公开(公告)号：US07629472B2

公开(公告)日：2009-12-08

申请号：US11812052

申请日：2007-06-14

申请人： Toru Yamano ,  Naohiro Taya ,  Akio Ojida

发明人： Toru Yamano ,  Naohiro Taya ,  Akio Ojida

IPC分类号： C07D233/54 ,  C07D211/80

CPC分类号： C07D233/64 ,  C07D213/55

摘要： The present invention provides a method for producing an optically active β-hydroxy ester compound represented by the general formula: wherein R1 represents an optionally substituted hydrocarbon group and the like, R2 represents a nitrogen-containing heterocyclic group different from R1, which is represented by the general formula: wherein the ring may be substituted and the like, R3 represents an optionally substituted hydrocarbon group and the like, R4 and R5 represent, the same or different, a hydrogen atom, a halogen atom and the like, the symbol “*” represents an optically active center, which comprises reacting in the presence of a cinchona alkaloid and the like a compound represented by the general formula: wherein R1 and R2 are as defined above with a compound represented by the general formula: wherein R3, R4 and R5 are as defined above, and X is a halogen atom.

摘要翻译： 本发明提供一种制备由以下通式表示的光学活性β-羟基酯化合物的方法：其中R 1表示任选取代的烃基等，R 2表示与R 1不同的含氮杂环基，其表示为 通式：其中环可以被取代等，R 3表示任选取代的烃基等，R 4和R 5表示相同或不同的氢原子，卤素原子等，符号“* “表示光学活性中心，其包括在cinchona生物碱等存在下反应，由通式表示的化合物：其中R 1和R 2如上所定义，与通式表示的化合物反应：其中R 3，R 4和 R5如上所定义，X为卤素原子。

公开(公告)号：US5247095A

公开(公告)日：1993-09-21

申请号：US935105

申请日：1992-08-27

申请人： Toru Yamano ,  Kazuo Nakahama ,  Kunio Takanohashi

发明人： Toru Yamano ,  Kazuo Nakahama ,  Kunio Takanohashi

IPC分类号： C07D495/04 ,  C12P17/18 ,  C12P41/00

CPC分类号： C07D495/04 ,  C12P17/18 ,  C12P41/004

摘要： There are disclosed a compound of the general formula (I): ##STR1## wherein the group R--CO-- is an acyl group and its production. There is also disclosed a process for producing optically active (.+-.)-(3a.alpha., 4.alpha., 6a.alpha.)-tetrahydro-4-acetoxy-1,3-dibenzyl-1H-thieno[3,4-d]imidazol-2(3H)-one by using the compound (I). The compound (I) can be used as an intermediate for producing D-biotin which is useful as medicaments and feed additives for animals.

公开(公告)号：US4845246A

公开(公告)日：1989-07-04

申请号：US205094

申请日：1988-06-10

申请人： Kunio Takanohashi ,  Mitsutaka Tanaka ,  Toru Yamano

发明人： Kunio Takanohashi ,  Mitsutaka Tanaka ,  Toru Yamano

IPC分类号： C07H7/06

CPC分类号： C07H7/06

摘要： 6-O-(2-keto-L-gulonoyl)-L-ascorbate substantially free from 2-keto-L-gulonic acid is produced by allowing an acid to act on 2-keto-L-gulonic acid in an inert organic solvent and recovering 6-O-(2-keto-L-gulonoyl)-L-ascorbate from the reaction mixture.6-O-(2-keto-L-gulonoyl)-L-ascorbate is more fat-soluble than L-ascorbic acid and is expected of the use as a prodrug for L-ascorbic acid that can be absorbed from the intestinal tract.

