| 序号 | 专利名 | 申请号 | 申请日 | 公开（公告）号 | 公开（公告）日 | 发明人 |
|---|---|---|---|---|---|---|
| 81 | Process for Producing alpha Substituted Ester | US13127955 | 2009-10-22 | US20110213176A1 | 2011-09-01 | Akihiro Ishii; Manabu Yasumoto |
| There is provided a process for producing an α-substituted ester by reaction of a fluorosulfuric acid ester of α-hydroxyester with a Grignard reagent in the presence of a zinc catalyst. It is newly found that the reaction for production of α-substituted esters, in which the raw reaction substrate is limited to expensive trifluoromethanesulfonic acid esters, can proceed favorably with the use of fluorosulfuric acid esters suitable for mass-production uses. By the use of the fluorosulfuric acid ester high in optical purity, it is possible to obtain the α-substituted ester with high optical purity upon inversion of the asymmetric carbon configuration. The process of the present invention can solve all of the prior art problems and can be applied for industrial uses. | ||||||
| 82 | ALANINE RACEMASE CHIRAL BINAPHTHOL DERIVATIVE WITH POWERFUL HYDROGEN BOND DONOR, AND OPTICAL RESOLUTION AND OPTICAL TRANSFORMATION METHODS USING THE SAME | US12912431 | 2010-10-26 | US20110040101A1 | 2011-02-17 | 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. | ||||||
| 83 | Alanine racemase chiral binaphthol derivative with powerful hydrogen bond donor, and optical resolution and optical transformation methods using the same | US12028566 | 2008-02-08 | US07847124B2 | 2010-12-07 | 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. | ||||||
| 84 | Process for Production of Optically Active Benzylamine Derivatives | US11993821 | 2006-06-20 | US20100081845A1 | 2010-04-01 | Teruaki Sugiyama; Akinori Fujishima; Atsushi Umetani; Nobutaka Matsunaga; Yoshiyuki Omori; Norihiko Seko |
| A benzylamine derivative has a structure represented by the following formula (1): In a method for optical resolution of the benzylamine derivative, optically active mandelic acid is used as an optical resolving agent. In an optical resolution step in a production method of the optically active benzylamine derivative, an optically active (S)-benzylamine derivative represented by the formula (3) is precipitated as (S)-mandelic acid salt from a solution containing the benzylamine derivative and (S)-mandelic acid: wherein Ar represents an aryl group that has 6 to 15 carbon atoms and may have a substituent, and *1 represents an asymmetric carbon atom. | ||||||
| 85 | CATALYST COMPOSITIONS AND THEIR USE IN THE DE-ENRICHMENT OF ENANTIOMERICALLY ENRICHED SUBSTRATES | US11577912 | 2005-10-27 | US20090163719A1 | 2009-06-25 | Andrew John Blacker; Matthew John Stirling |
| 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 diastereomer in the product composition being greater than the ratio of second to first enantiomer or diastereomer 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. | ||||||
| 86 | STEREOINVERSION OF AMINO ACIDS | US11963737 | 2007-12-21 | US20080153137A1 | 2008-06-26 | Ian Victor James Archer; Ian Fotheringham; Reuben 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. | ||||||
| 87 | Process for the production of specific isomer mixtures from oxindole alkaloids | US725879 | 1996-10-04 | US5723625A | 1998-03-03 | Dietmar Keplinger; Klaus Keplinger; Gerhard Laus |
| To produce defined isomer mixtures of compounds with spirocyclic beta-aminocarboxyl and/or beta-aminocarbonyl systems the invention supposes 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 prevented, influenced, or terminated by altering at least one of these factors and or by altering the temperature. | ||||||
| 88 | Process for the production of xylitol | US568601 | 1995-12-05 | US5714602A | 1998-02-03 | Roland Herwig Freidrich Beck; Myriam Elseviers; Sonia Marianne Jeannine Coomans |
| The present invention discloses a method of producing a pentitol from a hexaldonic acid. The hexaldonic acid is decarboxylated for example in the presence of sodium hypochlorite or hydrogen peroxide. After hydrogenation and optionally isomerisation the desired pentitol, which is obtained in high yield, can be purified. The present invention starts from gluconic acid in free or salt form or as a lactone, xylitol is the final product. | ||||||
| 89 | Method of intercoversion of enantiomers of acyclic 1,2-dihydroxy-3-alkenes | US999240 | 1992-12-31 | US5250743A | 1993-10-05 | Neil W. Boaz |
