公开(公告)号：US4916074A

公开(公告)日：1990-04-10

申请号：US113764

申请日：1987-10-28

申请人： Naoyuki Yoshida ,  Hiroshi Morita

发明人： Naoyuki Yoshida ,  Hiroshi Morita

IPC分类号： C09K19/12 ,  C12P7/62 ,  C12P13/00 ,  C12P41/00

CPC分类号： C12P13/004 ,  C09K19/126 ,  C12P41/004 ,  C12P7/62

摘要： The present invention provides a process for producing optically active compounds by a biochemical method in which specific compounds having hydroxyl groups are reacted with esters in the presence of enzymes. The compounds have the following general formula. ##STR1## wherein Y is selected from the group consisting halogen atoms, alkyl groups having 1-3 carbon atoms, cyano groups, and trifluoromethyl groups, W is selected from the group consisting substituted phenyl groups, and halogen atoms, cyano, trifluoromethyl and amino groups and alkylamino and alkyloxycarbonyl groups in which alkyl groups have 1-20 carbon atoms, R is methylene and n is 0 or 1.The enzymes having ability of transesterification reaction is preferably lipase, lipoprotein lipase, esterase and so on, and micro-organisms can be used in the above process.

摘要翻译： 本发明提供了通过生物化学方法制备光学活性化合物的方法，其中具有羟基的特定化合物在酯存在下与酯反应。 该化合物具有以下通式。 其中Y选自卤素原子，具有1-3个碳原子的烷基，氰基和三氟甲基，W选自取代的苯基，卤素原子，氰基，三氟甲基和氨基 基团和其中烷基具有1-20个碳原子的烷基氨基和烷氧基羰基，R是亚甲基，n是0或1.具有酯交换反应能力的酶优选为脂肪酶，脂蛋白脂肪酶，酯酶等，微生物 可用于上述过程。

公开(公告)号：US5256569A

公开(公告)日：1993-10-26

申请号：US931418

申请日：1992-08-24

申请人： Naoyuki Yoshida ,  Hiroshi Morita

发明人： Naoyuki Yoshida ,  Hiroshi Morita

IPC分类号： C12P7/62 ,  C12P7/64 ,  C12P41/00

CPC分类号： C12P7/6454 ,  C12P41/004 ,  C12P7/62 ,  Y10S435/874

摘要： An optically active alcohol of this invention is obtained from a process using an enzyme having the ability to conduct preferentially a transesterification reaction with a triglyceride and an (R,S)-alcohol represented by a general formula: ##STR1## wherein X indicates alkyl group having a carbon number of 2-10, Y indicates alkyl group having a carbon number of 1-3, CF.sub.3 or CN, and X.noteq.Y. In this process, the (R,S)-alcohol of the above formula (1) and the triglyceride are reacted under substantially anhydrous conditions. The obtained ester is resolved and the optically active alcohol which contains richly either R- or S-alcohol is produced the optically active alcohol is efficiently obtained by an industrially advantageous biochemical method.

摘要翻译： 本发明的光学活性醇是从使用具有优先与甘油三酯和由下列通式表示的（R，S） - 醇进行酯交换反应的能力的酶的方法获得的：其中X 表示碳数为2-10的烷基，Y表示碳数为1-3的烷基，CF 3或CN，X为等式Y。在该方法中，上式的（R，S） - 醇 （1）和甘油三酸酯在基本上无水的条件下反应。 通过工业上有利的生物化学方法有效地获得所得的酯，并且产生含有R-或S-醇的光学活性的醇。

公开(公告)号：US4962031A

公开(公告)日：1990-10-09

申请号：US189163

申请日：1988-05-02

申请人： Naoyuki Yoshida ,  Masakazu Kaneoya ,  Manabu Uchida ,  Hiroshi Morita

发明人： Naoyuki Yoshida ,  Masakazu Kaneoya ,  Manabu Uchida ,  Hiroshi Morita

IPC分类号： C12P7/62 ,  C12P13/00 ,  C12P41/00

CPC分类号： C12P13/001 ,  C12P13/002 ,  C12P41/004 ,  C12P7/62

摘要： The present invention provides a process for producing optically active compounds by a biochemical method in which specific compounds having hydroxyl groups are reacted with esters in the presence of hydrolases. The compounds have the following general formula: ##STR1## wherein X is selected from halogen atoms and a cyano group. Y is selected from the group constituting substituted phenyl groups, halogen atoms, cyano, trifluoromethyl and amino groups and alkylamino and alkyloxycarbonyl groups in which alkyl groups have 1-20 carbon atoms. R is an alkylene group having 1-20 carbon atoms and n is 0 or 1.

