Abstract: Provided is a method for producing an imide ether compound in high yield. The method is characterized in that a nitrile compound, an alcohol, and a hydrogen halide are continuously introduced into a flow reaction device comprising a mixer and a flow reactor, to be subjected to a reaction. Because a reaction proceeds in a ratio of 1:1 by a flow reactor, selectivity is improved and generation of by-products is decreased, and thus an imide ether compound can be efficiently produced.

Abstract: O-isopropyl-isourea hydrogen sulfate or sulfate represented by the formula (I): wherein X represents HSO4 or ½ SO4 and the production method thereof, wherein O-isopropyl-isourea hydrogen sulfate is obtained by reacting cyanamide and isopropyl alcohol in the presence of sulfuric acid and is neutralized with an alkali metal hydroxide to produce O-isopropyl-isourea sulfate.

Abstract: Hydroxyamidines and related compounds are provided which are suitable as antibacterial agents.

Abstract: Benzene-sulphonamide derivatives complying with the general formula (I): in which the different symbols have different meanings, their optical isomers and the salts pharmacologically acceptable of these derivatives, as well as their uses for drug manufacture and as radiolabelled pharmacological tools of the thromboxan A2 receptors.

Abstract: The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described. Preferred (R)-Chiral 1-Subsbitutedamino-(n+1)-Alkanol compounds are substituted (R)-Chiral N-phenoxy N-phenyl aminoalcohols.

Abstract: The use of an N-substituted urea derivative for the manufacture of a medicament for the treatment of a condition where there is an advantage in inhibiting the NO synthase enzyme, in particular cerbral ischemia, and pharmaceutical formulations therefor are disclosed. Novel N-substituted urea derivatives and processes for the preparation thereof are also described.

Abstract: A process for the preparation of an O-alkylisourea of the formula I, where R1 is C1- to C20-alkyl, in the form of an acid addition salt, in which urea and an alkyl-transferring reagent, if required dissolved or suspended in a diluent, are reacted at 40-200° C. in a continuously operated reactor, is described. The diluent is preferably a recycled part-stream of the O-alkylisourea acid addition salt obtained.

Abstract: A novel nitroisourea derivative and a process for producing the same, which is an important intermediate for the production of a nitroguanidine derivative having an insecticidal activity, and a process for producing a nitroguanidine derivative having an insecticidal activity using the nitroisourea derivative. The process for producing a nitroguanidine derivative represented by formula (1), effective as an insecticide is shown by reaction scheme (2): ##STR1## wherein R.sub.1 represents an alkyl group having from 1 to 4 carbon atoms or a benzyl group; R.sub.2 represents an alkyl group having from 1 to 4 carbon atoms; R.sub.3, R.sub.4, R.sub.5 and R.sub.6 each independently represents a hydrogen atom or an alkyl group having from 1 to 4 carbon atoms; and Q represents a 5-membered or 6-membered heterocyclic ring having at least one of the following: a nitrogen atom, an oxygen atom or a sulfur atom, one of the hydrogen atoms being substitutable with a halogen atom.

Abstract: A process for producing the compound [I] or a salt thereof having excellent pesticidal activity as shown in the following schema.

Abstract: Alkoxytriazolinones of the formula (I), ##STR1## are obtained in good yields and in high purity by reacting iminocarbonic diesters (II) with carbazinic esters (III) ##STR2## at -20.degree. C. to +120.degree. C. (1st step) and subjecting the semicarbazide derivatives (IV) formed in this process with elimination of R.sup.2 --OH ##STR3## to a cyclizing condensation reaction in the presence of a base at 20.degree. C. to 150.degree. C. with elimination of R.sup.3 --OH, if appropriate (2nd step) and, finally, by reacting the resulting 5-alkoxytriazolinones of the formula (V) ?=formula (I) where R.sup.1 =H! with an alkylating agent of the formula R.sup.1 --X (VI) at 0.degree. C. to 150.degree. C., if appropriate in the presence of a base.

Abstract: Disclosed is a process for the preparation of crystalline O-isopropylisourea hydrochloride, wherein cyanamide, chloroformamidinium chloride and isopropanol are reacted, an aprotic solvent preferably selected from the group consisting of ketones, ethers, esters and acetals, is added to the reaction mixture before, during and/or after the reaction and, optionally after cooling the reaction solution, the crystalline reaction product is separated off. O-isopropylisourea hydrochloride is obtained in a very pure and coarse crystalline form by the process of the invention.

