序号 | 专利名 | 申请号 | 申请日 | 公开(公告)号 | 公开(公告)日 | 发明人 |
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221 | METHOD FOR OBTAINING OPTICALLY PURE AMINO ACIDS | EP10756310 | 2010-03-19 | EP2412704A4 | 2015-04-15 | KIM KWAN-MOOK; KIM HOJUN |
222 | PROCESS FOR PRODUCING -SUBSTITUTED ESTER | EP09826005.2 | 2009-10-22 | EP2357164B1 | 2015-03-25 | Akihiro, ISHII; Manabu YASUMOTO |
223 | METHOD FOR PRODUCING OPTICALLY ACTIVE DIAMINE DERIVATIVE | EP10750859.0 | 2010-03-10 | EP2407450A1 | 2012-01-18 | KAWANAMI, Koutarou |
The problem to be solved is to provide an important intermediate for production of an FXa inhibitor. The solution thereto is a method for industrially producing a compound (1) or a compound (4), comprising: [Step 1]: adding a quaternary ammonium salt and a metal azide salt to water to prepare an aqueous solution of an azidification reagent complex comprising quaternary ammonium salt-metal azide salt, and subsequently dehydrating the aqueous solution using an aromatic hydrocarbon solvent to form a mixed solution of the azidification reagent complex comprising quaternary ammonium salt-metal azide salt and the aromatic hydrocarbon solvent with a water content of 0.2% or less; and [Step 2]: adding, to the mixed solution prepared in [Step 1], a compound (2) wherein L represents a leaving group.
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224 | Verfahren zur Herstellung eines Gemisches von Lactid-Derivaten | EP11004941.8 | 2009-08-28 | EP2392570A1 | 2011-12-07 | Hagen, Rainer; Verweij, Adam Bastiaan; Mühlbauer, Udo; Schulz, Joachim; Tietz, Wolfgang; Göhler, Klaus-Dieter |
Die vorliegende Erfindung betrifft drei Varianten zur Herstellung einer Mischung aus von Milchsäure abgeleiteten cyclischen Diestern und insbesondere eines Racemates von Dilactid. Dabei kann wahlweise von den entsprechenden α-Hydroxycarbonsäuren, den entsprechenden cyclischen Diestern oder Oligomeren der entsprechenden α-Hydroxycarbonsäuren ausgegangen werden. |
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225 | PROCESS FOR PRODUCING -FLUORO- -AMINO ACIDS | EP09738726 | 2009-04-21 | EP2246322A4 | 2011-09-14 | AKIHIRO ISHII; TAKAKO YAMAZAKI; MANABU YASUMOTO; TAKASHI MASUDA; HIDEYUKI TSURUTA |
226 | VERFAHREN ZUR HERSTELLUNG EINES GEMISCHES VON LACTID-DERIVATEN | EP09778182.7 | 2009-08-28 | EP2321294A2 | 2011-05-18 | HAGEN, Rainer; VERWEIJ, Adam, Bastiaan; MÜHLBAUER, Udo; SCHULZE, Joachim; TIETZ, Wolfgang; GÖHLER, Klaus-Dieter |
The present invention relates to three variants for preparing a mixture of cyclic diesters derived from lactic acid and especially a racemate of dilactide. This can proceed, as desired, from the corresponding a-hydroxycarboxylic acids, the corresponding cyclic diesters or oligomers of the corresponding a-hydroxycarboxylic acids. | ||||||
227 | PROCESS FOR PRODUCING -FLUORO- -AMINO ACIDS | EP09738726.0 | 2009-04-21 | EP2246322A1 | 2010-11-03 | Akihiro ISHII; Takako YAMAZAKI; Manabu YASUMOTO; Takashi MASUDA; Hideyuki TSURUTA |
By reacting a β-hydroxy-α-amino acid with sulfuryl fluoride (SO2F2) in the presence of an organic base, it is possible to produce an α-fluoro-β-amino acid of the formula [2].
