| 序号 | 专利名 | 申请号 | 申请日 | 公开（公告）号 | 公开（公告）日 | 发明人 |
|---|---|---|---|---|---|---|
| 21 | 用于制备光学活性二胺衍生物的方法 | CN201080011257.7 | 2010-03-10 | CN102348680A | 2012-02-08 | 川波光太郎 |
| 本发明要解决的问题是提供用于FXa抑制剂制备的重要中间体。其解决方案是用于工业制备化合物(1)或化合物(4)的方法，包括：[步骤1]：向水中添加季铵盐和叠氮化金属盐以制备包含季铵盐-叠氮化金属盐的叠氮化试剂复合物的水溶液，并且随后使用芳香烃溶剂对该水溶液进行脱水以形成水含量为0.2%或更低的包含季铵盐-叠氮化金属盐的叠氮化试剂复合物和芳香烃溶剂的混合溶液；以及[步骤2]：向[步骤1]中制备的混合溶液中添加化合物(2)，其中L表示离去基团。 | ||||||
| 22 | 制左旋布比卡因及类似物中所用的外消旋及不对称转变方法 | CN95195252.8 | 1995-09-22 | CN1104416C | 2003-04-02 | U·C·迪尔; C·J·劳克; M·伍兹 |
| 旋光富集的哌啶-2-酰胺化物的外消旋方法，包括，在链烷酸或芳基链烷酸存在下加热该化合物。这种化合物的不对称转变方法，包括，在上述酸、手性酸拆解试剂和惰性共溶剂存在下加热该化合物。 | ||||||
| 23 | Method for the production of a mixture of lactide derivatives | US13060553 | 2009-08-28 | US20120149920A1 | 2012-06-14 | Rainer Hagen; Adam Bastiaan Verweij; Udo Muhlbauer; Joachim Schulze; Wolfgang Tietz; Klaus-Dieter Göhler; Olga Renate Göhler |
| A mixture of cyclic diesters derived from lactic acid and in cases a mixture of a racemate of dilactide may be produced in several different processes. In some instances, the process can thereby start from the corresponding alpha-hydroxycarboxylic acids, the corresponding cyclic diesters or oligomers of the corresponding alpha-hydroxycarboxylic acids. | ||||||
| 24 | Alanine racemase chiral binaphthol derivative with powerful hydrogen bond donor, and optical resolution and optical transformation methods using the same | US12912431 | 2010-10-26 | US08193370B2 | 2012-06-05 | Kwan Mook Kim; Lijun Tang |
| Disclosed is an alanine racemase chiral binaphthol derivative 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. | ||||||
| 25 | Stereoinversion of amino acids in a single reactor | US11963737 | 2007-12-21 | US08133717B2 | 2012-03-13 | Ian Victor James Archer; Ian Fotheringham; Rueben Carr; Susan Alison Arnold |
| A process is described to prepare a single enantiomer of an amino acid from its opposite enantiomer or from a racemic mixture, using an oxidase biocatalyst and a supported metal catalyst in separate, sequential reactions in water. The process can be operated in batch or continuous mode. | ||||||
| 26 | Dehydroxyfluorination agent | US12306826 | 2007-06-25 | US08058412B2 | 2011-11-15 | Akihiro Ishii; Takashi Ootsuka; Manabu Yasumoto; Hideyuki Tsuruta; Kenjin Inomiya; Koji Ueda; Kaori Mogi |
| 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. | ||||||
| 27 | METHOD FOR THE PRODUCTION OF OPTICALLY ACTIVE ALPHA ALKYL CARBONYL COMPOUNDS | US12679125 | 2008-09-18 | US20100305352A1 | 2010-12-02 | Bernhard Breit; Christopher Studte |
| A method for the production of optically active α-alkylcarbonyl compounds with retention of the stereo information of the starting compound. The starting compound used here is a carbonyl compound which has, in the α-position, a leaving group which is substituted by an alkyl group with inversion of the configuration. The substitution of the leaving group is effected with the use of an alkylmagnesium Grignard and a zinc (II) salt or a zinc organyl. The method permits the production of optically active α-alkylcarbonyl compounds at very mild temperatures (for example 0° C.) with the use of starting compounds which are easy to prepare and economical and nontoxic catalysts, it also being possible to achieve a very high yield. | ||||||
