Abstract: Novel aminoethylphenoxyacetic acid derivatives represented by the general formula:
(wherein R1 represents a hydrogen atom, a lower alkyl group or an aralkyl group; R2 represents a hydrogen atom or a halogen atom; the carbon atom marked with (R) represents a carbon atom in (R) configuration; and the carbon atom marked with (S) represents a carbon atom in (S) configuration) and pharmaceutically acceptable salts thereof, which have stimulating effects on both &bgr;2- and &bgr;3-adrenoceptors and are useful as agents for relieving pain and promoting the removal of calculi in urolithiasis.
Abstract: Aliphatic esters, R'COOR are produced by reacting the corresponding alcohol, ROH having carbon numbers of the alkyl groups, R′ and R, between 0 and 9 and 1 and 10, respectively, with molecular oxygen in the presence of a dual functional catalyst comprising metal on acidic solid support. In particular, the process is used advantageously for production of ethyl acetate by conversion of ethanol. The reaction mixture from the reactor is separated through azeotropic distillation to recover the ethyl acetate as product and the by-product, acetaldehyde and acetic acid which could be recycled for further reaction. The process is characterized by high conversion of ethanol, high selectivity and high yield for ethyl acetate and low waste stream generation. The preferred catalyst is Pd on zeolites which is active, selective, stable and regenerable.
Abstract: Process for the preparation of amino acid derivatives of the general formula I
where R1-R4 are as defined herein,
from the corresponding malonic acid monoester amides of the general formula II
by Hofmann degradation using a hypohalite in an aqueously basic medium, which comprises carrying out the reaction in the presence of an alcohol or amine and using the hypohalite in amounts of from 1.0 to 1.5 equivalents and the base in amounts of from 0.8 to 4.0 equivalents per mole of starting material II.
Abstract: The invention concerns a method for preparing phosgene from diphosgene and/or triphosgene, by reaction on a catalyst comprising one or several compounds with one or several nitrogen atoms with a pair of deactivated electrons. The invention further concerns a device for preparing phosgene from diphosgene and/or triphosgene, for implementing said method.
Type:
Grant
Filed:
March 14, 2000
Date of Patent:
June 4, 2002
Assignee:
Dr. Eckert GmbH
Inventors:
Heiner Eckert, Bernhard Gruber, Norbert Dirsch
Abstract: A method for preparing acetic acid and/or methyl acetate by simultaneous isomerization and carbonylation reactions. A reaction mixture is provided containing at least one reagent which provides formyl radicals and at least one further reagent which provides methyl radicals, together with water in an amount of at most 5% by weight, carbon monoxide at a partial pressure between 0.1·105 Pa and 25·105 Pa, a solvent and a catalytic system which contains at least one halogenated promoter and at least one iridium-based compound. In a typical reaction mixture, methyl formate is isomerized to form acetic acid according to the reaction:
HCOOCH3CH3COOH
while methanol undergoes carbonylation to form acetic acid according to the reaction:
CH3OH+COCH3COOH
The reagent which provides the formyl radicals is kept at or below 20% by weight of the reaction mixture, while the molar ratio of methyl radicals to formyl radicals in the mixture is greater than 1.
Type:
Grant
Filed:
September 23, 1998
Date of Patent:
May 28, 2002
Assignee:
Acetex Chimie
Inventors:
Carl Patois, Robert Perron, Daniel Thiebaut
Abstract: The present invention provides a method of converting a hydroxy group in alcohols containing an electron withdrawing group into perfluoroalkane sulfonate and fluorosulfonate esters, which are good leaving groups, with inversion of configuration where the hydroxyl-bearing carbon is chiral. The method consists of converting an alcohol to an O—N,N-dialkylsulfamate ester and reacting it with a perfluoroalkansulfonic or fluorosulfonic acid. The method has applications in the synthesis of pharmaceutical and agrochemical compounds.
