Abstract: A method produces a 3,4-dihydro-1,2,3-oxathiazin-4-one-2,2-dioxide compound of following formula (2): wherein R1 and R2 are the same as or different from each other and are each hydrogen atom or an organic group inert to the reaction; and R3 is hydrogen atom or an organic group inert to the reaction, or a salt thereof, by subjecting a beta-ketoamide-N-sulfonic acid of following Formula (1): wherein R1, R2 and R3 are as defined above; and X is hydrogen atom, or a salt thereof, to cyclization in the presence of an acid anhydride with or without further subjecting the cyclized product to hydrolysis, in which the cyclization is continuously carried out using a continuous flow reactor.
Abstract: Derivatives of C2-substituted indan-1-ol compounds of formula I: its physiologically acceptable salts, and its physiologically functional derivatives for the prophylaxis or treatment of obesity are disclosed herein. Compositions comprising the same, methods for preparing the instant compounds, and methods for reducing weight in mammals and for the prophylaxis or treatment of obesity are also described.
Type:
Grant
Filed:
October 27, 2003
Date of Patent:
July 19, 2005
Assignee:
Aventis Pharma Deutschland GmbH.
Inventors:
Gerhard Jaehne, Volker Krone, Martin Bickel, Matthias Gossel
Abstract: Derivatives of C2-substituted indan-1-ol compounds, processes for their preparation and their use are disclosed. In particular, the invention relates to compounds of the formula I
and to their physiologically acceptable salts and physiologically functional derivatives. The compounds are suitable, for example, for use as anorectics.
Type:
Grant
Filed:
August 30, 2002
Date of Patent:
April 6, 2004
Assignee:
Aventis Pharma Deutschland GmbH
Inventors:
Gerhard Jaehne, Volker Krone, Martin Bickel, Matthias Gossel
Abstract: 2-aryl-ethane-sulphonic acids of the formulaAr.sup.1 --CH.sub.2 --CH.sub.2 --SO.sub.3 H (I),in whichAr.sup.1 denotes a carbocyclic or heterocyclic aromatic radical which can be bound to an anellated benzene nucleus,can be obtained by reaction of the underlying vinyl aromatic compound with sulphurous acid, if the reaction is carried out in the presence of an amine of the formulaN(R.sup.1,R.sup.2,R.sup.3 (III),in whichR.sup.1, R.sup.2 and R.sup.3 have the meaning mentioned in the description.
Type:
Grant
Filed:
September 8, 1994
Date of Patent:
April 30, 1996
Assignee:
Bayer Aktiengesellschaft
Inventors:
Jurgen-Dietrich Meier, Christian Munster, Volker Kass, Horst Siffrin
Abstract: Precursors and methods for the synthesis of mono- and difunctionalized acetylenes are described. The invention includes novel tricoordinate iodonium transfer reagents and novel alkynyldi(phenyliodonium) salts, both of which are precursors for the functionalized acetylenes. The iodonium transfer reagents take the general form of mixed iodonium sulfonates PhI.sup.+ (X)OSO.sub.2 R.sub.f, where X may be OAc, NHAc, NCO, or CN. These mixed iodonium sulfonates are produced by reaction of iodosobenzene with certain substituted trimethylsilanes.To make the alkynyldi(phenyliodonium) salt PhI.sup.+ C.tbd.CI.sup.+ Ph.cndot.2 R.sub.f SO.sub.3.sup.-,a mixed iodonium sulfonate is reacted with a bistin acetylene of the kind R'.sub.3 SnC.tbd.CSnR".sub.3. Alternatively, the reaction may be performed with disubstituted tin diacetylenes to produce PhI.sup.+ C.tbd.C-C.tbd.CI.sup.+ Ph.cndot.2 R.sub.f SO.sub.3.sup.- to produce a dialkynyldi(phenyliodonium) salt.
Type:
Grant
Filed:
July 19, 1991
Date of Patent:
February 15, 1994
Assignee:
University of Utah Research Foundation
Inventors:
Peter J. Stang, Charles M. Crittell, Bobby L. Williamson, Viktor Zhdankin
Abstract: A process for reducing the residual content of free alkylating agent in aqueous solutions of amphoteric or zwitterionic surface-active agents by aftertreatment with ammonia, an amino acid containing 2 to 8 carbon atoms, or an oligopeptide.
Abstract: The preparation is described of compounds of the structure ##STR1## in which the substituents have the meanings indicated in the description. The compounds, which are in part new, are used as intermediate products for dyestuffs.
Abstract: 6-Methyl-3,4-dihydro-1,2,3-oxathiazin-4-one 2,2-dioxide is prepared bya) reacting, an inert organic solvent, a salt of sulfamic acid, which is at least partially soluble therein, with at least approximately the equimolar amount of an acetoacetylating agent, in the presence of an amine or phosphine catalyst, and by cyclizing the acetoacetamide-N-sulfonate which is formed in this reaction, or the free sulfonic acid,b) by the action of at least approximately the equimolar amount of SO.sub.3, where appropriate in an inert inorganic or organic solvent, to give 6-methyl-3,4-dihydro-1,2,3-oxathiazin-4-one 2,2-dioxide, which is produced in the form of the acid in this reaction;it is possible, if desired, to obtain from the acid formc) the appropriate salts by neutralization with bases.The non-toxic salts-- in particular the potassium salt-- are valuable synthetic sweeteners.
Type:
Grant
Filed:
January 29, 1991
Date of Patent:
April 7, 1992
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Karl Clauss, Adolf Linkies, Dieter Reuschling
Abstract: The preparation is described of compounds of the structure ##STR1## in which the substituents have the meanings indicated in the descripion. The compounds, which are in part new, are used as intermediate products for dyestuffs.
Abstract: 6-Methyl-3,4-dihydro-1,2,3-oxathiazin-4-one 2,2-dioxide is prepared bya) reacting, in an inert organic solvent, a salt of sulfamic acid, which is at least partially soluble therein, with at least approximately the equimolar amount of an acetoacetylating agent, in the presence of an amine or phosphine catalyst, and by cyclizing the acetoacetamide-N-sulfonate which is formed in this reaction, or the free sulfonic acid,b) by the action of at least approximately the equimolar amount of SO.sub.3, where appropriate in an inert inorganic or organic solvent, to give 6-methyl-3,4-dihydro-1,2,3-oxathiazin-4-one 2,2-dioxide, which is produced in the form of the acid in this reaction;it is possible, if desired, to obtain from the acid formc) the appropriate salts by neutralization with bases. The non-toxic salts--in particular the potassium salt--are valuable synthetic sweeteners.
Type:
Grant
Filed:
April 16, 1990
Date of Patent:
April 30, 1991
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Karl Clauss, Adolf Linkies, Dieter Reuschling