Abstract: Alkoxytriazolinones of the general formula (I), ##STR1## in which R.sup.1 represents hydrogen, or represents in each case optionally substituted alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkylalkyl, aryl or arylalkyl, andR.sup.2 represents in each case optionally substituted alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkylalkyl, ary or arylalkyl,(which can be used as intermediates for the preparation of herbicidal active compounds) are obtained in very good yields and in high purity by reacting imino(thio)carbonic esters (II) with alkoxyethyl carbazinates (III) ##STR2## in which Q represents O or S, R.sup.3 represents (for example) alkyl, aryl or aralkyl and R.sup.4 represents (for example) alkyl,at -20.degree. C. to +150.degree. C. (1st step) and subjecting the new semicarbazide derivatives (IV) ##STR3## which are formed with elimination of R.sup.3 --QH, if appropriate after intermediate isolation, to a cyclizing condensation reaction at 0.degree. C. to 200.degree. C.

Abstract: N-carbamoyl-2-carboxyaryl-heterocyclic and hydrazinecarboximidamidehydrazone derivatives, intermediates and processes for their preparation, agricultural compositions containing them and their use as agricultural chemicals, in particular herbicides.

Abstract: R.sup.2 represents an optionally substituted alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkenyl, aralkyl or aryl radical, andR.sup.3 represents an optionally substituted alkyl, aralkyl, aryl or heteroaryl radical,and salts thereof, with the exception of the compounds:2-(2-methoxycarbonyl-phenylsulphonylaminocarbonyl)-4-methyl-5-methoxy-2,4-d ihydro-3H-1,2,4-triazol-3-one,2-(2-trifluoromethoxy-phenylsulphonylaminocarbonyl)-4-cyclopropnl-5-methoxy -2,4-dihydro-3H-1,2,4-triazol-3-one,2-(2-difluoromethoxy-phenylsulphonylaminocarbonyl)-cyclobutyl-5-ethoxy-2,4- dihydro-3H-1,2,4-triazol-3-one, and2-(2-methoxycarbonyl-phenylsulphonylaminocarbonyl)-4-ethyl-5-ethoxy-2,4-dih ydro-3H-1,2,4-triazol-3-one.

Abstract: The present invention relates to a novel class of phenylboronic acid complexing reagents useful for the preparation of bioconjugates, and the method of making and using such reagents. In the present invention, in the place of prior art Avidin-Biotin and Digoxigenin-anti-Digoxigenin systems, phenylboronic acid complexing reagents are utilized in conjunction with phenylboronic acid reagents (many of which are known in the prior art) to facilitate chemical conjugation without the use of intermediary biological macromolecules. Reagents suitable for the modification of a bioactive species for the purpose of incorporating a phenylboronic acid complexing moiety for subsequent conjugation to a different bioactive species having pendant phenylboronic acid moleties are of General Formula I or General Formula II. ##STR1## wherein group X is selected from either H, OH, NH.sub.2, NHCH.sub.3, NHOH and NHOCH.sub.

Abstract: Energetic compounds of the formula ##STR1## wherein R.sub.1 is --OCH.sub.2 CH.sub.2 C(NO.sub.2).sub.3, --OCH.sub.2 C.sub.2).sub.2 CH.sub.3, --OCH.sub.2 C(NO.sub.2).sub.3, --OCH.sub.2 CF(NO.sub.2).sub.2, --OCH.sub.2 CF.sub.2 (NO.sub.2), or --OCH.sub.2 CF.sub.3, and wherein R.sub.2 is --OCH.sub.2 CH.sub.2 C(NO.sub.2).sub.3, --OCH.sub.2 CF(NO.sub.2).sub.2, --OCH.sub.2 CF.sub.2 (NO.sub.2), --OCH.sub.2 CF.sub.3, --NH.sub.2, --NHCH.sub.2 CH.sub.2 ONO.sub.2, or --N(NO.sub.2)CH.sub.2 CH.sub.2 ONO.sub.2.

Abstract: The present invention provides novel fluorescein derivative compounds having fluorescence spectrum and quantum yield characteristics similar to those of fluorescein. The compounds are readily synthesized and purified and are readily soluble in water at self-quenching concentrations. Significantly, due to the presence of polar polyhydroxy group substituents and the absence of metal-chelating groups, these fluorescein derivatives are susceptible to minimal leakage across liposome membranes and have fluorescence characteristics minimally sensitive to the presence of metal ions. Compounds of the invention are thus exceptionally suitable for use in the development of highly storage stable liposome preparations to be employed in immunolytic assays involving human body fluid samples.