Type:
Grant
Filed:
October 27, 2000
Date of Patent:
May 28, 2002
Inventors:
Hans Jacob Edgar Loewenthal, Ron Benjamin Loewenthal
Abstract: This invention is directed to a method for treating a host infected with hepatitis B comprising administering an effective amount of an anti-HBV biologically active 2′-deoxy-&bgr;-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof, wherein the 2′-deoxy-&bgr;-L-erythro-pentofuranonucleoside has the formula:
wherein R is selected from the group consisting of H, straight chained, branched or cyclic alkyl, CO-alkyl, CO-aryl, CO-alkoxyalkyl, CO-aryloxyalkyl, CO-substituted aryl, alkylsulfonyl, arylsulfonyl, aralkylsulfonyl, amino acid residue, mono, di, or triphosphate, or a phosphate derivative; and BASE is a purine or pyrimidine base which may be optionally substituted.
Type:
Grant
Filed:
August 10, 1999
Date of Patent:
May 28, 2002
Assignees:
Novirio Pharmaceuticals Limited, Centre National da la Recherche Scientifique
Inventors:
Gilles Gosselin, Jean-Louis Imbach, Martin L. Bryant
Abstract: In a process for the catalytic gas-phase oxidation of propene to acrolein, the reaction gas starting mixture is passed with a propene loading of ≧160 l(S.T.P.)/l·h over a fixed-bed catalyst which is housed in two spatially successive reaction zones A,B, the reaction zone B being kept at a higher temperature than the reaction zone A.
Type:
Grant
Filed:
September 10, 2001
Date of Patent:
May 28, 2002
Assignee:
BASF Aktiengesellschaft
Inventors:
Heiko Arnold, Signe Unverricht, Ulrich Hammon, Hans-Peter Neumann, Klaus Harth, Andreas Tenten
Abstract: A process for preparing malonic acid from the hydrolysis of cyanoacetic acid in the presence of aqueous hydrochloric acid, the process conditions being such that they allow high yields in malonic acid product. The product of said acid hydrolysis is a mixture of malonic acid and ammonium chloride by-product; the mixture is concentrated, the ammonium chloride by-product is separated by dissolution with an oxygen solvent and isolated. Alternatively, said concentrated mixture is dissolved with a primary or secondary esterifying alcohol in C1-C10, the resulting mixture being esterified, while the ester product is purified by distillation under reduced pressure, the molar yields and purity of the ester product being high.
Type:
Grant
Filed:
January 14, 2000
Date of Patent:
May 28, 2002
Assignee:
Trikem S.A.
Inventors:
Otavio Vianna Carvalho, Ronaldo Mendonca Mansur, Sandro da Silva Aguiar, Jane Hitoni Fujiyama, Antonio Luiz Ribeiro de Castro
Abstract: The present invention relates to an improved process for producing an organic carboxylic acid having (n+1) carbon atoms by reacting an alcohol having n carbon atoms with carbon monoxide in the presence of a rhodium catalyst system. More particularly, the present invention relates to carbonylation of alcohol such as methanol catalyzed by a rhodium system to produce acetic acid. The characteristic of the present invention is the addition of a catalyst stabilizer in the reaction medium to avoid or to alleviate the precipitation of the catalyst in the liquid phase. The catalyst as used herein is a an inorganic salt of alkaline metal having the following formula (A):
XnMm (A)
X=Li+, Na+, K+;
M=CO3−2, HCO3−, PO4−3, HPO4−2, H2PO4−, SO4−2, HSO4−, C2O4−2, HC2O4−, B(C6Y5)4−1;
Y=H, F or CF3.
Type:
Grant
Filed:
January 12, 2000
Date of Patent:
May 28, 2002
Assignee:
China Petrochemical Development Corporation
Inventors:
Kuo-Chen Shih, Shu-Hei Wang, Tsu-Tseng Weng, Kou-Suein Ai
Abstract: Carnitine derivatives of formula (I) are described in racemic and/or optically active form, as well as the process for their preparation and their use as pharmaceutical anti-angina active ingredients for the treatment of ischaemic heart disease.
Also described is a process for producing the (R)-carnitine enantiomer from (S)-carnitine (or vice versa), using the derivatives of formula (I).
Abstract: A process for producing viscose wherein the caustic soda used previously in the alkalization of electron-untreated cellulose can be used in the alkalization of electron-treated cellulosic material, provided the level of dispersed solids in the caustic soda does not exceed 0.16 g/l.