公开(公告)号：US4794182A

公开(公告)日：1988-12-27

申请号：US073697

申请日：1987-07-14

申请人： Kunio Takanohashi ,  Toru Yamano ,  Mitsutaka Tanaka

发明人： Kunio Takanohashi ,  Toru Yamano ,  Mitsutaka Tanaka

IPC分类号： C07D239/42

CPC分类号： C07D239/42

摘要： A novel 2-lower alkyl-4-amino-5-substituted iminopyrimidine compound represented by the formula: ##STR1## wherein R is a lower alkyl, and Y is hydroxyl or amino which may be protected or a salt thereof is obtainable by allowing a formylpyrimidine compound represented by the formula: ##STR2## wherein R is a lower alkyl to react with a compound represented by the formula H.sub.2 N--Y, wherein Y is hydroxyl or amino which may be protected, or a salts thereof. The iminopyrimidine compound gives the known pyrimidine compound represented by the formula: ##STR3## wherein R is as defined above in high yield. Therefor, the process is very useful as an industrial production method.

摘要翻译： 由下式表示的新型2-低级烷基-4-氨基-5-取代的亚氨基嘧啶化合物：其中R为低级烷基，Y为可被保护的羟基或氨基或其盐可通过使 由下式表示的甲酰嘧啶化合物：其中R是与式H2N-Y表示的化合物反应的低级烷基，其中Y是可被保护的羟基或氨基，或其盐。 亚氨基嘧啶化合物以高产率得到由下式表示的已知嘧啶化合物：其中R如上定义。 因此，该方法作为工业生产方法是非常有用的。

公开(公告)号：US20070276143A1

公开(公告)日：2007-11-29

申请号：US11812052

申请日：2007-06-14

申请人： Toru Yamano ,  Naohiro Taya ,  Akio Ojida

发明人： Toru Yamano ,  Naohiro Taya ,  Akio Ojida

IPC分类号： C07D233/54 ,  C07D211/80

CPC分类号： C07D233/64 ,  C07D213/55

摘要： The present invention provides a method for producing an optically active β-hydroxy ester compound represented by the general formula: wherein R1 represents an optionally substituted hydrocarbon group and the like, R2 represents a nitrogen-containing heterocyclic group different from R1, which is represented by the general formula: wherein the ring may be substituted and the like, R3 represents an optionally substituted hydrocarbon group and the like, R4 and R5 represent, the same or different, a hydrogen atom, a halogen atom and the like, the symbol “*” represents an optically active center, which comprises reacting in the presence of a cinchona alkaloid and the like a compound represented by the general formula: wherein R1 and R2are as defined above with a compound represented by the general formula: wherein R3, R4and R5 are as defined above, and X is a halogen atom.

摘要翻译： 本发明提供一种制备由以下通式表示的光学活性β-羟基酯化合物的方法：其中R 1表示任选取代的烃基等，R 2 O >表示不同于R 1的含氮杂环基，其由以下通式表示：其中该环可以被取代等，R 3表示任选地 取代烃基等，R 4和R 5表示相同或不同的氢原子，卤素原子等，符号“*”表示 光学活性中心，其包括在cinchona生物碱等存在下反应，由通式表示的化合物：其中R 1和R 2如上定义 与由下列通式表示的化合物：其中R 3，R 4和R 5如上定义，X​​是卤素 原子。

公开(公告)号：US07247732B2

公开(公告)日：2007-07-24

申请号：US11451051

申请日：2006-06-12

申请人： Toru Yamano ,  Naohiro Taya ,  Akio Ojida

发明人： Toru Yamano ,  Naohiro Taya ,  Akio Ojida

IPC分类号： C07D213/46 ,  C07D233/60

CPC分类号： C07D233/64 ,  C07D213/55

摘要： The present invention provides a method for producing an optically active β-hydroxy ester compound represented by the general formula: wherein R1 represents an optionally substituted hydrocarbon group and the like,R2 represents a nitrogen-containing heterocyclic group different from R1, which is represented by the general formula: wherein the ring may be substituted and the like, R3 represents an optionally substituted hydrocarbon group and the like,R4 and R5 represent, the same or different, a hydrogen atom, a halogen atom and the like,the symbol “*” represents an optically active center, which comprises reacting in the presence of a cinchona alkaloid and the like a compound represented by the general formula: wherein R1 and R2 are as defined above with a compound represented by the general formula: wherein R3, R4 and R5 are as defined above, and X is a halogen atom.

