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71. 发明申请

US20110190527A1 METHOD OF PRODUCING OPTICALLY ACTIVE N-(HALOPROPYL) AMINO ACID DERIVATIVE 有权
标题翻译：制备光学活性N-（羟基丙酸）氨基酸衍生物的方法
公开(公告)号：US20110190527A1
公开(公告)日：2011-08-04
申请号：US12671565
申请日：2008-05-19
申请人： Jun Matsumoto , Toru Inoue
发明人： Jun Matsumoto , Toru Inoue
IPC分类号： C07C69/96 , C07C67/307 , C07C67/313 , C07C271/54
CPC分类号： C07B53/00 , C07B2200/07 , C07C229/12 , C07C233/83 , C07C271/22 , Y02P20/55
摘要： The present invention provides a method for producing an optically active N-(halopropyl)amino acid derivative, wherein the method comprises the steps of obtaining a compound represented by formula (III) by reacting an optically active alanine ester represented by formula (I) or a salt thereof (hereinafter sometimes simply referred to as an “alanine ester”) with a halogenated propane represented by formula (II); and obtaining an optically active N-(halopropyl)amino acid derivative represented by formula (IV) by introducing a protecting group onto the nitrogen atom of the compound represented by formula (III). The present invention provides a method for efficiently producing an optically active N-(halopropyl)amino acid derivative.
摘要翻译：本发明提供了一种光学活性N-（卤代丙基）氨基酸衍生物的制备方法，其中该方法包括以下步骤：通过使式（I）表示的光学活性丙氨酸酯或式其盐（以下有时简称为“丙氨酸酯”）与式（II）表示的卤代丙烷; 通过在式（III）表示的化合物的氮原子上引入保护基，得到由式（Ⅳ）表示的光学活性的N-（卤代丙基）氨基酸衍生物。本发明提供了有效制备光学活性N-（卤代丙基）氨基酸衍生物的方法。

72. 发明授权

US07989627B2 Optically active cyclic alcohol compound and method for preparing the same 有权
标题翻译：光学活性环状醇化合物及其制备方法
公开(公告)号：US07989627B2
公开(公告)日：2011-08-02
申请号：US12089170
申请日：2006-10-04
申请人： Masaki Okamoto , Akira Sakuragi , Yoshikazu Mori , Muneki Kishida
发明人： Masaki Okamoto , Akira Sakuragi , Yoshikazu Mori , Muneki Kishida
IPC分类号： C07D215/00 , C07D215/233
CPC分类号： C07D215/233 , B01J31/0252 , B01J31/146 , B01J31/1805 , B01J31/2295 , B01J2231/64 , B01J2231/643 , B01J2531/821 , C07B53/00 , C07D215/22 , C07D401/04 , Y02P20/55
摘要： The present invention relates to a method for preparing an optically active cyclic alcohol compound represented by general formula [I]: [wherein R represents a hydrogen atom or a protecting group for amino group, and * represents an astymmetric carbon atom.] which comprises a step of subjecting a cyclic ketone compound represented by general formula [II]: [wherein R has the same meaning as defined above.]to asymmetric reduction (A) in the presence of an optically active oxazaborolidine compound and a boron hydride compound, or (B) in the presence of an asymmetric transition metal complex obtained from a transition metal compound and an asymmetric ligand and a hydrogen donor, and relates to said compound.
摘要翻译：本发明涉及一种由通式[I]表示的光学活性环状醇化合物的制备方法：[其中R表示氢原子或氨基保护基，*表示非对称碳原子]，其包含在光学活性的恶唑硼烷化合物和硼氢化合物的存在下，将不饱和还原（A）进行不饱和还原（A）的步骤：（其中R具有与上述定义相同的含义） B）在由过渡金属化合物和不对称配体和氢供体获得的不对称过渡金属络合物的存在下，涉及所述化合物。