Abstract: An improved process for the production of high quality unsaturated dimethylesters by reacting dicarboxylic anhydrides, typically maleic anhydride or phthalic anhydride, with methanol. The process is characterized by the fact that the esterification is performed in two steps, the step 1 consisting in a non catalytic reaction of formation of monomethylesters, and the step 2 consisting in the catalytic reaction of formation of dimethylesters from the monomethylester, the said catalytic reaction taking place in a reactor consisting of a multi-tray column where the liquid phase containing the mono and diester mixture flows downwards from each tray coming to contact with a progressively drier upflowing stream of vapors in countercurrent, which continuously removes the water formed in the reaction from the liquid phase. The process uses an alkylbenzene sulfonic acid with an alkyl radical containing from 10 to 13 carbon atoms as esterification catalyst.
Abstract: Oral compositions containing therapeutical agents wherein the undesirable consumer aesthetics associated with these agents are mitigated using coolants and sweeteners.
Abstract: A method for recovering amino acids, which comprises supplying a mixed solution containing inorganic acid salts, amino acids and non-electrolytes such as saccharides to a first-step resin layer comprising an Na type or K type strongly acidic ion exchange resin; separating an effluent into at least a first fraction containing coloring matters, acidic amino acids and ashes, a second fraction containing neutral amino acids and saccharides, and a third fraction containing betaines; supplying the second fraction to a second-step resin layer comprising at least one resin selected from the group consisting of NH4 type, Ca type and Mg type strongly acidic ion exchange resins, and optionally further supplying it to a third-step resin layer comprising an Mg type or Ca type strongly acidic ion exchange resin different from the resin of the second-step resin layer, thereby recovering various kinds of amino acids contained in an effluent.
Type:
Grant
Filed:
June 19, 2001
Date of Patent:
May 21, 2002
Assignee:
Nippon Beet Sugar Mfg. Co., Ltd.
Inventors:
Takashi Kanno, Koji Sayama, Tsutomu Aritsuka, Hiroto Kikuchi
Abstract: A continuous process for the preparation of monofunctional aromatic chloroformates (MAC) having the structure (I)
wherein n is an integer from 1 to 5, and R1 represents hydrogen, a branched or unbranched alkyl group having from 1-15 carbon atoms, an aryl group which may be substituted or unsubstituted, a cycloaliphatic group which may be substituted or unsubstituted, or an arylalkyl group which may be substituted or unsubstituted, the method comprising the steps of
a) introducing
1) an aqueous caustic solution;
2) a carbonyl chloride;
3) at least one monofunctional hydroxyaromatic compound; and
4) at least one inert organic solvent into a continuous reaction system; and
b) effecting contact between 1), 2), 3) and 4) for a time and at conditions sufficient to produce a MAC of structure (I).
Type:
Grant
Filed:
March 30, 1999
Date of Patent:
May 21, 2002
Assignee:
General Electric Company
Inventors:
James Manio Silva, David Michel Dardaris, Peter David Phelps
Abstract: This invention relates generally to the production and use of inorganic-polymer complexes for the controlled release of compounds including medicinals. The inorganic compound used is advantageously calcium sulfate-hemihydrate. The invention includes a composition for the controlled release of an active agent comprising: a) a hydrated or crystallized inorganic compound, and b) a matrix polymer which slows the release of the active agent, wherein the composition is a solid matrix due to the hydration or crystallization of the inorganic compound. Further included is a composition for the controlled release of an active agent comprising: a) a hydrated or crystallized inorganic compound, and b) a complexing agent which forms a salt or conjugate with the active agent, wherein the composition is a solid matrix due to the hydration or crystallization of the inorganic compound.
Abstract: A method and composition for the treatment of HIV and HBV infections in humans and other host animals is disclosed that includes the administration of an effective amount of a [5-carboxamido or 5-fluoro]-2′,3′-dideoxy-2′,3′-didehydro-pyrimidine nucleoside or a [5-carboxamido or 5-fluoro]-3′-modified-pyrimidine nucleoside, or a mixture or a pharmaceutically acceptable derivative thereof, including a 5′ or N4 alkylated or acylated derivative, or a pharmaceutically acceptable salt thereof, in a pharmaceutically acceptable carrier.
Abstract: The invention relates to a process for the preparation of high purity lactic acid from an aqueous solution containing said acid in the form of salt(s), characterised in that the aqueous solution is treated with a strong acid in order to liberate lactic acid in the free form and to produce salts of the corresponding strong acid, said salts of the strong acid are crystallised by evaporative crystallisation and lactic acid is recovered in the free form in solution.