公开(公告)号：US20100324280A1

公开(公告)日：2010-12-23

申请号：US12521525

申请日：2007-12-26

申请人： Ippei Yamaoka ,  Naoyuki Yoshida ,  Kazushi Ishida ,  Shuji Sasaki

发明人： Ippei Yamaoka ,  Naoyuki Yoshida ,  Kazushi Ishida ,  Shuji Sasaki

IPC分类号： C07H15/04

CPC分类号： A61K31/717 ,  C08B5/14 ,  C08B11/10 ,  C08B15/005 ,  C08L1/16 ,  C08L1/284

摘要： The present invention provides a sodium absorption inhibitor, a potassium absorption inhibitor, and a phosphorus absorption inhibitor, and a preventive agent, a therapeutic agent and a food for diseases caused by overconsumption of common salt, potassium and phosphorus or diseases which require restriction of ingestion of common salt, potassium and phosphorus to actively and safely excrete overconsumed common salt, potassium and phosphorus excreted outside the body. R—O-A   (I) {In the formula (I), R represents a crosslinked cellulose residue and A represents a functional group a having cation-exchange ability.}

摘要翻译： 本发明提供了一种钠吸收抑制剂，钾吸收抑制剂和磷吸收抑制剂，以及预防药物，治疗剂和由食盐过多，钾和磷引起的疾病或需要限制摄取的疾病的食物。 的普通盐，钾和磷，以积极和安全地排泄体外过量消耗的普通盐，钾和磷。 R-O-A（I）{式（I）中，R表示交联纤维素残基，A表示具有阳离子交换能力的官能团。

公开(公告)号：US06265209B1

公开(公告)日：2001-07-24

申请号：US09318435

申请日：1999-05-25

申请人： Naoyuki Yoshida ,  Kunio Ogasawara

发明人： Naoyuki Yoshida ,  Kunio Ogasawara

IPC分类号： C07C104

CPC分类号： C07D307/77 ,  C07B2200/07 ,  C07C29/147 ,  C07C35/37 ,  C07C49/643 ,  C07C69/013 ,  C07C69/16 ,  C07C2603/68 ,  C07D303/32 ,  C07D317/70 ,  C07D473/00 ,  C07D493/08 ,  C07F7/1804 ,  C12P7/62 ,  C12P15/00 ,  C12P41/004 ,  C07C35/26

摘要： Intermediate compounds, including 2-(t-butyldimethylsilyloxymethyl)-3,4-[(dimethylmethylene)dioxy]-5-hydroxy-tricyclo[5.2.1.02,6]dec-8-ene, which are useful for the synthesis of neplanocin A having strong antitumor activity. Improved processes for the preparation of neplanocin A, starting from optically active 2-hydroxymethyl-5-hydroxy-tricyclo[5.2.1.02,6]deca-3,8-diene and via a key step comprising a retro-Diels-Alder reaction of the above intermediate.

公开(公告)号：US5973214A

公开(公告)日：1999-10-26

申请号：US154247

申请日：1998-09-16

申请人： Naoyuki Yoshida ,  Hitoshi Yano

发明人： Naoyuki Yoshida ,  Hitoshi Yano

IPC分类号： C12P7/62 ,  C12P41/00 ,  C07C29/03

CPC分类号： C12P7/62 ,  C12P41/004

摘要： Both enantiomers of optically active 2-alkanol are produced by transesterification reaction of racemic 2-alkanol and aliphatic acid 2,2,2-trichloroethylester in the presence of enzyme derived from Candida antarctica.Both enantiomers of optically active 2-alkanol, which are useful as starting materials of liquid crystal materials and have optical purity of 99% or more, can be efficiently produced.

摘要翻译： 光学活性2-链烷醇的两种对映异构体都是通过外消旋的2-链烷醇和脂肪酸2,2,2-三氯乙基酯在源自南极念珠菌的酶的存在下进行酯交换反应制备的。 作为液晶材料的起始原料，光学纯度为99％以上的光学活性2-链烷醇的两种对映异构体都可以有效地制造。

公开(公告)号：US5623078A

公开(公告)日：1997-04-22

申请号：US666742

申请日：1996-06-20

申请人： Yasuo Urata ,  Mamoru Fujita ,  Teruyo Sugiura ,  Fumitaka Ohizumi ,  Naoyuki Yoshida

发明人： Yasuo Urata ,  Mamoru Fujita ,  Teruyo Sugiura ,  Fumitaka Ohizumi ,  Naoyuki Yoshida

IPC分类号： C07D209/52 ,  C07D209/02

CPC分类号： C07D209/02

摘要： A production process with good efficiency, and applicable to production of a synthetic intermediate of a new quinolone anti-fungus agent CP-99219, is provided.A production process of an intermediate of a new quinolone compound expressed by the formula (IV) ##STR1## wherein R.sup.3 represents a benzyl group, a diphenylmethyl group, etc. and R.sup.4 represents a linear or branched alkyl group of 1 to 8C, a cycloalkyl group, etc.which process employs as a starting substance, a cyclopropanetricarboxylic acid triester expressed by the formula (I) ##STR2## wherein R.sup.1 and R.sup.2 represent a linear or branched alkyl group, a cycloalkyl group, an aryl group or an aralkyl group,and passes through seven steps.

