132 results about "Para-nitrophenyl" patented technology

The present invention provides an acid sensitive doxorubicin prodrug based on polyethylene glycol, and a method and an application of the acid sensitive doxorubicin prodrug based on polyethylene glycol. The preparation method comprises: preparing a polyethylene glycol whose end contains an acid sensitive acetal group and a p-nitrophenyl ester azide group by a reaction of a polyethylene glycol whose double ends contain diazido ethyl diacetal groups with a p-nitro phenyl propargyl carbonate; preparing the acid sensitive doxorubicin prodrug based on the polyethylene glycol by the reaction of the prepared polyethylene glycol with doxorubicin hydrochloride. The acid sensitive and water soluble doxorubicin prodrug has good biocompatibility and acid sensitivity, thereby being used as a stimulation sensitive antineoplastic prodrug.

Immunogenic compositions, cancer vaccines and methods for treating cancer are provided. Compositions comprising: (a) a glycan such as Globo H or an immunogenic fragment thereof, wherein the glycan is conjugated with a carrier protein by a linker such as para-nitrophenyl; and (b) an adjuvant comprising glycolipid capable of binding CDId on a dendritic cell, such as an a-galactosyl-ceramide derivative, wherein the immunogenic composition induces an immune response that induces a higher relative level of IgG isotype antibodies as compared to IgM isotype antibodies, are provided. Immunogenic compositions comprising the carrier protein diphtheria toxin cross-reacting material 197 (DT-CRM 197) and the adjuvant C34 are provided. Antibodies generated by immunogenic compositions disclosed herein further neutralize at least one of the antigens Globo H, stage-specific embryonic antigen-3 (SSEA-3) and stage-specific embryonic antigen-4 (SSEA-4). Therapeutics against breast cancer stem cells comprising immunogenic compositions comprising Globo H, SSEA-3 or SSEA-4 conjugated with DT-CRM 197.

The invention discloses an anti-tumor macromolecule bonding drug with a multidrug synergistic effect and a preparation method thereof. The preparation method comprises the steps of sequentially triggering the polymerization of lactide containing norbornene and alpha bromination caprolactone through methoxy polyethylene glycol so as to obtain a triblock copolymer; modifying a p-nitrophenyl formic ether lateral group and a carboxyl lateral group on the triblock copolymer so as to obtain a polymeric carrier; bonding the polymeric carrier, an anti-tumor drug containing hydroxyl and an anti-tumor drug containing amino so as to obtain the anti-tumor macromolecule bonding drug. The preparation method is simple to operate, moderate in reaction conditions, less in side reaction, high in yield, large in drug loading capacity, controllable, and high in product purity; according to the prepared anti-tumor macromolecule bonding drug, the anti-tumor activity is improved through a various signal channel effect (the synergistic effect), and meanwhile, due to the joint action of various drugs, the dosage of each drug can be reduced, so that a toxic and side effect of chemotherapy is reduced.

The invention discloses a method for preparing acetovanillone and acetosyringone (AS) through oxidation of lignin by using an oxidizing agent. According to the method, an oxidizing agent reacts with the lignin in an alkaline solution; the resulting reaction solution is subjected to acidification, extraction and concentration to obtain the crude product after completing the reaction; the treatments of recrystallization and rectification are performed to obtain the acetovanillone and the AS. The oxidizing agent is the one selected from p-nitrobenzoic acid, 3,5-dinitrobenzoic acid, 3-nitrosalicylic acid, 5-nitrosalicylic acid or 3,5-dinitrosalicylic acid. According to the present invention, the oxidizing agent has low toxicity, such that the harm to the environment can be reduced; the post-treatment steps are simplified, and the uses of the organic solvents are reduced, such that the secondary pollution to the environment is reduced; the yield is relatively high, the purities of the products are respectively 97.3% and 98.2% through the gas chromatography analysis; the two important chemical raw materials of guaiacol and lilac alcohol can be synchronously obtained when preparing the acetovanillone and the AS.

The invention provides a method for preparing an electrolyte for a chip aluminum electrolytic capacitor. The method comprises the following steps of: (1) weighing: weighing raw materials; (2) dissolving: adding ethylene glycol into a container with a stirrer and a thermometer, raising the temperature to 60 DEG C by using a closed electric heater, sequentially adding polyethylene glycol, 1,7-ammonium-sebacate, ammonium sebacate, 1,7-dimethyl-ammonium-sebacate, mannitol, ammonium hypophosphite, paranitrobenzoic acid or para-nitrophenyl methanol, and oxirane and epoxypropane copolyether, heating to 130 DEG C, and stirring to totally dissolve the components; and (3) cooling: standing and cooling to room temperature to obtain the electrolyte. The technology is simple, the condition is easy to control, and the preparation method is suitable for scale production. The invention also provides an electrolyte which has the characteristics of high temperature resistance, high spark voltage and long service life, and is applicable for making the chip aluminum electrolytic capacitor.