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228 | PROCESS FOR PRODUCTION OF CIS-3-SUBSTITUTED-3- AZABICYCLO[3.2.1]OCTAN-8-OL DERIVATIVE | EP08828642.2 | 2008-08-27 | EP2184274A1 | 2010-05-12 | HAKUTA, Hiroshi; IMAGAWA, Tsutomu; OOOKA, Hirohito; FUKUHARA, Shinya |
There are provided, according to the present invention, a method for producing a cis-3-substituted-3-azabicyclo[3.2.1]octan-8-ol derivative, the method characterized in that a trans-3-substituted-3-azabicyclo[3.2.1]octan-8-ol derivative or a mixture of the trans- and cis-3-substituted-3-azabicyclo[3.2.1]octan-8-ol derivatives is isomerized in the presence of an aluminum compound represented by a formula Al(OR1)3 (wherein R1 represents a hydrocarbon group in which a carbon atom having an oxygen atom bonded thereto is a secondary carbon atom). In the process, a ketone compound may be further added, in addition to the aluminum compound. |
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229 | Chiral binaphtol derivatives as alanine racemase mimics with powerful hydrogen bond donors: their use for optical resolution and optical inversion | EP08101348.4 | 2008-02-07 | EP2017244A3 | 2009-02-11 | Kim, Kwan Mook; Tang, Lijun |
Disclosed are chiral binaphthol derivatives as alanine racemase mimics having the ability to recognize amino alcohols selectively on the basis of chirality and transform amino acids from an L-form into a D-form. Methods for the optical resolution of amino acid or amino alcohol and for the optical transformation of D- and L-forms of amino acids using the binaphthol derivative are also provided. |
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230 | DEHYDROXYLATED FLUORINATING AGENT | EP07767494.3 | 2007-06-25 | EP2020402A1 | 2009-02-04 | ISHII, Akihiro; OOTSUKA, Takashi; YASUMOTO, Manabu; TSURUTA, Hideyuki; INOMIYA, Kenjin; UEDA, Koji; MOGI, Kaori |
There is provided a novel, useful dehydroxyfluorination agent containing sulfuryl fluoride (SO2F2) and an organic base that is free from a free hydroxyl group in the molecule. According to the present dehydroxyfluorination agent, it is not necessary to use perfluoroalkanesulfonyl fluoride, which is not preferable in large-scale use, and it is possible to advantageously produce optically-active fluoro derivatives, which are important intermediates of medicines, agricultural chemicals and optical materials, for example, 4-fluoroproline derivatives, 2'-deoxy-2'-fluorouridine derivatives, optically-active α-fluorocarboxylate derivatives, and monofluoromethyl derivatives, even in large scale. |
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231 | PROCESS FOR THE DE-ENRICHMENT OF ENANTIOMERICALLY ENRICHED SUBSTRATES | EP05804713.5 | 2005-10-27 | EP1809586A1 | 2007-07-25 | BLACKER, Andrew, John; STIRLING, Matthew, John |
There is provided a process for the de-enrichment of enantiomerically enriched compositions which comprises reacting an enantiomerically enriched composition comprising at least a first enantiomer or diastereomer of a substrate comprising a carbon-heteroatom bond, wherein the carbon is a chiral centre and the heteroatom is a group VI heteroatom, in the presence of a catalyst system and optionally a reaction promoter to give a product composition comprising first and second enantiomers or diastereomers of the substrate having a carbon-heteroatom bond, the ratio of second to first enantiomer or disatereomer in the product composition being greater than the ratio of second to first enantiomer or disatereomer in the enantiomerically enriched composition. Preferred substrates include compounds of Formula (1) wherein: X represents O, S; R1, R2 each independently represents an optionally substituted hydrocarbyl, a perhalogenated hydrocarbyl, an optionally substituted heterocyclyl group; or R1 & R2 are optionally linked in such a way as to form an optionally substituted ring(s); provided that R1 and R2 are selected such that * is a chiral centre. In a preferred process a compound of Formula : (2) wherein: X represents O, S; R1, R2 each independently represents an optionally substituted hydrocarbyl, a perhalogenated hydrocarbyl, an optionally substituted heterocyclyl group; or R1 & R2 are optionally linked in such a way as to form an optionally substituted ring(s); provided that R1 and R2 are different, may be obtained. | ||||||
232 | CATALYST COMPOSITIONS AND THEIR USE IN THE DE-ENRICHMENT OF ENANTIOMERICALLY ENRICHED SUBSTRATES | EP05804254.0 | 2005-10-27 | EP1809585A1 | 2007-07-25 | BLACKER, Andrew John; STIRLING, Matthew John |
There is provided a process for the de-enrichment of enantiomerically enriched compositions which comprises reacting an enantiomerically enriched composition comprising at least a first enantiomer or diastereomer of a substrate comprising a carbon-heteroatom bond, wherein the carbon is a chiral centre and the heteroatom is a group V heteroatom, in the presence of a catalyst system and optionally a reaction promoter to give a product composition comprising first and second enantiomers or diastereomers of the substrate having a carbon-heteroatom bond, the ratio of second to first enantiomer or disatereomer in the product composition being greater than the ratio of second to first enantiomer or disatereomer in the enantiomerically enriched composition. Preferred catalyst systems include transition metal halide complex of the formula MnXpYr wherein M is a transition metal; X is a halide; Y is a neutral optionally substituted hydrocarbyl complexing group, a neutral optionally substituted perhalogenated hydrocarbyl complexing group, or an optionally substituted cyclopentadienyl complexing group; and n, p and r are integers. The reaction promoter is preferably a halide salt. | ||||||