73. 发明申请

US20110172431A1 PROCESS FOR PRODUCING 1-SUBSTITUTED TRANS-4-(SUBSTITUTED AMINO) PIPERIDIN-3-OL 审中-公开
标题翻译：生产1-取代的反式-4-（取代的氨基）哌啶-3-醇的方法
公开(公告)号：US20110172431A1
公开(公告)日：2011-07-14
申请号：US13119852
申请日：2009-09-25
申请人： Toshiaki Aikawa , Osamu Tokuda , Tetsuya Ikemoto
发明人： Toshiaki Aikawa , Osamu Tokuda , Tetsuya Ikemoto
IPC分类号： C07D211/58 , C07D401/04
CPC分类号： C07D211/58 , C07B53/00
摘要： A process is provided for producing a 1-substituted trans-4-(substituted amino)piperidin-3-ol represented by formula (III-1): The process includes a step of reacting a 1-substituted-3,4-epoxypiperidine represented by formula (I): with an amine compound represented by formula (II) in the presence of an inorganic lithium salt. By utilizing the process, trans-4-aminopiperidin-3-ol compounds useful as various chemical products, such as medicine intermediates, can be produced.
摘要翻译：提供了制备由式（III-1）表示的1-取代的反式-4-（取代的氨基）哌啶-3-醇的方法：该方法包括使1-取代-3,4-环氧哌啶代表的通过式（I）表示：在无机锂盐存在下用式（II）表示的胺化合物。通过利用该方法，可以生产用作各种化学产品的反式-4-氨基哌啶-3-醇化合物，如医药中间体。

74. 发明申请

US20110166357A1 METHOD FOR PRODUCING N-SUBSTITUTED-TRANS-4-AZIDOPIPERIDINE-3-OL 审中-公开
标题翻译：用于生产N-取代的四氮杂多哌啶-3-醇的方法
公开(公告)号：US20110166357A1
公开(公告)日：2011-07-07
申请号：US13062967
申请日：2009-09-02
申请人： Osamu Tokuda , Toshiaki Aikawa , Tetsuya Ikemoto
发明人： Osamu Tokuda , Toshiaki Aikawa , Tetsuya Ikemoto
IPC分类号： C07D211/98
CPC分类号： C07D211/58 , C07B53/00 , C07D491/04
摘要： An N-substituted-trans-4-azidopiperidin-3-ol represented by formula (II-1) R1 is as defined below, which is useful as a pharmaceutical intermediate and so on, is produced by reacting an N-substituted-3,4-epoxypiperidine represented by formula (I): wherein R1 represents an aralkyl group having 7 to 24 carbon atoms or an alkyl group having 1 to 12 carbon atoms, with sodium azide in the presence of an inorganic lithium salt.
摘要翻译：由式（II-1）表示的N-取代的反式-4-叠氮基-3-哌啶-3-醇如下所定义，其可用作药物中间体等，其通过使N-取代的-3，由式（I）表示的4-环氧哌啶：其中R 1表示具有7至24个碳原子的芳烷基或具有1至12个碳原子的烷基，在无机锂盐存在下与叠氮化钠反应。

75. 发明申请

US20110166354A1 METHOD FOR PRODUCING OPTICALLY ACTIVE AMINO ACID DERIVATIVE 有权
标题翻译：生产光学活性氨基酸衍生物的方法
公开(公告)号：US20110166354A1
公开(公告)日：2011-07-07
申请号：US12993661
申请日：2009-06-02
申请人： Shohei Yamamoto , Akio Fujii , Masaru Mitsuda
发明人： Shohei Yamamoto , Akio Fujii , Masaru Mitsuda
IPC分类号： C07C227/08 , C07D207/06 , C07D495/04 , C07D401/12 , C07D211/60
CPC分类号： C07B51/00 , C07B53/00 , C07C227/18 , C07C229/08 , C07C229/28 , C07C2601/02 , C07D207/12 , C07D211/60 , C07D295/18 , C07D403/12 , C07D495/04
摘要： The present application relates to a method for producing an optically active α-amino acid derivative, comprising steps of reacting an α-haloester derivative represented by the general formula (1): of which alcohol part of the ester group is an optically active alcohol derivative, with an amine compound; then deprotecting the obtained compound; further carrying out an ester exchange reaction. According to the present invention method, it is possible to easily produce an optically active α-amino acid ester derivative which is useful as an intermediate for drugs with high selectivity.
摘要翻译：本申请涉及一种光学活性α-氨基酸衍生物的制造方法，包括使由通式（1）表示的α-卤代酯衍生物：酯基的醇部分为光学活性醇衍生物，与胺化合物; 然后使所得化合物脱保护; 进一步进行酯交换反应。根据本发明的方法，可以容易地制备可用作高选择性药物的中间体的光学活性α-氨基酸酯衍生物。