摘要翻译： 本发明提供一种制备由以下通式表示的光学活性β-羟基酯化合物的方法：其中R 1表示任选取代的烃基等，R 2 O >表示不同于R 1的含氮杂环基，其由以下通式表示：其中该环可以被取代等，R 3表示任选地 取代烃基等，R 4和R 5表示相同或不同的氢原子，卤素原子等，符号“*”表示 光学活性中心，其包括在cinchona生物碱等存在下反应，由以下通式表示的化合物：其中R 1和R 2如上定义 与下列通式表示的化合物：其中R 3，R 4和R 5如上所定义，X是卤代基 n原子。

公开(公告)号：US20060229457A1

公开(公告)日：2006-10-12

申请号：US11451051

申请日：2006-06-12

申请人： Toru Yamano ,  Naohiro Taya ,  Akio Ojida

发明人： Toru Yamano ,  Naohiro Taya ,  Akio Ojida

IPC分类号： C07D233/61

CPC分类号： C07D233/64 ,  C07D213/55

摘要： The present invention provides a method for producing an optically active β-hydroxy ester compound represented by the general formula: wherein R1 represents an optionally substituted hydrocarbon group and the like, R2 represents a nitrogen-containing heterocyclic group different from R1, which is represented by the general formula: wherein the ring may be substituted and the like, R3 represents an optionally substituted hydrocarbon group and the like, R4 and R5 represent, the same or different, a hydrogen atom, a halogen atom and the like, the symbol “*” represents an optically active center, which comprises reacting in the presence of a cinchona alkaloid and the like a compound represented by the general formula: wherein R1 and R2 are as defined above with a compound represented by the general formula: wherein R3, R4 and R5 are as defined above, and X is a halogen atom.

摘要翻译： 本发明提供一种制备由以下通式表示的光学活性β-羟基酯化合物的方法：其中R 1表示任选取代的烃基等，R 2 O >表示不同于R 1的含氮杂环基，其由以下通式表示：其中该环可以被取代等，R 3表示任选地 取代烃基等，R 4和R 5表示相同或不同的氢原子，卤素原子等，符号“*”表示 光学活性中心，其包括在cinchona生物碱等存在下反应，由通式表示的化合物：其中R 1和R 2如上定义 与下列通式表示的化合物：其中R 3，R 4和R 5如上所定义，X是卤代基 n原子。

公开(公告)号：US06800778B1

公开(公告)日：2004-10-05

申请号：US10111211

申请日：2002-04-22

申请人： Isao Aoki ,  Mari Adachi ,  Mitsuru Kawada ,  Toru Yamano ,  Naohiro Taya

发明人： Isao Aoki ,  Mari Adachi ,  Mitsuru Kawada ,  Toru Yamano ,  Naohiro Taya

IPC分类号： C07F906

CPC分类号： C07D233/64 ,  A61K31/4164 ,  C07B2200/07 ,  C07F9/5027 ,  C07F9/65744

摘要： The present invention provides a method of producing an optically active form of a compound represented by the formula (I) having a steroid C17,20-lyase inhibitory activity and is useful as an agent for the prophylaxis or treatment of prostatism, tumor such as breast cancer, and the like or a salt thereof, which method includes reacting a mixture of optically active compounds of a naphthalene derivative represented by the formula: wherein R is a nitrogen-containing heterocyclic group, R1 is a hydrogen atom, a hydrocarbon group or an aromatic heteromonocyclic group, R2 is a hydrogen atom or a lower alkyl group, * shows the position of an asymmetric carbon, R3, R4, R5, R6, R7, R8 and R9 are each independently a hydrogen atom, a hydrocarbon group, a hydroxy group, a thiol group, an amino group, a carbamoyl group, an acyl group or a halogen atom, and R7 is bonded with R6 or R8 to form, together with a carbon atom on a naphthalene ring, a 5 or 6-membered ring containing an oxygen atom, with an optically active form of a compound represented by the formula: wherein ring A is a benzene ring, R10 and R11 are the same or different and each is a hydrogen atom, a hydrocarbon group or a halogen atom, or R10 and R11 in combination show an alkylene group, * shows the position of an asymmetric carbon, and ring B and ring C are each an aromatic ring, separating the resulting salt, and isolating the optically active form, and a novel reagent for optical resolution.

