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1. 发明申请

US20110021780A1 MANUFACTURING METHOD FOR A PIPERIDINE-3-YLCARBAMATE COMPOUND AND OPTICAL RESOLUTION METHOD THEREFOR 审中-公开
标题翻译：哌啶-3-甲酸酯化合物的制备方法及其分解方法
公开(公告)号：US20110021780A1
公开(公告)日：2011-01-27
申请号：US12922706
申请日：2009-03-18
申请人： Yosuke Watanabe , Junichi Yasuoka , Tetsuya Ikemoto
发明人： Yosuke Watanabe , Junichi Yasuoka , Tetsuya Ikemoto
IPC分类号： C07D211/02 , C07D211/98
CPC分类号： C07D211/56 , B01J21/18 , B01J23/44 , C07B57/00 , C07D213/75
摘要： Provided is a manufacturing method for a piperidine-3-ylcarbamate compound in which a pyridine-3-ylcarbamate compound and hydrogen are brought into contact in the presence of a palladium catalyst.
摘要翻译：本发明提供了在钯催化剂存在下使吡啶-3-基氨基甲酸酯化合物与氢接触的哌啶-3-基氨基甲酸酯化合物的制造方法。

2. 发明申请

US20100331546A1 METHOD FOR OPTICAL RESOLUTION OF ALKYL PIPERIDIN-3-YL CARBAMATE AND INTERMEDIATE THEREFOR 审中-公开
标题翻译：烷基哌啶-3-基碳酸酯及其中间体的光学解析方法
公开(公告)号：US20100331546A1
公开(公告)日：2010-12-30
申请号：US12866506
申请日：2009-02-17
申请人： Yosuke Watanabe , Junichi Yasuoka , Tetsuya Ikemoto
发明人： Yosuke Watanabe , Junichi Yasuoka , Tetsuya Ikemoto
IPC分类号： C07D211/58
CPC分类号： C07D211/56 , C07B57/00 , C07C59/255
摘要： Disclosed is a method for optical resolution of an alkylpiperidin-3-yl carbamate, the method including bringing an RS mixture of an alkylpiperidin-3-yl carbamate into contact with an optically active tartaric acid in the presence of a solvent.
摘要翻译：公开了一种用于光学拆分烷基哌啶-3-基氨基甲酸酯的方法，该方法包括使烷基哌啶-3-基氨基甲酸酯的RS混合物与光学活性酒石酸在溶剂存在下接触。

3. 发明授权

US08742162B2 Method for producing optically active 1-amino-2-vinylcyclopropanecarboxylic acid ester 失效
标题翻译：光学活性1-氨基-2-乙烯基环丙烷羧酸酯的制备方法
公开(公告)号：US08742162B2
公开(公告)日：2014-06-03
申请号：US13388575
申请日：2010-08-05
申请人： Toshiaki Aikawa , Junichi Yasuoka , Tetsuya Ikemoto
发明人： Toshiaki Aikawa , Junichi Yasuoka , Tetsuya Ikemoto
IPC分类号： C07C67/30 , C07C67/317 , C07C69/743 , C07C69/747 , C07C67/48 , C07C67/62
CPC分类号： C07B53/00 , C07C227/32
摘要： 1-Amino-2-vinylcyclopropanecarboxylic acid ester, which is useful as a synthetic intermediate of pharmaceuticals, can be produced by a process of producing 1-amino-2-vinylcyclopropanecarboxylic acid ester represented by formula (4): including a step of hydrolysis of an optically active 1-N-(arylmethylene)amino-2-vinylcyclopropanecarboxylic acid ester represented by formula (3): which is obtained by reacting an N-(arylmethylene)glycine ester represented by formula (1): with a compound represented by formula (2): in the presence of a base and an optically active quaternary ammonium salt.
摘要翻译：可用作药物的合成中间体的1-氨基-2-乙烯基环丙烷羧酸酯可以通过制备由式（4）表示的1-氨基-2-乙烯基环丙烷羧酸酯的方法制备：包括水解由式（3）表示的光学活性的1-N-（芳基亚甲基）氨基-2-乙烯基环丙烷羧酸酯：其由式（1）表示的N-（芳基亚甲基）甘氨酸酯与式（2）：在碱和光学活性季铵盐的存在下。