Abstract: The present invention provides novel fluorescein derivative compounds having fluorescence spectrum and quantum yield characteristics similar to those of fluorescein. The compounds are readily synthesized and purified and are readily soluble in water at self-quenching concentrations. Significantly, due to the presence of polar polyhydroxy group substituents and the absence of metal-chelating groups, these fluorescein derivatives are susceptible to minimal leakage across liposome membranes and have fluorescence characteristics minimally sensitive to the presence of metal ions. Compounds of the invention are thus exceptionally suitable for use in the development of highly storage stable liposome preparations to be employed in immunolytic assays involving human body fluid samples.

Abstract: The invention relates relates to new sulphonyliso(thio)-urea derivatives of the general formula (I) ##STR1## in which R.sup.1 represent an optionally substituted radical from the series comprising alkyl, aralkyl, aryl and heteroarylR.sup.2 represents an optionally substituted and/or optionally fused 6-membered aromatic heterocyclic radial containing at least one nitrogen atom,R.sup.3 represents an optically substituted aromatic or heteroaromatic radical,X represents oxygen or sulphur andM represents hydrogen or an equivalent of a metal, and adducts of compounds of the formula (I) with strong acids, processes for their prepartion, and their use as herbicides.

Abstract: The invention relates to a process for the preparation of compounds of the formula I and salts or acid addition compounds thereof ##STR1## in which R denotes hydrogen, (halogenated) alkyl with the exception of CF.sub.3, a (substituted) aromatic radical, (substituted) heteroaryl, (substituted) phenoxy, (substituted) phenylthio, (substituted) phenylamino, halogen, hydroxyl, alkoxy, mercapto, (halogenated) cycloalkyl, alkylmercapto, amino, monoalkylamino or dialkylamino,R.sup.1 denotes (substituted alkyl, (substituted) phenyl or naphthyl, alkenyl, alkinyl, cycloalkyl, (substituted) benzyl or heteroaryl, and X denotes oxygen or sulfur, which comprises reacting a nitrile of the formula II with a compound of the formula IIIR--C.tbd.N (II)R.sup.

Abstract: Isoureas of the formula ##STR1## where X, Y and Z are each hydrogen, halogen, alkyl, alkoxy, haloalkyl, unsubstituted or substituted phenoxy or unsubstituted or substituted arylalkoxy, R.sup.1 is alkyl, R.sup.2 is alkyl or methoxy and R.sup.3 is benzyl or is phenyl which can be monosubstituted or polysubstituted by alkyl, halogen, alkoxy, haloalkoxy, hydroxyl, nitro, alkoxycarbonylmethoxy, alkoxycarbonylethoxy or a radical--NH--R.sup.4, processes for their preparation, and their use for controlling undesirable plant growth.

Abstract: Disclosed herein are tolrestat amides and methods of preparation. The amides are new aldose reductase inhibitors useful for the treatment or prevention of diabetic complications.

Abstract: Disclosed herein are tolrestat and oxotolrestat amides and methods of preparation. The amides are new aldose reductase inhibitors useful for the treatment or prevention of diabetic complications.

Abstract: A process for the preparation of a sulphonyliso(thio)urea of the formula ##STR1## in which R.sup.1 represents an optionally substituted radical from the group consisting of alkyl, aralkyl, aryl and heteroaryl,R.sup.2 represents an optionally substituted and/or optionally fused, six-membered aromatic heterocycle containing at least one nitrogen atom,R.sup.3 represents an optionally substituted radical from the group consisting of alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkyl-alkyl and aralkyl, andQ represents oxygen or sulphur,comprising reacting a sulphonylguanidine of the formula ##STR2## in which R.sup.4 represents an optionally substituted hydrocarbon radical,with a compound of the formulaH--Q--R.sup.3at a temperature between 0.degree. C. and 150.degree. C. The products are known herbicides.

Abstract: The invention relates to a new multistage process for the production of 4-amino-6,7-dimethoxy-2-[4-(furo-2-yl)-piperazin-1-yl]-quinazoline corresponding to the following formula ##STR1## and physiologically compatible salts thereof, which gives better yields and uses less expensive and more reactive materials than known processes. The intermediate product formed in this process, N"-cyano-N'-(3,4-dimethoxyphenyl)-O-phenylisourea, shows antihypertensive activity on its own.