89 results about "Azacyclopropane" patented technology

Dry powder formulations of drugs such as antihistamine for nasal administration are provided where the drug is retained in the nasal cavity, and systemic side effects minimized or eliminated, through the selection of a narrow particle size range, between approximately 10 and 20 microns in diameter. In a preferred embodiment wherein the drug is an antihistamine, retention of the antihistamine at the nasal mucosa is improved and the bitter aftertaste associated with liquid antihistamine formulations significantly reduced. By making a dry powder formulation of an antihistamine (e.g., azelastine) having an average particle size of between 10 and 20 microns, the antihistamine is restricted primarily to the desired target organ, the nasal mucosa. Because the active ingredient stays in the nasal region, a lower dose can be used to achieve the same desired effect. As demonstrated by the examples, this lower dose reduces the incidence of somnolence, and because the active ingredient remains at the target organ and does not accumulate in the back of the throat and mouth, this formulation does not impart a bitter taste.

Dry powder formulations of drugs such as antihistamine for nasal administration are provided where the drug is retained in the nasal cavity, and systemic side effects minimized or eliminated, through the selection of a narrow particle size range, between approximately 10 and 20 microns in diameter. In a preferred embodiment wherein the drug is an antihistamine, retention of the antihistamine at the nasal mucosa is improved and the bitter aftertaste associated with liquid antihistamine formulations significantly reduced. By making a dry powder formulation of an antihistamine (e.g., azelastine) having an average particle size of between 10 and 20 microns, the antihistamine is restricted primarily to the desired target organ, the nasal mucosa. Because the active ingredient stays in the nasal region, a lower dose can be used to achieve the same desired effect. As demonstrated by the examples, this lower dose reduces the incidence of somnolence, and because the active ingredient remains at the target organ and does not accumulate in the back of the throat and mouth, this formulation does not impart a bitter taste.

The invention discloses a method for performing ring-opening for cyclohexylaziridine by a carboxylic acid. The method includes that in a polar aprotic solvent system, alkali metal type inorganic base is utilized as a catalyst, a monocarboxylic acid is utilized as a nucleophilic reagent, and the cyclohexylaziridine which is activated by tosyl is subjected to a ring-opening reaction. The method has the advantages that the ring-opening reaction is simple in process, the reaction condition is mild, the solvent is environment-friendly, the carboxylic acid is utilized as the nucleophilic reagent, atom economical requirement of green chemistry is met, the catalytic agent is cheap, and the catalytic activity is high.

The invention provides a novel preparation method for taurine, substituted taurine and N-acylated derivates. The method comprises taking aziridine and substituted aziridine as raw material, obtaining N-acylated taurine derivates by opening loop and oxygenizing, hydrolyzing N-acylated taurine derivates to obtain taurine or substituted taurine. The raw material of the preparation method is simple and easy to get and prepare, especially convenient to separate and purify, and can be used for the preparation of optical activity substituted taurine and N-acyl group substituted taurine. The obtained compounds can be used as nutrient substance, medicament, enzyme inhibitors, antibacterial agents, surface active agents, plant growth regulators and raw materials for preparing sulfonopeptides.

The invention discloses water solubility high-speed grinding fluid for machining a settlement bearing. The water solubility high-speed grinding fluid comprises the following components by weight percent: 1 to 5 percent of settlement additive; 15 to 25 percent of mineral oil, 5 to 10 percent of synthetic ester, 2 to 5 percent of organic acid, 8 to 15 percent of organic amine, 5 to 10 percent of surface active agent, 15 to 20 percent of antirust additive, 2 to 5 percent of coupling agent and the balance of distilled water. The settlement additive is a mixture of fatty amine polyoxyethylene ether, aziridine and dibenzyl ether. The water solubility high-speed grinding fluid has excellent rust resistance, wettability, lubricity and grinding ash settling performance. Meanwhile, the invention provides a preparation method of the water solubility high-speed grinding fluid for machining the settlement bearing.

The present invention relates to a method for preparing macromolecular species with a modified surface, comprising a step (e) in which macromolecular species (M), initially carrying -OH and / or -SH functions, are brought into contact with: a catalyst (C) carrying at least one conjugated guanidine function; and reactive species (E), comprising reactive groups including: (i) at least one group including an alpha,beta-unsaturated carbonyl group C=C-C=O and / or an alpha, beta-unsaturated thiocarbonyl group C=C-C=S; and / or (ii) at least one heterocyclic group comprising from 3 to 5 ring members, the group being selected from cyclic ethers, cyclic thioethers and aziridine rings; and / or (iii) at least one group selected from isocyanate -N=C=O or thioisocyanate -N=C=S groups, and trivalent groups of formula >C=CZ-, where Z is an electron-withdrawing group. The invention also relates to the macromolecular species with a modified surface that are obtained in this context.