76. 发明授权

US07964743B2 Catalyst for asymmetric synthesis, ligand for use therein, and process for producing optically active compound through asymmetric synthesis reaction using them 有权
标题翻译：用于不对称合成的催化剂，其中使用的配体，以及通过使用它们的不对称合成反应制备光学活性化合物的方法
公开(公告)号：US07964743B2
公开(公告)日：2011-06-21
申请号：US11884537
申请日：2006-02-17
申请人： Norio Miyaura , Yasunori Yamamoto
发明人： Norio Miyaura , Yasunori Yamamoto
IPC分类号： C07F15/00 , C07F9/00
CPC分类号： C07B53/00 , B01J31/185 , B01J31/186 , B01J2231/344 , B01J2231/348 , B01J2231/44 , B01J2531/0266 , B01J2531/821 , B01J2531/822 , B01J2531/827 , C07B2200/07 , C07C29/38 , C07C45/69 , C07C67/343 , C07C209/16 , C07C231/12 , C07F9/657154 , C07F15/0066 , C07F15/0073 , C07F15/008 , C07C69/618 , C07C211/28 , C07C233/11 , C07C33/34
摘要： Compounds represented by the following general formula (1a) or (1b). A complex comprising a center metal of rhodium and a compound represented by the following general formula (1a) or (1b) as a ligand. A catalyst for optically active beta-substituted carbonyl compound synthesis and catalyst for asymmetric 1, 2 addition reaction being composed of the complex. A method of production of an optically active beta-aryl compound from an alpha, beta-unsaturated compound and an aryl-boronic acid derivative and method of production of an optically active aryl alcohol compound from an aldehyde compound and aryl boronic acid derivatives using the catalyst. A complex comprising a center metal of palladium and a compound represented by the following general formula (1a) or (1b) as a ligand. A catalyst for asymmetric allylic substitution reaction being composed of the complex. A method of production of an optically active dialkyl (1,3-disubstituted propeny)malonate compound from a 1,3-disubstituted ally acetate compound and a dialkyl malonate and method of production of an optically active allylamine compound from a 1,3-disubstituted ally acetate compound and an amine compound. The compounds have not only the versatility of being usable in the synthesis of wide-ranging optically active aryl compounds but also the selectivity and reactivity permitting synthesis with high yield within a short period of time under industrially advantageous mild conditions.
摘要翻译：由以下通式（1a）或（1b）表示的化合物。包含铑的中心金属和由以下通式（1a）或（1b）表示的化合物作为配体的络合物。用于光学活性β-取代羰基化合物合成的催化剂和由络合物组成的不对称1,2加成反应的催化剂。从α，β-不饱和化合物和芳基硼酸衍生物制备光学活性β-芳基化合物的方法和使用催化剂从醛化合物和芳基硼酸衍生物制备光学活性芳基醇化合物的方法。包含钯的中心金属和由以下通式（1a）或（1b）表示的化合物作为配体的络合物。不对称烯丙基取代反应的催化剂由络合物组成。从1,3-二取代的烯丙基乙酸酯化合物和丙二酸二烷基酯生产光学活性的二烷基（1,3-二取代的丙烯醛）丙二酸酯化合物的方法和由1,3-二取代的烯丙基化合物烯丙酸酯化合物和胺化合物。该化合物不仅具有广泛的光学活性芳基化合物合成中的多功能性，而且在工业上有利的温和条件下，在短时间内能够以高收率合成的选择性和反应性。