The invention relates to oligoarginine modified phospholipid, nanoparticles assembled by the oligoarginine modified phospholipid, a preparation method of the oligoarginine modified phospholipid and an application of the nanoparticles. After oligoarginine peptide chains are activated by DCC (dicyclohexylcarbodiimide)/NHS (N-hydroxysuccinimide), the oligoarginine peptide chains react with phosphatidyl ethanolamine, purification is performed, and oligoarginine modified phosphatidyl ethanolamine is obtained; or the oligoarginine peptide chains react with DCC/NHS activated phosphatidic acid, and oligoarginine modified phosphatidic acid is obtained through purification; or the oligoarginine peptide chains react with nitrophenyl chloroformate activated phosphatidylcholine, and oligoarginine modified phosphatidylcholine is obtained through purification. The nanoparticles assembled by the oligoarginine modified phospholipid is used for supporting genes, small-interfering RNA, polypeptides or proteinic drugs, antibodies and chemical drugs, and the formed aqueous dispersion of the drug-carrying nanoparticles is used for delivering drugs for in-vitro cells or in-vivo local intravenous injection. The nanoparticles are effectively promoted to enter the cells, and the intracellular drug delivery efficiency is improved.

The invention discloses photocatalytic coating. The photocatalytic coating is prepared from the following raw materials in parts by weight: 50-60 parts of water-based fluorocarbon resin emulsion, 15-59 parts of AS resin I, 1-10 parts of AS resin II, 0.1-0.2 part of nano carbon dioxide, 3-6 parts of anatase type lanthanum sulfide co-doped nano titanium dioxide, 5-25 parts of heat conducting filler, 0.25-2.5 parts of infrared reflection titanium dioxide, 0.1-0.5 part of a light stabilizer, 0.5-5 parts of a chemical resistant modifying agent, 0.5-1.5 parts of tea polyphenol, 2-4 parts of folium artemisiae argyi oil, 2-4 parts of vanillic aldehyde, 2-4 parts of thymol, 10-20 parts of acrylpimaric(2-p-nitrophenyl)thiadiazole, 1.5-2 parts of pigment and 0.5-2 parts of other auxiliaries. The photocatalytic coating can carry out good catalytic degradation and purification on gaseous pollutants in the air environment and also has good weather resistance, contamination resistance, corrosion resistance and antibacterial property.

The invention relates to a pichia pastoris gene engineering strain for producing lipase and a building method of the pichia pastoris gene engineering strain. During the enzymic catalytic reaction of the lipase, if the reaction promotes esterolysis in the oil-water interface, enzymatic synthesis and ester exchange can be achieved in the organic phase, and accordingly biodiesel can be synthesized by using waste edible oil, waste industrial oil and low-carbon alcohol as the raw materials. The lipase is massively fermented by transferring recombinant lipase Lip14 genes into pichia pastoris X33. P-nitrophenyl palmitate is used as the substrate to measure the long-chain lipid hydrolysis ability of the lipase, p-nitrophenyl laurate and p-nitrophenyl octoate are used to measure the medium-chain lipid hydrolysis ability of the lipase, p-nitrophenyl butyrate is used to measure the short-chain lipid hydrolysis ability of the lipase, and accordingly the long-chain, medium-chain and short-chain lipid hydrolysis activity of the lipase can be determined and a foundation is laid for the application of the lipase to the catalytic production of biodiesel.

The invention relates to a method for preparing p-aminophenyl-beta-hydroxyethyl sulfone, in particular to a method for preparing beta-hydroxyethyl sulfone. The method solves the problems of high production cost, difficulty in catalyst recycling, low product yield and serious pollution to the environment existed in the prior art for preparing the p-aminophenyl-beta-hydroxyethyl sulfone. The method is as follows: p-aminophenyl-beta-hydroxyethyl sulfide and nickel aluminium alloy catalyst and solvent are added in a hydrogenation reactor; after nitrogen which removes off the air is introduced, hydrogen is introduced and the pressure of the hydrogen is controlled at 0.5MPa to 6MPa; meanwhile, stirring is carried out at the speed of 500r/min to 1000r/min and the temperature is raised to 40 DEG C to 100 DEG C for reaction for 4h to 12h; after filtration, distillation and drying, the p-aminophenyl-beta-hydroxyethyl sulfone is obtained. The method has the advantages of low production cost, easy-recycling catalyst, high product yield, high product pureness and less pollution to the environment. The pureness of the product is more than 97 percent and the yield is more than 95 percent (calculated by nitro compounds).