A light-sensitive silver halide photographic film material has been provided, said film material comprising a transparent support and on both sides thereof at least one light-sensitive emulsion layer having spectrally and chemically sensitized tabular silver halide grains rich in silver bromide, further having silver iodide in an amount of less than 3 mole % based on silver, with two flat parallel {111} crystal faces, said grains accounting for a total projective surface of said parallel crystal faces in said emulsion of at least 50%, further having an average aspect ratio of at least 2:1, a grain thickness of from 0.05 up to 0.15 mum, a site-directing azacyanine compound satisfying the general formulae disclosed herein in an amount of not less than 1x10-4 mole per mole of silver halide coated and one or more J-aggregating spectrally sensitizing dye(s), wherein a molar ratio amount between said site directing compound and said J-aggregating spectrally sensitizing dye(s) is at least 1:6 for a grain coverage of said {111} tabular grains exceeding 50%.A radiographic screen / film combination has also been described comprising said light-sensitive silver halide photographic film material and two supporting or self-supporting X-ray intensifying screens) comprising luminescent phosphors, wherein by contacting the film material with a sandwich of a pair of said intensifying screens and exposing said combination to X-rays, emission of radiation by said luminescent phosphors in the wavelength range for which said material has been made spectrally sensitive provides a black-and-white diagnostic image after processing of said exposed radiographic film material.

In order to impart excellent solvent resistance and conduction reliability to the insulating coated conductive particles suitable for anisotropic conductive adhesive conductive particles, the surface of the conductive particles is coated with a carboxyl group using a polyfunctional aziridine compound. The insulating resin layer of the insulating-coated electrically-conductive particle covered with the insulating resin layer formed of insulating resin is surface-treated. As the aziridine compound, for example, trimethylolpropane-tri-β-aziridine propionate, tetramethylolmethane-tri-β-aziridine propionate, or N,N-hexamethylene-1,6-bis-1-aziridine carboxamide, etc. The insulating resin layer is preferably composed of an insulating resin having an acrylic monomer unit or a methacrylic monomer unit. Specifically, an acrylic-styrene copolymer is preferable.

The invention discloses a method for synthetizing DL-cysteine, comprising the following steps: obtaining 2-bromine-azacyclopropane through the reaction of azacyclopropane and bromine water, obtaining 2-cyano-azacyclopropane through the reaction of the 2-bromine-azacyclopropane and cyanide, obtaining 2-sulfydryl-3-aminopropyl cyanide through a ring-opening reaction of 2-cyano-azacyclopropane and sodium sulfide and obtaining the DL-cysteine through the acid hydrolysis of the 2-sulfydryl-3-aminopropyl cyanide. The method disclosed by the invention has the advantages of mild reaction condition, high reaction yield, adequate raw material source, low production cost and simple production process.

Disclosed is a heat-sensitive recording material comprising a supporting body and a heat-sensitive recording layer formed on the supporting body and containing a dye precursor-containing composite particle and a developer. This heat-sensitive recording material is characterized in that the dye precursor-containing composite particle is obtained by dissolving a solute containing a dye precursor into a solvent containing a polyvalent isocyanate compound-containing polymerization component, then emulsifying and dispersing the thus-obtained solution into an aqueous medium, and then performing a polymerization reaction of the polyvalent isocyanate compound-containing polymerization component in the presence of a polyethylene imine having a molecular weight of 200-1,500. Also disclosed is a method for producing such a heat-sensitive recording material.

The invention discloses a preparation method for chiral pentabasic bicyclic guanidine based on aziridine. The method comprises the following steps: (1) using amino acid to synthesize alkamine; (2) using the alkamine to synthesize the aziridine; (3) using the aziridine to synthesize-NHTs triamine; (4) removing protection to obtain triamine; and (5) cyclizing to obtain the pentabasic bicyclic guanidine. The method overcomes the defects of high cost of the purifying technique, complexity in operation, -78 DEG C of low temperature reaction, high danger coefficient, expensive prices of raw materials, high cost and difficulty in industrial production in the original technique; and the method has the advantages of simplicity, feasibility, excellent reaction temperature, cheap raw materials, simple operation, reduced cost and improved feasibility of industrial production.

This invention relates to aziridine derivatives, i.e., (1Z, 4Z,5Z)-6-N-n-hexadecyl / octadecyl-6-aza-2-oxo-3-oxa-4-methoxy-bicyclo[3.1.0]hexane, as shown in chemical formulae I and II. This invention also provides a method for preparing the aziridine derivatives. The preparation method comprises: synthesizing 5-methoxy-3-bromo-2(5H)-furanone, reacting with hexadecylamine / octadecylamine, and Et3N in DMSO to obtain the aziridine derivatives. The aziridine derivatives have good inhibitive effects on colon cancer cells, human gastric cancer cells and human ovarian cancer cells, and can be used in drugs for treating colon cance, gastric cancer and ovarian cancer. The preparation method avoids traditional phase transfer catalysis and water / oxygen-free operation, and adopts room temperature homogeneous catalytic condition, thus has such advantages as simple operation, low cost and high target compound yield. Besides, another diasteromer can be obtained.