77. 发明申请

US20110137046A1 PREPARATION METHOD OF (4S,5R)-SEMIESTER 审中-公开
标题翻译：（4S，5R）-SEMIESTER的制备方法
公开(公告)号：US20110137046A1
公开(公告)日：2011-06-09
申请号：US12996078
申请日：2009-06-05
申请人： Fen-Er Chen , Fei Xiong , Xu-Xiang Chen , Lei Zhao , Zhong-Hua Wang
发明人： Fen-Er Chen , Fei Xiong , Xu-Xiang Chen , Lei Zhao , Zhong-Hua Wang
IPC分类号： C07D233/02
CPC分类号： C07D233/34 , C07B53/00
摘要： A preparation method of (4S,5R)-semiester in which cycloanhydride conducts enantioselective ring-opening with alcohol in the presence of 9-epiquininurea. With this method, (4S,5R)-semiester is prepared at room temperature with high yield and high stereoselectivity.
摘要翻译：（4S，5R） - 酯的制备方法，其中环酸酐在9-表氯脲存在下与醇进行对映选择性开环。使用该方法，在室温下以高产率和高立体选择性制备（4S，5R） - 酯。

78. 发明申请

US20110118500A1 METHOD FOR PRODUCING OPTICALLY ACTIVE a-IONONE 有权
标题翻译：用于生产光学活性α-离子的方法
公开(公告)号：US20110118500A1
公开(公告)日：2011-05-19
申请号：US13012199
申请日：2011-01-24
申请人： Tetsuya Yamamoto , Kenji Yagi , Kenya Ishida
发明人： Tetsuya Yamamoto , Kenji Yagi , Kenya Ishida
IPC分类号： C07C69/78 , C07C69/533 , C07C69/63 , C07C69/24 , C07C69/708
CPC分类号： C12P7/26 , A23L2/56 , A23L27/204 , A61K8/37 , A61Q11/00 , A61Q13/00 , C07B53/00 , C07B2200/07 , C07C403/08 , C07C403/12 , C07C403/14 , C07C2601/16 , C12G3/06 , C12P41/004
摘要： Provided that a method for inexpensively producing optically active α-ionone with a high yield and a high asymmetric yield and with good workability in a short process, and a perfume composition comprising the optically active α-ionone obtained by the aforementioned method. A method for producing optically active α-ionone, comprising allowing α-ionone as a mixture of optical isomers to react with an esterification agent, and hydrolyzing the obtained α-ionone enol ester; a method for producing optically active α-ionone comprising subjecting α-ionone as a mixture of optical isomers to an asymmetric reduction, allowing the obtained optically active α-ionol to react with an esterification agent to give an optically active α-ionol ester, hydrolyzing the obtained optically active α-ionol ester after purification as necessary, and then oxidizing the obtained optically active α-ionol; and a perfume composition comprising thus obtained optically active α-ionone.
摘要翻译：本发明提供了一种低成本地生产光学活性α-紫罗兰酮的方法，其具有高产率和高不对称产率，并且在短时间内具有良好的可加工性，以及包含通过上述方法获得的光学活性α-紫罗兰酮的香料组合物。一种光学活性α-紫罗兰酮的制造方法，其特征在于，使作为旋光异构体的混合物的α-紫罗烯酮与酯化反应，水解得到的α-紫罗烯酮烯醇酯; 一种光学活性α-紫罗兰酮的制造方法，其特征在于，将α-紫罗烯酮作为光学异构体的混合物进行不对称还原，使得所得光学活性α-离子酚与酯化反应，得到光学活性α-离子醇酯，水解根据需要纯化后得到的光学活性α-离子醇酯，然后氧化所得光学活性α-离子醇; 和包含这样得到的光学活性α-紫罗兰酮的香料组合物。

