| 序号 | 专利名 | 申请号 | 申请日 | 公开（公告）号 | 公开（公告）日 | 发明人 |
|---|---|---|---|---|---|---|
| 41 | Method of racemizing optically active N-acyl amino acids in aqueous solution | US935835 | 1978-08-22 | US4182904A | 1980-01-08 | Giselher Franzmann; Hans-Leo Hulsmann |
| A process has been invented for the racemization of optically active N-acylamino acids in aqueous solution which comprises treating said optically active N-acylamino acids with ketene. | ||||||
| 42 | Racemization of optically active allethrolone | US597813 | 1975-07-21 | US4001334A | 1977-01-04 | Takeaki Umemura |
| The present invention provides a process for preparing racemic allethrolone which comprises reacting (-) allethrolone with hydroxylamine to form the corresponding allethrolone.oxime and then hydrolyzing the oxime in water or a mixture of water and an organic solvent miscible with water in the presence of an acid. | ||||||
| 43 | Method for preparing racemic or optically active D- or L-A-glycerophosphoryl choline solids | US15468136 | 2017-03-24 | US10023596B2 | 2018-07-17 | Soon Ook Hwang; Dae Myoung Yun; Chang-min Kim |
| The present invention is characterized in that racemic or optically active D- or L-α-glycerophosphoryl choline solids are prepared from liquid type racemic or optically active D- or L-α-glycerophosphoryl choline using an organic solvent. The present invention can produce solids at a high yield more easily through phase transformation rather than a method using a difference in solubility in a solvent, which is an existing method. | ||||||
| 44 | Atropisomers and Methods of Altering Enantiomeric Excess | US15854885 | 2017-12-27 | US20180179120A1 | 2018-06-28 | Kenneth Hanson; Suliman A. Ayad; Victoria A. Posey |
| Provided herein are methods of altering enantiomeric excess. The methods may include irradiating an atropisomer that includes at least one chiral substituent to alter the enantiomeric excess of the atropisomer. The at least one chiral substituent may be removed following irradiation. | ||||||
| 45 | Method for producing optically active carboxylic acid ester | US15115764 | 2015-02-02 | US09796640B2 | 2017-10-24 | Isamu Shiina |
| Provided is a method for producing an optically active carboxylic acid ester at a high yield and with high enantioselectivity using dynamic kinetic resolution, said optically active carboxylic acid ester having an α-nitrogen substituent. This method for producing an optically active carboxylic acid ester includes a step in which racemic carboxylic acid represented by formula (a) and a specific alcohol or phenol derivative are reacted in a polar solvent having a dipole moment of at least 3.5 in the presence of an acid anhydride and an asymmetric catalyst, one enantiomer of the racemic carboxylic acid is selectively esterified, and the other enantiomer is racemized. In formula (a), Ra1 represents a nitrogen-containing heteroaromatic ring group bonded to an assymetric carbon via a nitrogen atom constituting a ring, and Ra2 is an organic group. | ||||||
| 46 | METHOD FOR PRODUCING OPTICALLY ACTIVE CARBOXYLIC ACID ESTER | US15115764 | 2015-02-02 | US20170008820A1 | 2017-01-12 | Isamu SHIINA |
| Provided is a method for producing an optically active carboxylic acid ester at a high yield and with high enantioselectivity using dynamic kinetic resolution, said optically active carboxylic acid ester having an α-nitrogen substituent. This method for producing an optically active carboxylic acid ester includes a step in which racemic carboxylic acid represented by formula (a) and a specific alcohol or phenol derivative are reacted in a polar solvent having a dipole moment of at least 3.5 in the presence of an acid anhydride and an asymmetric catalyst, one enantiomer of the racemic carboxylic acid is selectively esterified, and the other enantiomer is racemized. In formula (a), Ra1 represents a nitrogen-containing heteroaromatic ring group bonded to an assymetric carbon via a nitrogen atom constituting a ring, and Ra2 is an organic group. | ||||||
| 47 | Method for producing racemate of compound | US14439597 | 2013-10-28 | US09284260B2 | 2016-03-15 | Tomoaki Takahashi; Taro Hirose |
| A method for producing a racemate of a compound represented by Formula (1), including bringing a transition metal catalyst into contact with an optically active form of the compound represented by Formula (1): [in Formula (1), a ring X1 represents an aromatic ring; R1 represents a C1-6 alkyl group, a C3-8 cycloalkyl group, or a C1-6 halo-alkyl group; R2 is a group different from R1 and represents a C1-6 alkyl group, a C3-8 cycloalkyl group, or a C1-6 halo-alkyl group, or R2 and the ring X1 are bonded to each other to form a ring; a hydrogen atom(s) of the ring X1 is optionally replaced with a C1-6 alkyl group, a C1-6 halo-alkyl group, a cyano group, a nitro group, a C1-6 alkoxy group, or a halogen atom; and * represents an asymmetric carbon atom]. | ||||||