摘要翻译： 本发明提供了具有类固醇C17,20-裂解酶抑制活性的由式​​（I）表示的化合物的光学活性形式的方法，可用作预防或治疗前列腺症，肿瘤如乳腺癌 癌症等或其盐，该方法包括使由下式表示的萘衍生物的光学活性化合物的混合物：其中R是含氮杂环基，R 1是氢原子，烃 基团或芳族杂单环基团，R 2是氢原子或低级烷基，*表示不对称碳的位置，R 3，R 4，R 5，R 6， R 7，R 8和R 9各自独立地为氢原子，烃基，羟基，硫醇基，氨基，氨基甲酰基，酰基或卤素原子，以及 R 7与R 6或R 8键合，与萘环上的碳原子一起形成5或6元环， 具有下式表示的化合物的光学活性形式的氧原子：其中环A是苯环，R 10和R 11相同或不同，各自为氢原子，烃基 或卤素原子，或R 10和R 11组合表示亚烷基，*表示不对称碳的位置，环B和环C各自为芳环，分离所得盐，并分离 光学活性形式和用于光学拆分的新型试剂。

公开(公告)号：US5637734A

公开(公告)日：1997-06-10

申请号：US553027

申请日：1995-11-03

申请人： Haruomi Honda ,  Toru Yamano ,  Masayuki Yamashita

发明人： Haruomi Honda ,  Toru Yamano ,  Masayuki Yamashita

IPC分类号： C07D307/62

CPC分类号： C07D307/62

摘要： A process for producing L-ascorbic acid, which comprises reacting 2-keto-L-gulonic acid with an acid in an ether or an inert organic solvent containing an ether in the presence of water and a surfactant.

摘要翻译： 一种生产L-抗坏血酸的方法，其包括在水和表面活性剂的存在下，使2-酮-L-古洛糖酸与乙酸或含有醚的惰性有机溶剂中的酸反应。

公开(公告)号：US07084278B2

公开(公告)日：2006-08-01

申请号：US10506309

申请日：2003-03-05

申请人： Toru Yamano ,  Naohiro Taya ,  Akio Ojida

发明人： Toru Yamano ,  Naohiro Taya ,  Akio Ojida

IPC分类号： C07D213/16 ,  C07D213/28 ,  C07D233/64

CPC分类号： C07D233/64 ,  C07D213/55

摘要： The present invention provides a method for producing an optically active β-hydroxy ester compound represented by the general formula: wherein R1 represents an optionally substituted hydrocarbon group and the like, R2 represents a nitrogen-containing heterocyclic group different from R1, which is represented by the general formula: wherein the ring may be substituted and the like, R3 represents an optionally substituted hydrocarbon group and the like, R4 and R5 represent, the same or different, a hydrogen atom, a halogen atom and the like, the symbol “*” represents an optically active center, which comprises reacting in the presence of a cinchona alkaloid and the like a compound represented by the general formula: wherein R1 and R2 are as defined above with a compound represented by the general formula: wherein R3, R4 and R5 are as defined above, and X is a halogen atom.

摘要翻译： 本发明提供一种制备由以下通式表示的光学活性β-羟基酯化合物的方法：其中R 1表示任选取代的烃基等，R 2 O >表示不同于R 1的含氮杂环基，其由以下通式表示：其中该环可以被取代等，R 3表示任选地 取代烃基等，R 4和R 5表示相同或不同的氢原子，卤素原子等，符号“*”表示 光学活性中心，其包括在cinchona生物碱等存在下反应，由通式表示的化合物：其中R 1和R 2如上定义 与下列通式表示的化合物：其中R 3，R 4和R 5如上所定义，X是卤代基 n原子。