233 | VERFAHREN ZUR ISOMERISIERUNG VON SPIROZYKLISCHEN BETA-AMINOCARBOXYL- UND BETA-AMINOCARBONYLVERBINDUNGEN | EP95906212.6 | 1995-01-31 | EP0741727B1 | 2001-03-28 | KEPLINGER, Dietmar; KEPLINGER, Klaus; LAUS, Gerhard |
To produce defined isomer mixtures of compounds with spiro β-aminocarboxyl and/or β-aminocarbonyl systems the invention proposes that they be dissolved in solvents which have good dissolving power for these compounds, whose relative permittivity is sufficient to stabilize the amphoteric intermediates occuring in isomerization, which as proton donors constitute hydrogen bridges, whose basicity is less than that of the compounds for isomerization and whose boiling point is so high that an adequate reaction speed can be attained by raising temperature. Further, the invention proposes that the isomerization be influenced or terminated by altering at least one of these factors and/or by altering the temperature. | ||||||
234 | RACEMISATION AND ASYMMETRIC TRANSFORMATION PROCESSES USED IN THE MANUFACTURE OF LEVOBUPIVACAINE AND ANALOGUES THEREOF | EP95932092.0 | 1995-09-22 | EP0782569A1 | 1997-07-09 | DYER, Ulrich, Conrad; LOCK, Christopher, James; WOODS, Martin |
A process for the racemisation of an optically-enriched piperidine-2-carboxanilide compound, comprises heating the compound in the presence of an alkanoic or arylalkanoic acid. A process for the asymmetric transformation of such a compound comprises heating the compound in the presence of an acid as defined above, a chiral acid resolving agent and an inert cosolvent. | ||||||
235 | A PROCESS FOR THE PREPARATION OF ENANTIOMERIC 2-ALKANOIC ACIDS | EP91918099.0 | 1991-09-13 | EP0549710A1 | 1993-07-07 | ANTON, David, Leroy; FALLON, Robert, Donald; LINN, William, Joseph; STIEGLITZ, Barry; WITTERHOLT, Vincent, Gerard |
L'invention a trait à l'hydrolyse énantiosélective catalysée biologiquement de certains nitriles racémiques en R- ou S-amides correspondants, l'hydrolyse catalysée chimiquement ou biologiquement des amides en R- ou S-acides correspondants dans un traitement par l'eau ou dans un traitement continu utilisant l'obtention de racémiques et le recyclage de produits intermédiaires de nitriles énantiomères, les nitriles racémiques étant choisis dans le groupe AC(R1)(R2)CN, dans lequel A, R1 et R2 ont la notation ci-définie, ainsi que certaines matières biologiques utilisées pour catalyser le traitement. | ||||||
236 | Optical resolution method | EP91307218.7 | 1991-08-06 | EP0471498A3 | 1993-03-03 | Kawashima, Masatoshi |
The present invention provides three optical resolution methods. The first aspect comprises the steps of adding an optically active bifunctional resolving reagent to a bifunctional compound to form a liquid material, precipitating crystals therefrom, treating the crystals and the liquid material separately with an acidic material, a basic material, or a basic material and an acidic material, to obtain a pair of enantiomers of an optically active bifunctional compound. The second aspect comprises an optical resolution method by which one necessary enantiomer of a pair of enantiomers in an optically active bifunctional compound is exclusively obtained. The third aspect comprises a method for racemizing one unnecessary enantiomer of a pair of enantiomers in an optically active bifunctional compound which is formed by the optical resolution method of the present invention. |
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237 | Optical resolution method | EP91307218.7 | 1991-08-06 | EP0471498A2 | 1992-02-19 | Kawashima, Masatoshi |
The present invention provides three optical resolution methods. The first aspect comprises the steps of adding an optically active bifunctional resolving reagent to a bifunctional compound to form a liquid material, precipitating crystals therefrom, treating the crystals and the liquid material separately with an acidic material, a basic material, or a basic material and an acidic material, to obtain a pair of enantiomers of an optically active bifunctional compound. The second aspect comprises an optical resolution method by which one necessary enantiomer of a pair of enantiomers in an optically active bifunctional compound is exclusively obtained. The third aspect comprises a method for racemizing one unnecessary enantiomer of a pair of enantiomers in an optically active bifunctional compound which is formed by the optical resolution method of the present invention. |
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238 | Process for racemization of an optically active amino acid amide | EP91200307.6 | 1991-02-14 | EP0442585A1 | 1991-08-21 | Boesten, Wilhelmus Hubertus Joseph |
Process for the racemization of an optically active amino acid amide by reacting the amino acid amide with a carboxylic acid in the presence of a solvent, of water and of 0.5-4 equivalents of an aldehyde, calculated relative to the quantity of amino acid amide. Instead of an amino acid amide, the Schiff base of an amino acid amide and an aldehyde can also be used, in which case no extra aldehyde has to be added and the required quantity of water amounts to at least 1 equivalent relative to the quantity of Schiff base. This process gives fast racemization and a high yield of salt of the racemized amino acid amide and the carboxylic acid. |
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239 | Process for racemization of optically active 4-phenylbutanoic acid esters | EP90119178.3 | 1990-10-05 | EP0421472A1 | 1991-04-10 | Nohira, Hiroyuki; Onishi, Takashi; Yamamoto, Kazuo; Kumagai, Noriaki |
A process for the racemization of optically active 4-phenylbutanoic acid esters which comprises treating optically active 4-phenylbutanoic acid esters of the general formula (I)
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240 | Racemization process | EP86301417.1 | 1986-02-27 | EP0193405B1 | 1989-03-08 | Misner, Jerry Wayne |