance, inexpensive and readily available raw materials, and a simple reaction process suitable for large-scale synthesis, but also provides a new method for pharmaceutical chemical synthesis. Furthermore, due to the high functionalization and special structure of the pyridine compound, it exhibits better efficacy in treating chronic stable angina pectoris, central respiratory depression and circulatory failure, and in the treatment of various organoiodinated phosphate poisonings.

The invention provides a method for preparing kasatinib, a novel intermediate used in the method and application of the novel intermediate, and belongs to the field of medicine preparation. According to the method for preparing the kasatinib, a protecting group is introduced to a key starting material azaindole ring (pyrrolopyrimidine) for synthesizing the kasatinib, the protecting group is selected from p-toluenesulfonyl (Tos), t-butyloxycarboryl (Boc) and (trimethylsilyl) ethoxymethyl (SEM), the reaction yield is increased, the total yield reaches 58.4%, and the material cost is reduced.

The invention belongs to the technical field of photoelectric materials, and particularly relates to a perovskite thin film based on N-p-toluenesulfonyl-L-arginine modification, a preparation method of the perovskite thin film and a solar cell. N-p-toluenesulfonyl-L-arginine is added into a CsPbI2Br perovskite precursor solution, and a CsPbI2Br perovskite thin film grows by adopting stage spin coating and gradient annealing. Through the interaction between the N-p-toluenesulfonyl-L-arginine and the CsPbI2Br perovskite thin film, the light absorption performance, the luminescence performance, the room-temperature black phase stability, the air stability and the optical stability of the CsPbI2Br perovskite thin film are remarkably improved, so that the photoelectric conversion efficiency and the stability of a device are remarkably improved. The material system shows excellent characteristics in photovoltaic power generation application, the thin film prepared based on the technology can effectively improve the energy conversion efficiency of photoelectric devices such as solar cells and the like, a feasible technical path is provided for industrial application of new-generation efficient solar cells, and the material system has remarkable market application value and industrial prospects.

The invention discloses a synthesis method of (S)-(-)-1-(4-methoxyphenyl) ethylamine and an intermediate compound thereof, and belongs to the technical field of synthesis of medical intermediates. The method comprises the following steps: by taking p-methoxyacetophenone as an initial raw material, carrying out asymmetric reduction to obtain a chiral alcohol mixture, condensing the chiral alcohol mixture with N-p-toluenesulfonyl-L-proline, and recrystallizing to enrich an intermediate compound (R)-3A; further, the (R)-3A is subjected to alkaline hydrolysis, azidation and reduction reaction to obtain the (S)-(-)-1-(4-methoxyphenyl) ethylamine. According to the method, preparation of high-optical-purity (S)-(-)-1-(4-methoxyphenyl) ethylamine is achieved through the strategy of chiral introduction-configuration enrichment-functional group conversion, the chiral purity of the product is larger than 99%, a customized high-price catalyst is replaced with a conventional commercial reagent, a key intermediate can be recycled and reused, operation is easy and convenient, cost is controllable, environment friendliness is achieved, and the method is suitable for industrial production. The method is suitable for industrial large-scale production.

The present invention relates to fungicidal mixtures containing 5-fluoro-4-imino-3-methyl-1-(p-tolylsulfonyl) pyrimidin-2-one as compound I) and at least one active compound II and at least one active compound III. The invention also relates to an agrochemical composition comprising the composition and a solvent of a solid carrier. In addition, the invention relates to the non-therapeutic use of the composition of the invention to control phytopathogenic harmful fungi.

The present invention provides a process for preparing a compound having the formula (I):whereinR is alkyl or alkylaryl;each of X1, X2, X3, X4 and X5 is, independently, H, alkyl, alkenyl, alkynyl, alkoxy, haloalkyl, haloalkoxy, alkylthio, haloalkylthio, amino, alkylamino, dialkylamino, alkoxycarbonyl, alkyl carbonyl, hydroxyalkyl, ester, acid halogen, —SH, —OH, —NH2, —NO2, —CN or CF3;Y is O or S; andand Z is a halogen.

