Abstract: A process for producing difluoromaleic anhydride by reacting sulfur trioxide with a fluorinated precursor selected from the group consisting of hexafluoro-2,5-dihydrofuran, hexafluoro-2,5-dihydrothiophene, difluoro-2,5-dihydrothiophene-2,5-dione and tetrafluoro-2,5-dihydrothiophene-2-one. Also disclosed are the compounds difluoro-2,5-dihydrothiophene-2,5-dione and tetrafluoro-2,5-dihydrothiophene-2-one. Difluoromaleic anhydride is useful for example as a component of fluoropolymers.
Abstract: The invention relates to pyridine-2,4- and -2,5-dicarboxylic acid derivatives of the formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4 and X have the meanings given, a process for the preparation of these compounds and their use, in particular in medicaments for influencing the metabolism of collagen and collagne-like substances or the biosynthesis of Cl.sub.q.
November 13, 1989
Date of Patent:
August 6, 1991
Martin Bickel, Dietrich Brocks, Harald Burghard, Volkmar Gunzler, Stephan Henke, Hartmut Hanauske-Abel, Jurgen Mohr, Georg Tschank
Abstract: The object of the invention is a process for the preparation of derivatives of 3-sulfonyl indolizine of general formula: ##STR1## in which: R is selected from hydrogen, alkyl, cycloalkyl, substituted or unsubstituted phenyl,R.sub.1 is a protecting group for hydroxyl,R.sub.2 and R.sub.3, identical or different, is each selected from hydrogen, methyl or ethyl or halogen.These compounds are intermediates which can be used for the preparation of 3-aminoalkoxyphenylsulfonyl-indolizines, which are useful in the treatment of certain diseases of the cardiovascular system.
Abstract: The invention concerns compounds of formula I ##STR1## or a salt thereof, wherein R.sup.1 and R.sup.2 each independently represent hydrogen, lower alkyl, lower alkoxy, carboxyloweralkyl, carboxy, hydroxyloweralkyl, halogen, haloloweralkyl, lower alkoxycarbonyl, optionally substituted aryl or optionally substituted aralkyl, n represents an integer from 3 to 6; R.sup.3 which is optionally present represents single or multiple substitution on one or more of the aliphatic carbons by one or more substituents selected from lower alkyl, optionally substituted aryl and optionally substituted aralkyl; A represents a group of formula (i) or (ii) below:--CR.sup.4 R.sup.5 --(CR.sup.6 R.sup.7).sub.m -- (i)--CX--(CR.sup.6 R.sup.7).sub.m -- (ii)in which R.sup.4, R.sup.6 and R.sup.7 each independently represent hydrogen or lower alkyl (providing that when R.sup.5 is NH.sub.2, R.sup.4 is hydrogen); m is 0 or 1; R.sup.5 represents hydrogen, NH.sub.2, OH or loweralkoxy, and X is .dbd.O, .dbd.NH or .dbd.
Abstract: Crude maleic anhydride produced by catalytic oxidation is distilled and then n-propyl gallate, cuprous chloride and zinc chloride are added thereto.Alternatively, crude maleic anhydride is distilled in the presence of tridecyl phosphite. Further, these procedures can be used in combination. Thermal stability and color stability of the maleic anhydride is improved.
Abstract: Compounds represented by the general formula: ##STR1## in which R.sub.1 and R.sub.2 are selected from hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.2 -C.sub.6 alkenyl , phenyl or benzyl or R.sub.1 and R.sub.2 form together with the nitrogen atom to which they are attached a C.sub.4 -C.sub.8 saturated heterocycle, R.sub.3 is selected from hydrogen, C.sub.1 -C.sub.6 alkyl, phenyl or C.sub.7 -C.sub.9 phenyl-alkyl, R.sub.4 is selected from hydrogen or C.sub.1 -C.sub.4 alkyl, R.sub.5 and R.sub.6 are selected from hydrogen or halogen, C.sub.1 -C.sub.3 or alkoxy, nitro or trifluoromethyl; Z is selected from OH, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.4 alkyl, benzyl, C.sub.4 -C.sub.6 aryl with or without a heteroatom, or NR.sub.8 R.sub.9, R.sub.8 and R.sub.9 being selected from hydrogen, C.sub.1 -C.sub.4 alkyl, phenyl or benzyl; R.sub.10 is selected from hydrogen, C.sub.1 -C.sub.
June 6, 1989
Date of Patent:
June 25, 1991
Etienne Mendes, Jean-Claude Vernieres, Peter E. Keane, Andre Bachy
Abstract: Bicyclic heterocyclyl containing N-(bicyclic heterocyclyl)-4-piperidinamines having antihistaminic and serontonin-antagonistic properties which compounds are useful agents in the treatment of allergic diseases.
