52 results about "Tosyl" patented technology

The invention relates to a nitrogen-containing bowl-shaped conjugated pH-responsive fluorescent probe and a preparation method and application thereof, the nitrogen-containing bowl-shaped conjugated pH-responsive fluorescent probe is characterized in that the structural formula of the nitrogen-containing bowl-shaped conjugated pH-responsive fluorescent probe is # imgabs0 #, and R is hydrogen, acetyl or p-toluenesulfonyl. Compared with the prior art, the nitrogen-containing bowl-shaped conjugated molecule provided by the invention shows a highly sensitive response characteristic in an acid-base medium. Due to the introduction of nitrogen atoms, the electronic structure of molecules is obviously changed, lone pair electrons of the nitrogen atoms can participate in the reaction, and the protonation behavior is obvious under the acidic condition. After protonation, the fluorescence intensity of the molecule is obviously enhanced, and the emission wavelength has obvious red shift, so that the probe has important application value in the aspect of developing a high-sensitivity acid-base sensor. In addition, the nitrogen-containing polycyclic aromatic hydrocarbon compound also shows application prospects in the fields of organic light-emitting diodes, information safety, biological imaging and the like.

A fungicidal composition containing a fungicidally effective amount of the compound of Formula I:5-fluoro-4-imino-3-methyl-1-tosyl-3,4-dihydropyrimidin-2(1H)-one, and at least one fungicide to provide synergistic control of selected fungi wherein the at least one fungicide is a fungicidal sterol biosynthesis-inhibitor.

The invention is applicable to the technical field of fuel cells, and provides a blending modified polybenzimidazole proton exchange membrane and a preparation method thereof, and the preparation method comprises the following steps: S1, preparing 4-methyl-N-toluenesulfonyl benzene sulfonamide; s2, preparing 4, 4 '-[imino bis (sulfonyl)] dibenzoic acid; s3, preparation of PSI: dissolving CBSI and a proper amount of anhydrous lithium chloride in a proper amount of a mixed solution of pyridine, triphenyl phosphite and pyrrolidone, adding diamino molecules after complete dissolution, heating and stirring the solution for 12 h, pouring the solution into methanol, filtering and collecting a product, washing with water, and drying to obtain the product PSI; and S4, preparing the PSI / OPBI blended membrane. The blended membrane prepared by the invention has excellent proton conductivity and good mechanical properties, and meets the performance requirements of the proton exchange membrane of the fuel cell; moreover, the raw materials are low in cost and easy to obtain, the synthesis conditions are mature, the yield is high, the feasibility is high, and the application prospect is wide.

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.

A fungicidal composition containing a fungicidally effective amount of the compound of Formula I:5-fluoro-4-imino-3-methyl-1-tosyl-3,4-dihydropyrimidin-2(1H)-one, and at least one fungicide to provide synergistic control of selected fungi wherein the at least one fungicide is a multi-site inhibitor or a strobilurin inhibitor.

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 method for preparing an olaparib key intermediate compound as shown in a formula (1). The method comprises the following steps: (a) reacting a compound as shown in a formula (2) with a compound as shown in a formula (3) to generate a compound as shown in a formula (4); (b) carrying out intramolecular cyclization on the compound as shown in the formula (4) under the catalysis of acid to generate a compound as shown in a formula (5); (c) hydrolyzing the compound as shown in the formula (5) in an alkali solution, and acidifying to obtain a compound as shown in a formula (1); wherein in the compounds as shown in the formula (3), the formula (4) and the formula (5), R is formyl, acetyl, propionyl, butyryl, benzoyl, methoxycarbonyl, ethoxycarbonyl, t-butyloxycarbonyl, methylsulfonyl, benzenesulfonyl or p-toluenesulfonyl. The invention also discloses a compound shown in a formula (4) or a formula (5). The method is high in yield, mild in reaction condition, easy to purify and suitable for industrial large-scale production. # imgabs0 #

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.

Disclosed in the present invention is a preparation method for 4-((1-hydroxy-1,3-dihydrobenzo[c][1,2]oxaborol-5-yl)oxy)benzonitrile, comprising the following steps: in an organic solvent, under an alkaline condition, enabling compound II and compound III to be subjected to a substitution reaction as shown in the following, wherein R is hydrogen, sulfonyl or p-toluenesulfonyl, and X is F, Cl, or Br. The preparation method of the present invention avoids the use of noble metal as a catalyst, involves low costs, simple operation and high product yield, and is suitable for industrial production.

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 fungicidal composition containing a fungicidally effective amount of the compound of Formula I:5-fluoro-4-imino-3-methyl-1-tosyl-3,4-dihydropyrimidin-2(1H)-one, and at least one fungicide to provide synergistic control of selected fungi wherein the at least one fungicide is a multi-site inhibitor or a strobilurin inhibitor.

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 fungicidal composition containing a fungicidally effective amount of the compound of Formula I:5-fluoro-4-imino-3-methyl-1-tosyl-3,4-dihydropyrimidin-2(1H)-one, and at least one fungicide to provide synergistic control of selected fungi wherein the at least one fungicide is a fungicidal sterol biosynthesis-inhibitor.

The invention provides a paratoluensulfonyl-containing magnetic polymer microsphere as well as a preparation method and application thereof. The preparation method comprises the following steps: firstly, coating the surface of the magnetic polymer microsphere with a benzene ring-containing polymer; then sequentially carrying out chloromethyl modification, hydroxyl modification and p-toluenesulfonyl chloride modification on the magnetic polymer microspheres coated with the benzene ring polymer, so as to obtain magnetic polymer microspheres containing p-toluenesulfonyl; the preparation method has the advantage of high group utilization rate, and the prepared paratoluensulfonyl-containing magnetic polymer microspheres have the advantages of high detection accuracy, low physical adsorption of non-target objects and the like, and can be applied to multiple aspects of targeted capture, separation and purification and the like.

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 relates to the field of agricultural protection technology, in particular to a leucine salt derivative and its application in preventing and controlling plant viruses and sterilizing. The leucine salt derivative includes a compound represented by formula (I): #imgabs0# wherein R 1 Includes at least one of hydrogen, methyl, methoxy, F, Cl, Br, I and cyano; R 2 Includes at least one of hydrogen, methyl, methoxy, F, Cl, Br, I, trifluoromethyl and methoxycarbonyl; R 3 including at least one of methyl, cyclopropylmethyl, cyclohexylmethyl, 2,2-dimethylpropyl and benzyl; R 4 The leucophylline salt derivatives have good plant virus prevention and control and good fungicidal activity.

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.