Abstract:
NEW MATERIAL:An allantoin derivative shown by the formula I (R is lower alkyl, cycloalkyl, or aryl; this lower alkyl group may be replaced with hydroxyl group or alkoxycarbonyl group). EXAMPLE:8-(1'Hydroxymethylpropyl)allantoin. USE:Showing antipeptic ulcer action, suppressing action on gastriointestinal disorder, protecting action on the skin, remedying action on skin disease or trauma, useful as an antipeptic ulcer, remedy for wound, etc. Also useful as an intermediate for synthesizing drugs. Being administered orally and parenterally. PREPARATION:A compound shown by the formula II is condensed with an amine shown by the formula R-NH2, to give a compound shown by the formula I . The condensation is preferably carried out by using a condensation agent such as N,N'-dicyclohexylcarbodiimide or its derivative, or N-ethoxycarbonyl-2- ethoxy-1,2-dihydroquinoline, etc.
Abstract:
PROBLEM TO BE SOLVED: To provide a method for producing type-A crystal of 3-pyridyl-1-hydroxy-1,1-bisphosphonic acid sodium salt 2.5 hydrate. SOLUTION: The production method comprises (1) a step to dissolve 1-2 equivalent of an alkali metal hydroxide to a 8:2 mixture of water and an organic solvent and add the obtained liquid to a mixture of an aqueous suspension of 3-pyridyl-1,1-bisphosphonic acid and an organic solvent at a volume ratio of 7:3 to 9:1, (2) a step to heat the mixture at 45-90°C for 1-3 hr and (3) a step to cool the mixture. COPYRIGHT: (C)2008,JPO&INPIT
Abstract:
NEW MATERIAL:Methylene-bis-(2,2-dibromo-2-nitroethyl)ether shown by formula I. USE:Showing strongly germicidal action on bacteria and fungi and useful as a germicide, antiseptic, mildewcide, etc. PREPARATION:A compound shown by formula II is reacted with formaldehyde or paraformaldehyde in the presence of an acidic catalyst to give a compound shown by formula I. The compound of formaldehyde used is preferably 0.3-0.7mol based on 1mol compound shown by formula II. The reaction temperature is 25-150 deg.C, preferably 60-90 deg.C. The starting compound shown by formula II is synthesized by condensing formaldehyde with nitromethane by a caustic alkali and treating the condensate with bromine.
Abstract:
PURPOSE:To provide the titled controlling agent containing a specific halogen- containing acetophenone compound as an active component, exhibiting excellent antibacterial activity and effective in controlling slime in process water in the paper-making industry. CONSTITUTION:The objective agent contains a compound of formula (X is F, Cl or Br; m and n are 1 or 2), e.g. alpha-bromo-2-bromoacetophenone, alpha,alpha- dibromo-4-fluoroacetophenone, etc., as an active component. The compound of formula can be easily produced e.g. by brominating methyl halogenophenyl ketone with Br2 in an inert solvent such as CCl4. The compound is used in the form of solution or suspension by dissolving in a solvent such as dimethylsulfoxide, xylene, etc., or suspended in water as fine particles. Sufficient effect can be attained by adding the controlling agent to the process water for paper-making at a concentration of 0.1-100ppm in terms of the active component.
Abstract:
NEW MATERIAL:A compound of formula (n is 1-3). EXAMPLE:Dihydroxyaluminum methioninate-S-methyl chloride. USE:Remedy for peptic ulcer. The compound is stable and can be easily prepared. PROCESS:The compound of formula can be prepared by reacting S-methylmethionine sulfonium chloride with a compound of formula Al(OR)3 (R is H or lower alkyl). The value of n in the formula can be adjusted to a desired value by selecting the molar ratio of the raw materials.
Abstract:
PROBLEM TO BE SOLVED: To provide an oxyquinolinecarboxylic acid anhydride usable as an antibacterial agent for medical use. SOLUTION: The oxyquinolinecarboxylic acid anhydride expressed by formula II is produced by dissolving oxyquinolinecarboxylic acid of formula I in an organic solvent and adding anhydrous hydrogen chloride to the solution. The organic solvent may be a solvent dissolving the compound of formula I or a mixture of the solvent dissolving the compound and a solvent scarcely dissolving the compound.
Abstract:
PURPOSE:The titled remedy, containing 5-methylallantoin as an active constituent, and having a remedial effect on the peptic ulcer with low toxicity. CONSTITUTION:A remedy for peptic ulcer containing 5-methylallantoin of formulaIas an active constituent. The active constituent of formulaIis synthesized by reacting a urea compd. of formula II with an alpha-ketocarboxylic acid of formula III in the presence of a dehydrating agent, preferably an acidic catalyst at room temperature or under a little warming. An inorganic acid, e.g. hydrochloric or sulfuric acid, is used as the acidic catalyst. The melting point, etc. of the 5-methylallantoin of formulaIare not described in literature, and the structure thereof is determined by elementary analyses and measurement of various spectra with the estimated 211 deg.C melting point. In use as the titled remedy, the dosage form for the oral administration is a tablet, capsule, powder, etc. may be cited, and the daily dose of the active constituent is suitably 100mg-1g for an adult.
Abstract:
PROBLEM TO BE SOLVED: To provide a method for producing ribavirin R-II type crystal which is assumed to be an effective ingredient in a ribavirin medicine. SOLUTION: The manufacturing method comprises dissolving ribavirin in an organic solvent and a small amount of water followed by refluxing and subsequent recrystallization. Concretely, the ribavirin R-II type crystal is produced by dissolving 1 pt.wt. of ribavirin in a mixed solvent of at least 20 pts.wt. of a 3C or higher alcohol solvent with at most 25 wt.%, based on the alcohol solvent, of water followed by refluxing under heating, and subsequently cooling the mixed solvent down to 10°C or lower followed by filtration. COPYRIGHT: (C)2008,JPO&INPIT