| 28 | METHOD FOR PRODUCING CIS-3-SUBSTITUTED-3-AZABICYCLO[3.2.1]OCTAN-8-OL DERIVATIVE | US12674326 | 2008-08-27 | US20100286398A1 | 2010-11-11 | Hiroshi Hakuta; Tsutomu Imagawa; Hirohito Oooka; Shinya Fukuhara |
| 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. | ||||||
| 29 | Dehydroxyfluorination Agent | US12306826 | 2007-06-25 | US20090250658A1 | 2009-10-08 | Akihiro Ishii; Takashi Ootsuka; Manabu Yasumoto; Hideyuki Tsuruta; Kenjin Inomiya; Koji Ueda; Kaori Mogi |
| 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. | ||||||
| 30 | ALANINE RACEMASE CHIRAL BINAPHTHOL DERIVATIVE WITH POWERFUL HYDROGEN BOND DONOR, AND OPTICAL RESOLUTION AND OPTICAL TRANSFORMATION METHODS USING THE SAME | US12028566 | 2008-02-08 | US20090023931A1 | 2009-01-22 | Kim Kwan Mook; Tang Lijun |
| Disclosed is an alanine racemase chiral binaphthol derivative 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. | ||||||
| 31 | Racemization of precursors to levobupivacaine and analogues thereof | US250473 | 1999-02-12 | US6156900A | 2000-12-05 | Ulrich Conrad Dyer; Martin Woods; Raymond McCague |
| A process for the preparation of optically-enriched pipecolic acid as a salt with an optically-active acid, comprises asymmetric transformation of pipecolic acid, as a racemic mixture of a mixture enriched in the opposite enantiomer from that desired, with the optically-active acid in a solvent comprising an acid that causes racemisation, in the absence of aldehyde. | ||||||
| 32 | Racemization and asymmetric transformation processes used in the manufacture of levobupivacaine and analogues thereof | US809941 | 1997-05-30 | US5786484A | 1998-07-28 | Ulrich Conrad Dyer; Christopher James Lock; Martin Woods |
| 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. | ||||||
| 33 | Optical resolution method | US293036 | 1994-08-19 | US5510520A | 1996-04-23 | Masatoshi Kawashima |
| 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, and 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. | ||||||
| 34 | Racemization process for optically active carboxylic acids, salts and esters | US971115 | 1992-11-04 | US5278338A | 1994-01-11 | Rhonda L. Trace |
| A method for racemizing an optically active carboxylic acid, or ester thereof, of the formula: ##STR1## where R.sub.1 is hydrogen, hydroxy, halo, cyano, C.sub.1 to C.sub.6 linear or branched alkoxy, amino or substituted amino or the group ##STR2## is nitrile; R.sub.2, R.sub.3 and R.sub.4 are different and are hydrogen or C.sub.1 to C.sub.6 linear or branched alkyl, C.sub.1 to C.sub.6 linear or branched haloalkyl, aralkyl, cycloalkyl, alkyl substituted cycloalkyl, C.sub.6 to C.sub.10 aryl, C.sub.1 to C.sub.6 linear or branched alkoxy, C.sub.6 to C.sub.10 aryloxy, C.sub.1 to C.sub.6 alkylthio, C.sub.3 to C.sub.8 cycloalkylthio, C.sub.6 to C.sub.10 arylthio, C.sub.6 to C.sub.10 arylcarbonyl, C.sub.4 to C.sub.8 cycloalkenyl, trifluoromethyl, halo, C.sub.4 to C.sub.5 heteroaryl, C.sub.10 to C.sub.14 aryl, or biphenyl unsubstituted or substituted with methyl or halo, comprising heating said optically active carboxylic acid or ester thereof in the presence of water at a temperature of from about 40.degree. C. to about 200.degree. C. in the presence of a catalytically effective amount of a compound of the formula M(XO).sub.n where M is an alkali or alkaline earth metal, X is halogen, where n is 1 or 2 for a time sufficient to racemize said carboxylic acid or ester thereof. | ||||||