| 48 | Method for producing optically active diamine derivative | US13231081 | 2011-09-13 | US09175012B2 | 2015-11-03 | Koutarou Kawanami |
| 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. | ||||||
| 49 | Process of separating chiral isomers of chroman compounds and their derivatives and precursors | US14116880 | 2012-05-08 | US08987480B2 | 2015-03-24 | Gerhard Schiefer; Thomas Netscher; Alexander Lucia Leonardus Duchateau |
| The present invention relates to a process of separating chiral isomers of chroman compounds, particularly tocopherols and tocotrienols as well as the esters and intermediates thereof. It has been found that this process allows a separation of the desired isomer with a higher yield and enables the use of the non-desired isomers in a very efficient way. Said process is particularly useful when implemented in an industrial process. Furthermore, it has been found that this process allows using isomer mixtures as they result from traditional industrial synthesis. | ||||||
| 50 | PROCESS OF SEPARATING CHIRAL ISOMERS OF CHROMAN COMPOUNDS AND THEIR DERIVATIVES AND PRECURSORS | US14116880 | 2012-05-08 | US20140155636A1 | 2014-06-05 | Gerhard Schiefer; Thomas Netscher; Alexander Lucia Leonardus Duchateau |
| The present invention relates to a process of separating chiral isomers of chroman compounds, particularly tocopherols and tocotrienols as well as the esters and intermediates thereof. It has been found that this process allows a separation of the desired isomer with a higher yield and enables the use of the non-desired isomers in a very efficient way. Said process is particularly useful when implemented in an industrial process. Furthermore, it has been found that this process allows using isomer mixtures as they result from traditional industrial synthesis. | ||||||
| 51 | Process for producing α-fluoro-β-amino acids | US12919108 | 2009-04-21 | US08217196B2 | 2012-07-10 | 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]. By using a C8-12 tertiary amine having two or more alkyl groups of C3 or higher, and especially diisopropylethylamine, as the organic base, by-production of quantery ammonium salts is effectively suppressed. By applying the production process of the present invention, it is possible to very easily produce (2R)-3-(dibenzylamino)-2-fluoropropionic acid methyl ester, which is extremely important as a pharmaceutical intermediate, with high positional selectivity even on an industrial scale. | ||||||
| 52 | METHOD FOR OBTAINING OPTICALLY PURE AMINO ACIDS | US13258948 | 2010-03-19 | US20120016157A1 | 2012-01-19 | Kwan-Mook Kim; Hojun Kim |
| This invention relates to a method for obtaining optically pure amino acids, including optical resolution and optical conversion. This method significantly shortens the time taken for optical transformation, and enables the repeated use of an organic solution containing a enantioselective receptor, to thereby obtain optically pure amino acids in a simple and remarkably efficient manner, and to enable the very economical mass production of optically pure amino acids. | ||||||
| 53 | PROCESS FOR THE MANUFACTURE OF RACEMIC 2-ARYL-PROPIONIC ACID | US13001893 | 2009-06-30 | US20110172460A1 | 2011-07-14 | Stephen John Martin; Scott Dale Makin |
| There is described a process for the manufacture of a racemic 2-aryl propionic acid compound, or a pharmaceutically acceptable salt thereof, which comprises reacting the S- or R-enantiomer of the corresponding 2-aryl propionic acid compound with a base. | ||||||
| 54 | Compositions, Methods For Preparing Amino Acids And Nuclear Magnetic Resonance Spectroscopy | US13004321 | 2011-01-11 | US20110104076A1 | 2011-05-05 | Brian Keith Shull |
| The present invention relates to amino acids, complexes, and compounds comprising deuterium and tritium isotopes preferably alpha deuterated amino acids, polypeptides, antibodies, derivatives and saccharide-amino acid complexes and conjugates. In some embodiments, the invention relates to methods of using compounds comprising deuterium for imaging biochemical concentrations and distributions in mammalian tissues using nuclear magnetic resonance spectroscopy. In some embodiments, the invention relates to the used of said amino acids derivatives and complexes in boron neutron capture therapy. In some embodiments, the present invention relates to the preparation of amino acids, polypeptides, antibodies, derivatives and saccharide complexes/conjugates comprising heavy hydrogen isotopes. In some embodiments, the invention relates to racemizing amino acids starting from compositions of any optical purity. In further embodiments, the invention relates to the preparation of amino acids and their N-acyl counterparts with deuterium incorporated at the alpha carbon. | ||||||