A novel analog of thalidomide and its preparing process are disclosed.

The invention discloses traditional Chinese medicine composition with antibacterial and anti-inflammation effects and a preparation method of the composition. The traditional Chinese medicine composition is prepared from 5-15 parts of Rumex crispus, 10-15 parts of dandelions, 5-10 parts of original aloe juice, 3-7 parts of lemon ferment powder, 6-10 parts of pine needle powder, 3-15 parts of common cnidium fruits, 3-17 parts of caulis lonicerae, 3-10 parts of an olive leaf extract, 5-10 parts of a red date leaf extract, 6-10 parts of a milk thistle extract, 4-10 parts of a cranberry extract and 10-15 parts of a rosin derivative which is acrylpimaric acid(2-p-nitrophenyl)thiadiazole. A special technology is adopted, multiple effective ingredients are obtained, and the scientific ratio is adopted, so that the obtained composition has significant antibacterial and anti-inflammation effects and is safe to use and free of side effects.

Disclosed herein are mixed steroidal tetraoxanes having the following structural formula 1

wherein n is 0, 1, 2, or 3; R is H; ethanoyl, propanoyl, or benzoyl; R1 is H, methyl, ethyl, or isopropyl; R2 is H, methyl, or ethyl; R3 is H, methyl, or ethyl; R4 is H, methyl, ethyl, tert-butyl, phenyl, p-hydroxyphenyl, p-methoxyphenyl, or p-nitrophenyl, or

wherein Y is a C₁-C₄ straight or branched-chain alkoxy, or

wherein W is N, R5 is hydrogen, methyl, ethyl, n-propyl, isopropyl, or methyl ethanoate 2-yl, and R6 is hydrogen, methyl, ethyl, or n-propyl, or R5 and R6 are part of a pyrrolidine or piperidine ring; X is a C₁-C₄ straight or branched-chain alkoxy, a primary amino, a N-alkylamino wherein the alkyl is a straight-chain alkyl groups containing from 1 to 4 carbon atoms, methyl ethanoate-2-yl, N-phenylamino, p-nitrophenyl, N,N-dimethylamino, N,N-diethylamino, N,N-di(n-propyl)amino, N-pyrrolidino, or N-piperidino as single compounds, and any mixture of all possible stereoisomers at C(4″). n may be 0, 1, 2, or 3, and methods of making and using thereof. As disclosed herein, the mixed steroidal tetraoxanes of the present invention exhibit antimalarial, antibacterial, and antiproliferative activity. Thus, as disclosed herein, the mixed steroidal tetraoxanes of the present invention may be used to treat, prevent, or inhibit malaria, bacterial infections, and diseases and disorders associated with cell proliferation in a subject.

The present invention discloses one kind of forcipated diimidazoline palladium compound in the structure as shown and its application in Suzuki reaction. The forcipated diimidazoline palladium compound is synthesized through heating and refluxing diimidazoline benzene and palladium acetate in glacial acetic acid, the subsequent evaporating to dry, adding acetone/water solution of lithium chloride, stirring at room temperature to extract, drying, concentrating and thin-layer chromatographic separation. The compound is used in catalyzing coupling Suzuki reaction to synthesize biaryl compound.

The invention discloses a 2-thiazolyl acrylonitriles coumpound, a synthesis process and an application. The structure of 2-thiazolyl acrylonitriles is showed as formula (I), wherein R is C1-C10 alkyl, C1-C5 halogenated alkyl, C3-C6 cycloalkyl, phenyl, benzyl or p-nitro phenyl. The synthesis process of the invention comprises conducting nucleophilic substitution towards2- cyanide-4-(2, 6-difluorophenyl) thiazole showed as formula (II) and acyl chloride showed in formula (III) in protonic solvent or nonprotonic solvent for 1-20h with 0-100 DEG C under the effect of acid binding agent to obtain reaction solution, and treating reaction solution to obtain 2-thiazolyl acrylonitriles compound. The 2-thiazolyl acrylonitriles compound can be used as herbicide, pesticide and pesticide, and adds new matters for the screening of herbicide, pesticide and pesticide.

The invention discloses a method for the effective synthesis of optically active oxazoline-2-ketone derivative. The optically active oxazoline-2-ketone derivative has a structure represented by the formula (I), wherein, R is phenyl, para-methoxyphenyl, para-chlorophenyl, para-fluorophenyl, ortho-chlorophenyl, ortho-methoxyphenyl, meta-bromophenyl, 1-naphthyl, para-bromophenyl, para-nitrophenyl, para-methylphenyl or 3,4-difluorophenyl; R is phenyl, para-methylphenyl, para-methoxyphenyl, para-fluorophenyl, para-chlorophenyl, para-bromophenyl or 2-furyl. Such compounds can be obtained by means of high diastereoselectivity and high enantioselectivity of tandem reaction of organically catalytic C2 symmetrical chiral sulfur ylide and nitroolefin.