| 35 | Racemization process | US706373 | 1985-02-27 | US4777291A | 1988-10-11 | Jerry W. Misner |
| The present invention provides a process for the epimerization of (+)-N-methyl-3-(2-methylphenoxy)- 3-phenylpropylamine to its racemic form with an anion forming compound in a suitable solvent. | ||||||
| 36 | Racemization and resolution of .alpha.-amino acids | US770508 | 1985-08-28 | US4647692A | 1987-03-03 | Victor W. Jacewicz |
| Process for racemization of amino acids by use of a ketone and an organic acid such as acetic acid. In particular, a process for resolution of free .alpha.-amino acids with in situ racemization. The resolution of 4-hydroxyphenylglycine and 3,4-dihydroxyphenylglycine with 3-bromocamphor-9-sulphonic acid with in situ racemization are specifically mentioned. | ||||||
| 37 | Racemization of optically active compounds having a bromine substituted chiral carbon atom | US771092 | 1985-08-30 | US4613690A | 1986-09-23 | Samun K. Dahod |
| Optically active compounds having a chlorine atom attached to the chiral carbon atom such as 2-bromoaliphatic acids can be racemized without by-product formation by heating an acidified solution of the organic acid at a temperature sufficient to accomplish racemization, the solution being substantially devoid of ionized halogen other than bromine ions. The preferred acidifying agent is hydrobromic acid. The use of hydrochloric acid causes extensive by-product formation. | ||||||
| 38 | Racemization of optically active compounds having a chlorine substituted chiral carbon atom | US771091 | 1985-08-30 | US4613689A | 1986-09-23 | Patricia Siuta-Mangano; Samun K. Dahod |
| Optically active compounds having a chlorine atom attached to the chiral carbon atom such as 2-chloroaliphatic acids can be racemized without by-product formation by heating an acidified solution of the compound in the presence of chloride ion at sufficient strength, and at a pH and temperature sufficient to accomplish racemization. The preferred acidifying agent and source of chloride ion is hydrochloric acid. The use of hydrochloric acid at room temperature as well as the use of either sulfuric acid or caustic soda failed to produce racemization. | ||||||
| 39 | Process for racemizing optically active .alpha.-amino acids or a salt thereof | US337322 | 1982-01-05 | US4401820A | 1983-08-30 | Ichiro Chibata; Shigeki Yamada; Chikara Hongo; Ryuzo Yoshioka |
| DL-.alpha.-amino acids or a salt thereof can be obtained by racemizing an optically active .alpha.-amino acid or a salt thereof in the presence of an aliphatic acid and an aldehyde. | ||||||
| 40 | Method for racemization of optically active amines | US686575 | 1976-05-14 | US4246424A | 1981-01-20 | Tsuneyuki Nagase; Gohu Suzukamo; Yoshio Suzuki |
| A method for racemization of optically active amines which comprises contacting an optically active amine of the formula: ##STR1## wherein C* is an asymmetric carbon atom, R.sub.1 is alkyl, aralkyl or aryl and R.sub.2 is aryl or alkoxycarbonyl, the aryl or aralkyl moiety bearing optionally one or more alkyl or alkoxy groups on the aromatic ring, provided that R.sub.1 and R.sub.2 are always different from each other, with a catalyst comprising an alkali metal and a polycyclic aromatic hydrocarbon until a sufficient amount of the optically active amine is racemized. | ||||||
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