摘要翻译： 提供了一种效率高，适用于生产新型喹诺酮类抗真菌剂CP-99219的合成中间体的生产方法。 由式（IV）表示的新型喹诺酮化合物的中间体（IV）的制备方法，其中R 3表示苄基，二苯基甲基等，R 4表示1〜8的直链或支链烷基 ，该方法用作起始物质的环烷基等，由式（I）表示的环丙烷三羧酸三酯，支化烷基，环烷基，芳基或芳烷基，并通过七个步骤。

公开(公告)号：US5395983A

公开(公告)日：1995-03-07

申请号：US182566

申请日：1994-01-18

申请人： Kazutoshi Miyazawa ,  Teruyo Sugiura ,  Yasuyuki Koizumi ,  Naoyuki Yoshida

发明人： Kazutoshi Miyazawa ,  Teruyo Sugiura ,  Yasuyuki Koizumi ,  Naoyuki Yoshida

IPC分类号： C07C29/78 ,  C07C33/26 ,  C07C29/76

CPC分类号： C07C29/78 ,  C07C33/26 ,  C07B2200/07

摘要： R or S-1-phenyl-1,3-propanediols having optical purity of 100% ee were obtained by recrystallization of R or S-1-phenyl-1,3-propanediols having optical purity of 20% ee to below 100% ee, the last diols are represented by the formula, ##STR1## It is possible to obtain optically pure 1-phenyl-3-propanediols from optically impure 1-phenyl-1,3-propanediols by a simple method.

摘要翻译： 光学纯度为100％ee的R或S-1-苯基-1,3-丙二醇通过将光学纯度为20％ee的R或S-1-苯基-1,3-丙二醇重结晶至低于100％ee ，最后的二醇由下式表示：通过简单的方法可以从光学上不纯的1-苯基-1,3-丙二醇获得光学上纯的1-苯基-3-丙二醇。

公开(公告)号：US5166341A

公开(公告)日：1992-11-24

申请号：US670443

申请日：1991-03-11

申请人： Tatsuya Kon ,  Shiro Kato ,  Toshiya Morie ,  Tadahiko Karasawa ,  Naoyuki Yoshida

发明人： Tatsuya Kon ,  Shiro Kato ,  Toshiya Morie ,  Tadahiko Karasawa ,  Naoyuki Yoshida

IPC分类号： C07D243/08 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14

CPC分类号： C07D401/14 ,  C07D243/08 ,  C07D403/12 ,  C07D405/14

摘要： Indazole-3-carboxylic acid derivatives represented by the following general formula (I) and their physiologically acceptable acid addition salts or quaternary ammonium salts, ##STR1## are useful as a potent and selective antagonist of serotonin 3 (5-HT.sub.3) receptor. Also disclosed are compounds of the formula ##STR2## which are useful as intermediates in the production of the disclosed final product compounds.

摘要翻译： 由下列通式（I）表示的吲唑-3-羧酸衍生物及其生理上可接受的酸加成盐或季铵盐可用作5-羟色胺3（5-HT 3）受体的有效和选择性拮抗剂。 还公开了式（IMAGE）的化合物，其可用作制备所公开的最终产品化合物的中间体。

公开(公告)号：US5128252A

公开(公告)日：1992-07-07

申请号：US690256

申请日：1991-04-25

申请人： Kazutoshi Miyazawa ,  Naoyuki Yoshida

发明人： Kazutoshi Miyazawa ,  Naoyuki Yoshida

IPC分类号： C12P41/00

CPC分类号： C12P41/004

摘要： The invention provides an optically active compound which is R- or S- ester having the general formula: ##STR1## wherein R.sup.1 is hydrogen or acyl of 2-20 carbon atoms, R.sup.2 is alkyl, alkenyl or alkynyl of 3-40 carbon atoms, and the carbon indicated by * is an asymmetric carbon atom.

摘要翻译： 本发明提供了具有以下通式的R-或S-酯的光学活性化合物：其中R1是氢或2-20个碳原子的酰基，R2是3-40的烷基，烯基或炔基 碳原子，由*表示的碳是不对称碳原子。