The invention relates to a process for preparing chiral (R)- or (S)-1,1'-bi-2-naphthol, which comprises mixing racemic or non-racemic 1,1'-bi-2-naphthol and chiral inclusion agent by the mol ratio of 1.0:0.5-3.0 in organic polar solvent, heating, dissolving and cooling down for evolution of inclusion compound and crystallizing, decomposing the inclusion compound crystallization to obtain (S)-1,1'-bi-2-naphthol, evaporating the mother liquor, crystallizing the purifying the residue to obtain (R)-1,1'-bi-2-naphthol, the chiral inclusion agent is chloride (1S,2S)-1,3-dihydroxyl-1(nitrophenyl)-2-(N-benzyl-N,N-dimethyl) propanaminiumchloride.

The invention relates to a sulfur-containing heterocyclic compound. The compound is 2-sulfohydantoin; a chemical structure of the 2-sulfohydantoin is shown in a formula (I) in the specification; and in the formula (I), R is one of C1-12 alkyl, p-nitrophenyl, p-cyano phenyl, p-methoxyphenyl, p-butyl phenyl, 3,5-di(trifluoromethyl)phenyl and phenyl. The 2-sulfohydantoin is obtained by reacting isothiocyanate with para hydroxy phenylglycine methyl ester, has an anion recognition performance, and can be used for detecting fluorinion.

The invention discloses p-nitrophenoxy betulin (28) formyl ester and betulin derivatives synthesized therefrom, and a preparation method and an application thereof, and belongs to the technical fieldof pharmaceutical chemical. Four derivatives are synthesized with betulin as a matrix, that is to say, the tail end of a structure of the betulin is modified, a carbonacylation agent nitrophenyl chloroformate is introduced to a C-28 site, p-nitrophenoxy betulin (28) formyl ester is generated, and based on the p-nitrophenoxy betulin (28) formyl ester, four kinds of groups having biological activityand functionality are introduced. Specifically, with introduction of a structure of aminoethyl alcohol, the solubility is improved; with introduction of an N-amino morpholine group having a lysosomepositioning action and a triphenylphosphine active group having mitochondria targeted positioning, the product targetedly acts on cell organelles, the bioavailability is improved, and the higher biological activity is played; with introduction of a p-aminophenol structure, the synthesized compounds have certain antioxidant effects, and certain pharmacological activities are played by regulating the balance of redox in cells.

The invention relates to a preparation method of a PEGylated dendritic macromolecule drug carrier, which comprises the following steps of: mixing trimethylolpropane triacrylate and ethylenediamine inan ice-water bath, reacting alternately in an organic solvent in a protective atmosphere at the reaction temperature of 25-60 DEG C, obtaining an amino-terminated dendritic macromolecule using ethylenediamine as a core or an acrylate-terminated dendritic macromolecule using trimethylolpropane triacrylate as a core; dissolving PEG, p-nitrophenyl chloroformate and triethylamine in an organic solvent, reacting at 20-30 DEG C, and obtaining PEGylated p-nitrophenyl carbonate after the reaction is complete; reacting the amino-terminated dendritic macromolecule using the ethylenediamine as the core or acrylate-terminated dendritic macromolecule using the trimethylolpropane triacrylate as the core with the PEGylated p-nitrophenyl carbonate in an organic solvent at a reaction temperature of 20-30 DEG C. The method is easy to operate, high in yield and low in cost; and the prepared drug carrier has excellent drug carrying performance on drugs which are difficult in dissolving in water.

The invention discloses a lysine-based polyesteramide nano drug delivery system as well as a preparation method and application thereof. The preparation method of the polyesteramide polymer includes the following steps: synthesizing a dicarboxylic acid di-p-nitrophenyl ester monomer; synthesizing a di-lysine di-p-toluenesulfonate ester monomer; and adding the dicarboxylic acid di-p-nitrophenyl ester monomer and the di-lysine di-p-toluenesulfonate ester monomer according to a mass ratio of equal to or less than 1:1 into a reaction solvent, adding triethylamine dropwise under stirring at 65-85 DEG C as a reaction catalyst, and performing a heating reaction at 60-80 DEG C for 24-96 h to obtain the polyesteramide polymer with good water solubility. The polyesteramide polymer can efficiently load and deliver and controllably release water-soluble protein drugs, has good biosecurity and drug release, and significantly improves the stability and bioavailability of the protein drugs in a systemic circulation.