| 55 | Process for Producing Alpha-Fluoro-Beta-Amino Acids | US12919108 | 2009-04-21 | US20110015428A1 | 2011-01-20 | 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]. By using a C8-12 tertiary amine having two or more alkyl groups of C3 or higher, and especially diisopropylethylamine, as the organic base, by-production of quantery ammonium salts is effectively suppressed. By applying the production process of the present invention, it is possible to very easily produce (2R)-3-(dibenzylamino)-2-fluoropropionic acid methyl ester, which is extremely important as a pharmaceutical intermediate, with high positional selectivity even on an industrial scale. | ||||||
| 56 | Ibuprofen amine salts and synthesis thereof | US12380207 | 2009-02-25 | US20100022798A1 | 2010-01-28 | Tu Lee; Yeh-Wen Wang |
| The present invention discloses an ibuprofen amine salt and the synthesis thereof, and more particularly an ibuprofen amine salt yielded by the neutralization reaction of a racemic mixture of ibuprofen with tris(hydroxymethyl)aminomethane in a solution system of water and an organic solvent. Compared with racemic mixtures of ibuprofen, the ibuprofen amine salt has higher solubility and a higher melting point, thereby having better bioavailability and properties than racemic mixtures of ibuprofen during pharmaceutical processing. Further, the ibuprofen amine salts of the present invention are stable between pH 4 and 9 so that they can be more widely applied to medicines. | ||||||
| 57 | Processes for preparing armodafinil intermediate | US11999597 | 2007-12-05 | US20080214862A1 | 2008-09-04 | Ben-Zion Dolitzky; Kobi Chen |
| The present invention encompasses processes for preparing intermediates of armodafinil, and the conversion of the intermediates to armodafinil. | ||||||
| 58 | Racemisation process | US11836422 | 2007-08-09 | US07408082B1 | 2008-08-05 | John Blacker |
| The present invention relates to a novel process for obtaining (1S,4S)N-methyl-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-naphthaleneamine from a mixture of its isomers. The process involves isomerising the 1-position and the 4-position and effecting separation of the desired isomer by methods such as fractured crystallization. The process can be operated as a continuous process. | ||||||
| 59 | Compositions, methods of preparing amino acids, and nuclear magnetic resonance spectroscopy | US11594299 | 2006-11-08 | US20070104648A1 | 2007-05-10 | Brian Shull |
| The present invention relates to amino acids, complexes, and compounds comprising deuterium and tritium isotopes preferably alpha deuterated amino acids, polypeptides, antibodies, derivatives and saccharide-amino acid complexes and conjugates. In some embodiments, the invention relates to methods of using compounds comprising deuterium for imaging biochemical concentrations and distributions in mammalian tissues using nuclear magnetic resonance spectroscopy. In some embodiments, the invention relates to the used of said amino acids derivatives and complexes in boron neutron capture therapy. In some embodiments, the present invention relates to the preparation of amino acids, polypeptides, antibodies, derivatives and saccharide complexes/conjugates comprising heavy hydrogen isotopes. In some embodiments, the invention relates to racemizing amino acids starting from compositions of any optical purity. In further embodiments, the invention relates to the preparation of amino acids and their N-acyl counterparts with deuterium incorporated at the alpha carbon. | ||||||
| 60 | Racemisation process | US797524 | 1997-02-07 | US5821369A | 1998-10-13 | Raymond McCague |
| A process for the racemization of an enantiomerically-enriched compound of formula (3), comprises treatment of enantiomerically-enriched (3) with a base to obtain anion (4), optionally in protonated form, which is then combined with CH.sub.2 =CH--Y.sup.1 to form racemic (3), ##STR1## wherein Ar=aryl or heteroaryl; Ak=C.sub.1-20 alkyl; X=CN, CO.sub.2 R, CONR.sup.1 R.sup.2, and COR; Y and Y.sup.1 are independently selected from CN, CO.sub.2 R, CONR.sup.1 R.sup.2 and R, R.sub.1 and R.sub.2 are independently selected from H and C.sub.1-20 alkyl; optionally as a salt thereof. This racemization process can be used as part of an efficient synthesis of enantiomerically-enriched verapamil or aminoglutethimide. | ||||||
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