79. 发明授权

US07928257B2 Method for producing optically active aziridine compounds and amine compounds as well as complexes and their intermediates used in this method 失效
标题翻译：光学活性氮丙啶化合物和胺化合物的制备方法以及该方法中使用的络合物及其中间体
公开(公告)号：US07928257B2
公开(公告)日：2011-04-19
申请号：US12654824
申请日：2010-01-05
申请人： Tsutomu Katsuki , Kazufumi Omura , Tatsuya Uchida , Ryo Irie
发明人： Tsutomu Katsuki , Kazufumi Omura , Tatsuya Uchida , Ryo Irie
IPC分类号： C07F15/00 , C07C211/09
CPC分类号： C07C43/30 , C07B53/00 , C07C45/00 , C07C45/673 , C07C47/57 , C07C47/575 , C07C251/24 , C07C303/36 , C07C2601/10 , C07C2602/08 , C07D203/24 , C07D203/26 , C07F15/0053 , C07C311/20
摘要： This invention provides a method for producing an optically active aziridine compound or amine compound, which uses as a catalyst a Ru(salen)(CO) complex represented by the following formula (I) or its enantiomer having a high stability, in a high turnover number (TON) and a high enantioselectivity. In the formula (I), Ar is represented by the following formula (VI) or (VII), wherein in the formula (VI), Xs are independently a halogen or a halogenated alkyl group and R1 and R2s are independently hydrogen or an alkyl group or a trialkylsilyl group having a carbon number of 1-4, and in the formula (VII), R3 is a bulky group.
摘要翻译：本发明提供了一种制备光学活性氮丙啶化合物或胺化合物的方法，其用作催化剂，由下式（I）表示的Ru（salen）（CO）络合物或其具有高稳定性的对映异构体，其成交量高数（TON）和高对映选择性。在式（I）中，Ar由下式（VI）或（VII）表示，其中在式（VI）中，Xs独立地为卤素或卤代烷基，R 1和R 2独立地为氢或烷基或碳数为1-4的三烷基甲硅烷基，在式（VII）中，R 3为大体积基团。

80. 发明授权

US07906667B2 Method for producing optically active alcohol compound 失效
标题翻译：光学活性醇化合物的制造方法
公开(公告)号：US07906667B2
公开(公告)日：2011-03-15
申请号：US12161695
申请日：2007-01-31
申请人： Kazuaki Sasaki
发明人： Kazuaki Sasaki
IPC分类号： C09B45/00 , C07C37/00
CPC分类号： C07C41/03 , B01J31/2243 , B01J2231/485 , B01J2531/0252 , B01J2531/22 , B01J2531/62 , B01J2531/845 , C07B53/00 , C07B2200/07 , C07C251/24 , C07C43/23 , C07C43/295
摘要： A method for producing an optically active alcohol compound comprising reacting a cyclic ether compound with a phenol compound in the presence of an asymmetric complex obtained by reacting an optically active metal complex represented by the formula (1): wherein R1, R2, R3, R4, R5, R6, R7 and R8 are the same or different and each independently represent a hydrogen atom, an alkyl group or the like; one of R9 and R10 is a hydrogen group and the other is a substituted or unsubstituted phenyl group or the like; Q represents a single bond, a C1-C4 alkylene group or the like; M represents a metal ion; and when an ionic valency of the metal ion is same as a coordination number of a ligand, A is nonexistent, and when the above-mentioned ionic valency is different from the coordination number, and A represents a counter ion or a ligand, with a metal sulfonate.
摘要翻译：一种制备光学活性醇化合物的方法，包括使环醚化合物与酚化合物在通式（1）表示的光学活性金属络合物反应得到的不对称络合物的存在下反应：其中R1，R2，R3，R4 R5，R6，R7和R8相同或不同，各自独立地表示氢原子，烷基等; R9和R10中的一个是氢基团，另一个是取代或未取代的苯基基团等; Q表示单键，C1-C4亚烷基等; M表示金属离子; 当金属离子的离子价与配位体的配位数相同时，A不存在，当上述离子价与配位数不同时，A表示抗衡离子或配体，金属磺酸盐。

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