4. 发明申请

US20120130116A1 METHOD FOR PRODUCING OPTICALLY ACTIVE 1-AMINO-2-VINYLCYCLOPROPANECARBOXYLIC ACID ESTER 失效
标题翻译：生产光学活性1-氨基-2-乙烯基环戊烷羧酸酯的方法
公开(公告)号：US20120130116A1
公开(公告)日：2012-05-24
申请号：US13388575
申请日：2010-08-05
申请人： Toshiaki Aikawa , Junichi Yasuoka , Tetsuya Ikemoto
发明人： Toshiaki Aikawa , Junichi Yasuoka , Tetsuya Ikemoto
IPC分类号： C07C229/48 , C07C227/16
CPC分类号： C07B53/00 , C07C227/32
摘要： 1-Amino-2-vinylcyclopropanecarboxylic acid ester, which is useful as a synthetic intermediate of pharmaceuticals, can be produced by a process of producing 1-amino-2-vinylcyclopropanecarboxylic acid ester represented by formula (4): including a step of hydrolysis of an optically active 1-N-(arylmethylene)amino-2-vinylcyclopropanecarboxylic acid ester represented by formula (3): which is obtained by reacting an N-(arylmethylene)glycine ester represented by formula (1): with a compound represented by formula (2): in the presence of a base and an optically active quaternary ammonium salt.
摘要翻译：可用作药物的合成中间体的1-氨基-2-乙烯基环丙烷羧酸酯可以通过制备由式（4）表示的1-氨基-2-乙烯基环丙烷羧酸酯的方法制备：包括水解由式（3）表示的光学活性的1-N-（芳基亚甲基）氨基-2-乙烯基环丙烷羧酸酯：通过使由式（1）表示的N-（芳基亚甲基）甘氨酸酯与式（2）：在碱和光学活性季铵盐的存在下。

5. 发明授权

US08293926B2 Method of producing optically active 4-amino-3-substituted phenylbutanoic acid 有权
标题翻译：光学活性4-氨基-3-取代苯基丁酸的制备方法
公开(公告)号：US08293926B2
公开(公告)日：2012-10-23
申请号：US12086056
申请日：2006-12-08
申请人： Junichi Yasuoka , Shoji Fukuyo , Tetsuya Ikemoto
发明人： Junichi Yasuoka , Shoji Fukuyo , Tetsuya Ikemoto
IPC分类号： C07D207/273 , C07C229/34
CPC分类号： C07C205/53 , C07B53/00 , C07B2200/07 , C07C229/34 , C07D207/26 , C07D207/277
摘要： The present invention provides a method of producing a compound (IIa) or a compound (IIb), provides a method of producing a compound (IIIa) or a compound (IIIb), provides a method of producing a compound (Va) or its salt or a compound (Vb) or its salt, provides a method of producing a compound (IIIa) or a compound (IIIb), further, provides a method of producing a compound (Va) or its salt or a compound (Vb) or its salt including these production methods.
摘要翻译：本发明提供化合物（IIa）或化合物（IIb）的制造方法，提供化合物（IIIa）或化合物（IIIb）的制造方法，提供化合物（Va）或其盐或化合物（Vb）或其盐，提供化合物（IIIa）或化合物（IIIb）的制造方法，进一步提供化合物（Va）或其盐或化合物（Vb）或其化合物盐包括这些生产方法。