| In accordance with the present invention, a method for the interconvertion of the enantiomers of acyclic 1,2-dihydroxy-3-alkenes or for converting either enantiomer of acylic 1,2-dihydroxy-3-alkenes to the corresponding antipodal 1-hydroxy-2-alkoxy-3-alkene compounds has been discovered, comprising reacting in an acidic reaction media either enantiomer of an acylic vinyl epoxide (which can be derived from the corresponding acyclic 1,2-dihydroxy-3-alkene) with water, alcohol, or a mixture thereof. When substantially optically pure acyclic vinyl epoxide compounds are employed in the inventive method, the interconverted acyclic 1,2-dihydroxy-3-alkene or 1-hydroxy-2-alkoxy-3-alkene compound products are also substantially optically pure. | ||||||
| 90 | Process for racemization of optically active 4-phenylbutanoic acid esters | US588545 | 1990-09-26 | US5066826A | 1991-11-19 | Hiroyuki Nohira; Takashi Onishi; Kazuo Yamamoto; Noriaki Kumagai |
| 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 (1) ##STR1## wherein R.sup.1 represents a hydroxy group, a hydroxy group protected by vinyl ester, or a lower acyloxy group and R.sup.2 represents a lower alkyl group with a base selected from the group consisting of alkali metal alcoholates, alkali metal hydrides, and alkali metal amides is provided. | ||||||
| 91 | Method for racemizing an optically active amino acid | US89551 | 1987-08-26 | US4769486A | 1988-09-06 | Tsuneo Harada; Kiyotaka Oyama |
| A method for racemizing an optically active amino acid, which comprises heating the optically active amino acid in an aqueous solution under an alkaline condition in the presence of an alkali metal salt. | ||||||
| 92 | Method for racemization of optically active amines | US861515 | 1977-12-16 | US4158016A | 1979-06-12 | 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. | ||||||
| 93 | Process for racemization of allethrolone | US795021 | 1977-05-09 | US4111993A | 1978-09-05 | Charles Pavan; Jacques Bulidon |
| A novel process for the preparation of racemic allethrolone of the (R,S) configuration comprising heating optically active allethrolone of the (R) configuration or of the (S) configuration or a mixture of the (R) and (S) configurations in non-equimolecular proportions with formic acid to form the formate of racemic allethrolone of (R,S) configuration and hydrolyzing the latter in the presence of an acid or base to obtain racemic (R,S) allethrolone. | ||||||
| 94 | METHOD FOR OBTAINING OPTICALLY PURE AMINO ACIDS | PCT/KR2010001707 | 2010-03-19 | WO2010110555A3 | 2010-12-09 | KIM KWAN-MOOK |
| The present invention relates to a method for obtaining optically pure amino acids, including optical resolution and optical conversion. The method of the present invention significantly shortens the time taken for optical transformation, and enables the repeated use of an organic solution containing a chiral selective 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. | ||||||
| 95 | ラセミまたは光学的に活性のあるＤまたはＬ−α−グリセロホスホリルコリン固体の製造方法 | JP2017536504 | 2015-09-24 | JP2017534677A | 2017-11-24 | オオク ワング，ソオン; ミョウング ユン，ダエ; キム，チャング‐ミン |
| 本発明は、液状のラセミまたは光学的に活性のあるDまたはL−α−グリセロホスホリルコリンを有機溶媒を用いてラセミまたは光学的に活性のあるDまたはL−α−グリセロホスホリルコリン固体を製造することを特徴とし、従来の方式である溶媒の溶解度差を利用した方法ではなく、相変化を通じてより容易に高収率の固体を製造することができるという効果を奏する。【選択図】図1 | ||||||
| 96 | 光学活性カルボン酸エステルの製造方法 | JP2015560069 | 2015-02-02 | JPWO2015115650A1 | 2017-03-23 | 椎名 勇; 勇 椎名 |
| 動的速度論的光学分割を用いて、α−窒素置換基を有する光学活性カルボン酸エステルを高収率かつ高エナンチオ選択率で製造する方法を提供する。本発明に係る光学活性カルボン酸エステルの製造方法は、下記式(a)で表されるラセミのカルボン酸と、特定のアルコール又はフェノール誘導体とを、酸無水物及び不斉触媒の存在下、双極子モーメント3.5以上の極性溶媒中で反応させ、上記ラセミのカルボン酸のうち一方のエナンチオマーを選択的にエステル化するとともに、他方のエナンチオマーをラセミ化する工程を含む。式(a)中、Ra1は環を構成する窒素原子を介して不斉炭素に結合した含窒素複素芳香環基を示し、Ra2は有機基を示す。 | ||||||
| 97 | Method of separating a chroman compounds as well as chiral isomer of the derivative and precursor | JP2014509706 | 2012-05-08 | JP2014520074A | 2014-08-21 | ゲルハルト シーファー，; トーマス ネッチェル，; アレクサンダー ルチア レオナルドゥス デュシャトー， |
| 本発明は、クロマン化合物、特にトコフェロール及びトコトリエノール並びにそれらのエステル及び中間体の、キラル異性体を分離する方法に関する。 本方法は、所望の異性体のより高い収率での分離を可能にし、かつ非常に効率的なやり方で非所望の異性体の使用を可能にすることが見出された。 前記方法は、工業プロセスにおいて実施される場合に特に有用である。 更に、本方法は、従来の工業的合成から生じる異性体混合物を使用することを可能にすることが見出された。 | ||||||
| 98 | Cis-3-production method of substituted-3-azabicyclo [3.2.1] octane-8-ol derivative | JP2009530152 | 2008-08-27 | JP5258771B2 | 2013-08-07 | 浩 白田; 務 今川; 浩仁 大岡; 慎也 福原 |
| 99 | 光学活性なジアミン誘導体の製造方法 | JP2011503838 | 2010-03-10 | JPWO2010104106A1 | 2012-09-13 | 光太郎 川波 |
| 課題は、FXa阻害薬の製造のための重要中間体を提供することである。解決手段は、化合物(1)及び化合物(4)を工業的に製造する方法であって;[第1操作]:4級アンモニウム塩及びアジ化金属塩を水に添加して4級アンモニウム塩−アジ化金属塩からなるアジ化試薬複合体の水溶液を調製し、引き続いて該水溶液を、芳香族炭化水素系溶媒を用いて脱水処理を行い、水分含量が0.2%以下の4級アンモニウム塩−アジ化金属塩からなるアジ化試薬複合体の芳香族炭化水素系溶媒混合液とすること;次いで、[第2操作]:上記の[第1操作]で調製した混合液に、化合物(2)(Lは脱離基を示す。)を添加すること;を特徴とする製造方法である。 | ||||||
| 100 | Method of obtaining optically pure amino acids | JP2012501927 | 2010-03-19 | JP2012521415A | 2012-09-13 | クァンムク キム; ホジュン キム |
| 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. | ||||||
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