December 7, 1989
Date of Patent:
June 18, 1991
Janssen Pharmaceutica N.V.
Frans E. Janssens, Joseph L. G. Torremans, Jozef F. Hens, Theophilus T. J. Van Offenwert
Abstract: Novel compounds represented by the formula: ##STR1## wherein R represents hydrogen, optionally substituted alkyl radicals having from 1 to about 10 carbon atoms, optionally substituted alkenyl radicals having from 1 to about 10 carbon atoms, optionally substituted aryl, alkaryl and aralkyl radicals having from about 6 to about 16 carbon atoms and optionally substituted acyl and acyloxy radicals having from about 1 to about 10 carbon atoms, manifest glycosidase inhibition activity.
Abstract: The oxidation of butane to maleic anhydride in a recirculating solids reactor using a stoichiometric excess of oxygen, a vanadium-phosphorus oxide catalyst in oxidized form, and separate regeneration of the resultant reduced catalyst is disclosed.
Abstract: There are provided novel 2-(2-imidazolin-2-yl)pyridine and quinoline compounds, a process and intermediate compounds for the preparation thereof, and a method for controlling a wide variety of annual asnd perennial plant species therewith.
Abstract: Alkenyl succinic anhydrides having a decreased amount of tar and color bodies are made by the reaction of an olefin with maleic anhydride in the presence of a tri-orthoalkylphenyl phosphite and optionally a hindered phenolic antioxidant such as 2,4,6-tri-(3,5-di-tert-butyl-4-hydroxybenzyl) mesitylene.
Abstract: A compound of the formula ##STR1## wherein R.sup.1 is hydrogen or a protecting group; R.sup.2 is C.sub.1 -C.sub.3 alkyl or C.sub.3 -C.sub.7 cycloalkyl; R.sup.3 is hydrogen, hydroxy, or amino; R.sup.4 is halogen; R.sup.5 and R.sup.6 each is identically or differently hydrogen or C.sub.1 -C.sub.3 alkyl; W is C.sub.1 -C.sub.3 alkylidene; X is N or C-Y; Y is hydrogen or halogen; or a pharmaceutically acceptable salt thereof, having a more potent antibacterial activity against G(+) and G(-) bacteria than known analogues, useful as antibacterial agents.
Abstract: Compounds having the formula ##STR1## and their pharmaceutically acceptable acid addition salts, wherein --X-- is --O--, --CH.sub.2 -- or --; .dbd.Y is .dbd.O or a derivatized keto group which is hydrolyzable or enzymatically convertible to a keto group; R is alkyl having from 1 to 12 carbon atoms or aralkyl having from 7 to 20 carbon atoms; and Ar is the 3-aromatic or heterocyclic residue of a 1-alkylamino-2-propanol having an aromatic or heterocyclic substituent at the 3-position and having .beta.-adrenergic blocking properties; are useful as .beta.-adrenergic blocking agents and are of particular interest in the treatment of glaucoma or for lowering intraocular pressure.
Abstract: Racemic Compounds of the formula ##STR1## A is --C.tbd.C--R.sub.6, --CH.sub.2 --CH.sub.2 --R.sub.7 or ##STR2## R.sub.1 is hydrogen or lower alkanoyl, R.sub.2, R.sub.3, and R.sub.4 independently are hydrogen or lower alkyl,R.sub.5 is lower alkyl,R.sub.6 is a heteroaromatic radical or an aromatic radical selected from phenyl, naphthyl or phenanthryl, which aromatic radical may optionally be substituted by one or more substituents selected from chlorine, fluorine, lower alkyl, lower alkoxy, phenyl lower alkoxy, lower alkanoyl, lower alkanoyloxy, hydroxy-lower alkyl, carboxy, lower alkoxycarbonyl, hydroxyimino lower alkyl, amino, amino lower alkyl, mono- or di-lower alkylamino, mono- or di-lower alkylamino-lower alkyl, lower alkanoylamino, aminocarbonyl, lower alkylaminocarbonyl, lower dialkylaminocarbonyl, trifluoroacetylamino, trifluoromethyl, hydroxy, pyridyl, or on adjacent carbons can be ##STR3## wherein R' is hydrogen, lower alkanoyl, trifluoroacetyl and R" hydrogen or lower alkyl,R.sub.
Abstract: A continuous process for production of maleic anhydride is disclosed wherein maleic anhydride is produced in high yield and catalyst productivity is in the range of from about 0.12 to about 0.18 pounds of maleic anyhdride produced per pound of catalyst per hour. The catalyst comprises vanadium-phosphorus-oxygen and a modifier, preferably molybdenum. The increased catalyst productivity substantially increases production rates without necessity for extensive equipment modification.