6. 发明申请

US20090137819A1 Method of Producing Optically Active 4-Amino-3-Substituted Phenylbutanoic Acid 有权
标题翻译：生产光学活性4-氨基-3-取代苯基丁酸的方法
公开(公告)号：US20090137819A1
公开(公告)日：2009-05-28
申请号：US12086056
申请日：2006-12-08
申请人： Junichi Yasuoka , Shoji Fukuyo , Tetsuya Ikemoto
发明人： Junichi Yasuoka , Shoji Fukuyo , Tetsuya Ikemoto
IPC分类号： C07D207/12 , C07C69/612
CPC分类号： C07C205/53 , C07B53/00 , C07B2200/07 , C07C229/34 , C07D207/26 , C07D207/277
摘要： The present invention provides a method of producing a compound (IIa) or a compound (IIb), provides a method of producing a compound (IIIa) or a compound (IIIb), provides a method of producing a compound (Va) or its salt or a compound (Vb) or its salt, provides a method of producing a compound (IIIa) or a compound (IIIb), further, provides a method of producing a compound (Va) or its salt or a compound (Vb) or its salt including these production methods.
摘要翻译：本发明提供化合物（IIa）或化合物（IIb）的制造方法，提供化合物（IIIa）或化合物（IIIb）的制造方法，提供化合物（Va）或其盐或化合物（Vb）或其盐，提供化合物（IIIa）或化合物（IIIb）的制造方法，进一步提供化合物（Va）或其盐或化合物（Vb）或其化合物盐包括这些生产方法。

7. 发明申请

US20090176999A1 Process for producing hexahydrofurofuranol derivative 有权
标题翻译：六氢呋喃醇衍生物的制备方法
公开(公告)号：US20090176999A1
公开(公告)日：2009-07-09
申请号：US11920774
申请日：2006-06-05
申请人： Tetsuya Ikemoto , Yosuke Watanabe
发明人： Tetsuya Ikemoto , Yosuke Watanabe
IPC分类号： C07D493/04 , C07C31/18
CPC分类号： C07B53/00 , C07C45/30 , C07C45/72 , C07C47/198 , C07D493/04 , Y02P20/55 , C07C47/277
摘要： The present invention provides; a process for producing a compound (IV) comprising a step of reacting a compound (I) with a compound (II) in the presence of an optionally substituted cyclic secondary amine to obtain a compound (III) and a step of sequentially or simultaneously eliminating R1 and R2 from the compound (III), and then cyclizing the R1- and R2-eliminated compound to obtain the compound represented by the formula (IV); a process for producing a high purity compound (IV); an intermediate thereof; and a process for producing an intermediate.
摘要翻译：本发明提供：一种制备化合物（Ⅳ）的方法，包括在任意取代的环状仲胺存在下，使化合物（Ⅰ）与化合物（Ⅱ）反应得到化合物（Ⅲ）和顺序或同时除去的步骤 R1和R2，然后使R 1和R 2消去的化合物环化，得到由式（IV）表示的化合物; 一种生产高纯度化合物（Ⅳ）的方法; 其中间体; 和中间体的制造方法。

8. 发明授权

US07951977B2 Process for producing hexahydrofurofuranol derivative 有权
标题翻译：六氢呋喃醇衍生物的制备方法
公开(公告)号：US07951977B2
公开(公告)日：2011-05-31
申请号：US11920774
申请日：2006-06-05
申请人： Tetsuya Ikemoto , Yosuke Watanabe
发明人： Tetsuya Ikemoto , Yosuke Watanabe
IPC分类号： C07C47/00 , C07C31/18 , C07D493/04
CPC分类号： C07B53/00 , C07C45/30 , C07C45/72 , C07C47/198 , C07D493/04 , Y02P20/55 , C07C47/277
摘要： The present invention provides; a process for producing a compound (IV) comprising a step of reacting a compound (I) with a compound (II) in the presence of an optionally substituted cyclic secondary amine to obtain a compound (III) and a step of sequentially or simultaneously eliminating R1 and R2 from the compound (III), and then cyclizing the R1- and R2-eliminated compound to obtain the compound represented by the formula (IV); a process for producing a high purity compound (IV); an intermediate thereof; and a process for producing an intermediate.
摘要翻译：本发明提供：一种制备化合物（Ⅳ）的方法，包括在任意取代的环状仲胺存在下，使化合物（Ⅰ）与化合物（Ⅱ）反应得到化合物（Ⅲ）和顺序或同时除去的步骤 R1和R2，然后使R 1和R 2消去的化合物环化，得到由式（IV）表示的化合物; 一种生产高纯度化合物（Ⅳ）的方法; 其中间体; 和中间体的制造方法。