The present invention discloses a method for preparing a series of vonoprazan intermediates using an isonitrile and a Michael acceptor. In the method of the present invention, α-(p-toluenesulfonyl)-2-fluorobenzylisonitrile is used as the starting material, which attacks a series of Michael acceptors under basic conditions and undergoes cyclization to form a series of 3-substituted 5-(2-fluorophenyl)-1H-pyrroles. These 3-substituted pyrrole intermediates can be further chemically transformed to prepare vonoprazan. Compared with the prior art, the technical means of the present invention are characterized by a short synthetic route, high overall yield, simple post-treatment, and low cost.

This invention belongs to the field of biomedical technology, specifically relating to a dihydroporphyrin e6 conjugate and its applications. Using dihydroporphyrin e6 and N-p-toluenesulfonyl ethylenediamine as raw materials, an N-p-toluenesulfonyl ethylenediamine-dihydroporphyrin e6 conjugate is prepared by condensation; then, the N-p-toluenesulfonyl ethylenediamine-dihydroporphyrin e6 conjugate is condensed with excess galactosamine hydrochloride to prepare an N-p-toluenesulfonyl ethylenediamine-dihydroporphyrin e6-digalactosamine conjugate. This conjugate exhibits improved water solubility and can target liver cancer cells and the intracellular endoplasmic reticulum, showing potential application value in the field of photodynamic immunotherapy for liver cancer.

The present invention provides stable, liquid compositions comprising (a) a fungicidally effective amount of a compound of Formula I and (b) a liquid carrier. The present invention also provides mixtures and compositions comprising (a) a fungicidally effective amount of a compound of Formula I and (b) at least one adjuvant selected from the group consisting of: (i) polyalkylene oxide alkyl ether; (ii) siloxane polyalkyleneoxide copolymer; (iii) esters of fatty acid; (iv) vinylpyrrolidones and derivatives thereof; and (v) sugar-based surfactants. The present invention also provides methods of use of the mixtures and compositions disclosed herein and processes of preparing the mixtures and compositions disclosed herein.

The application discloses a nirmatrelvir intermediate and a preparation method and application thereof, and belongs to the technical field of drug synthesis. The nirmatrelvir intermediate and the preparation method thereof are characterized in that 3-methyl-2-butenal is used as a starting material, and a first reactant is obtained through reductive amination reaction of the 3-methyl-2-butenal and benzylamine; acylation reaction of the first reactant and bromoacetyl bromide is performed to obtain a second reactant; under the condition that tetramethylguanidine is used as an alkali, diazotization reaction of the second reactant and N,N'-bis(p-tolylsulfonyl)hydrazine is performed to obtain a diazo compound; and the diazo compound is catalyzed by a metal catalyst to obtain a chiral pure cyclopropane compound, namely the nirmatrelvir intermediate. The method for preparing the nirmatrelvir intermediate has the advantages that a metal catalyst is used for catalysis, the reaction condition is mild, and the ee value of the obtained target product can reach 92.6%.

The invention belongs to the field of synthetic chemistry and biological medicine, and particularly relates to a difluoromethyl modified chiral diamine derivative as well as a synthetic method and application thereof. The difluoromethyl modified chiral diamine derivative is obtained by taking p-toluenesulfonyl difluoromethyl diazomethane, aromatic amine, organic aldehyde and electron-rich aromatic hydrocarbon as raw materials and taking chiral phosphoric acid as a chiral inducer and an organic reagent as a solvent through a one-step reaction under the catalysis of transition metal. According to the difluoromethyl modified chiral diamine derivative and the synthesis method, the raw materials are cheap and easy to obtain, safe and non-toxic, the reaction condition is mild, the operation is simple and safe, and the synthesized difluoromethyl modified chiral diamine derivative has good anti-tumor activity and has huge development potential in the field of drug research and development.