9. 发明授权

US07605286B2 Hydroxy-protecting reagent and method of protecting hydroxy with the same 失效
标题翻译：羟基保护试剂和保护羟基的方法
公开(公告)号：US07605286B2
公开(公告)日：2009-10-20
申请号：US10567150
申请日：2004-06-23
申请人： Tetsuya Ikemoto , Yosuke Watanabe
发明人： Tetsuya Ikemoto , Yosuke Watanabe
IPC分类号： C07C69/66 , C07C43/20
CPC分类号： C07B41/04 , C07D307/32 , Y02P20/55
摘要： The present invention relates to a method of protecting a hydroxyl group, which includes reacting a hydroxyl group-containing compound with a compound represented by the formula (I): wherein R is a phenyl group optionally having substituent(s), an alkyl group optionally having substituent(s) or a benzyl group optionally having substituent(s), and X is a halogen atom, in the presence of an acid catalyst to substitute the hydrogen atom of the hydroxyl group of the hydroxyl group-containing compound with a protecting group represented by the formula (II): wherein R is as defined above. The present invention provides a method capable of introducing an acetal type protecting group into a hydroxyl group under mild conditions, and a protecting reagent therefor and a method of producing the protecting reagent.
摘要翻译：本发明涉及保护羟基的方法，其包括使含羟基的化合物与式（I）表示的化合物反应：其中R是任选具有取代基的苯基，任选地具有取代基的烷基具有取代基或任选具有取代基的苄基，X是卤素原子，在酸催化剂存在下，用保护基取代含羟基化合物的羟基的氢原子由式（II）表示：其中R如上所定义。本发明提供能够在温和条件下将缩醛型保护基引入羟基的方法及其保护试剂，以及制备保护试剂的方法。

10. 发明授权

US07700642B2 Process for producing an aromatic unsaturated compound 失效
标题翻译：芳族不饱和化合物的制造方法
公开(公告)号：US07700642B2
公开(公告)日：2010-04-20
申请号：US10569486
申请日：2004-08-25
申请人： Weiqi Wang , Tetsuya Ikemoto
发明人： Weiqi Wang , Tetsuya Ikemoto
IPC分类号： A61K31/404 , C07D209/04 , C07D209/18
CPC分类号： C07D209/24 , C07B37/04 , C07C67/343 , C07D209/08 , C07D209/10 , C07D209/12 , C07D209/18 , C07C69/734
摘要： The present invention provides a process for producing an aromatic unsaturated compound of the formula (4) wherein Ar represents an optionally substituted aromatic group or an optionally substituted heteroaromatic group, and Y represents an electron withdrawing group, which comprises reacting (a) a compound of the formula (1) Ar—H (1) wherein Ar has the same meaning as defined above with (b) a compound of the formula (2) wherein Y has the same meaning as defined above, and Z represents a lower alkoxy, or a compound of the formula (3) wherein Y and Z have the same meanings as defined above, in the presence of (c) an acid or a compound which generates a mineral acid by its hydrolysis.
摘要翻译：本发明提供一种制备式（4）的芳族不饱和化合物的方法，其中Ar表示任选取代的芳族基团或任选取代的杂芳基，Y表示吸电子基团，其包括使（a）式（1）Ar-H（1）其中Ar具有与上述定义相同的含义（b）式（2）的化合物，其中Y具有与上述相同的含义，Z表示低级烷氧基，或在（c）酸或通过其水解生成无机酸的化合物的存在下，式（3）的化合物，其中Y和Z具有与上述相同的含义。

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