公开(公告)号：EP1055671B1

公开(公告)日：2004-12-01

申请号：EP99959738.8

申请日：1999-12-10

申请人： KANEKA CORPORATION

发明人： TAOKA, Naoaki ,  INOUE, Kenji

IPC分类号： C07D309/30 ,  C07D319/06

CPC分类号： C07D319/06 ,  C07D309/30 ,  Y02P20/55

摘要： A convenient, efficient and industrially favorable process for producing simvastatin which is useful as an HMG-coA reductase inhibitor. This process comprises deacylating lovastatin by treating with an inorganic base and a secondary or tertiary alcohol to thereby form diol lactone, and then selectively protecting, acylating, deblocking and lactonizing the diol lactone by using a ketal or acetal protective group to thereby give simvastatin.

公开(公告)号：EP1104750B1

公开(公告)日：2004-04-14

申请号：EP00935526.4

申请日：2000-06-02

申请人： KANEKA CORPORATION

发明人： NISHIYAMA, Akira ,  INOUE, Kenji

IPC分类号： C07C67/343

CPC分类号： C12P7/62 ,  C07B2200/07 ,  C07C67/343 ,  C07C253/30 ,  C07D319/06 ,  C07C69/716 ,  C07C255/21 ,  C07C69/738

公开(公告)号：EP0827943B1

公开(公告)日：2003-05-21

申请号：EP97901761.3

申请日：1997-01-29

申请人： KANEKA CORPORATION

发明人： SUGAWA, Tadashi ,  MOROSHIMA, Tadashi ,  INOUE, Kenji ,  KAN, Kazunori

IPC分类号： C07B41/02 ,  C07C29/143 ,  C07C33/22 ,  C07C213/00 ,  C07C215/28 ,  C07C271/10 ,  C07C323/43

CPC分类号： C07B53/00 ,  C07B41/02 ,  C07C29/143 ,  C07C213/00 ,  C07C269/06 ,  C07C319/20 ,  C07C323/43 ,  C07C271/16 ,  C07C271/22 ,  C07C33/22 ,  C07C33/46

公开(公告)号：EP1153919A1

公开(公告)日：2001-11-14

申请号：EP00903975.1

申请日：2000-02-16

申请人： KANEKA CORPORATION

发明人： AMANO, Susumu ,  TAOKA, Naoaki ,  MITSUDA, Masaru ,  INOUE, Kenji

IPC分类号： C07D213/50 ,  C07D213/64 ,  C07D213/72 ,  C07D213/75 ,  C07D405/04

CPC分类号： C07D213/30 ,  C07D213/50 ,  C07D213/74 ,  C07D213/75 ,  C07D405/04

摘要： It is an objective to produce intermediates of optically active beta-3 adrenaline receptor agonists from readily available raw materials in a safe, efficient and industrially advantageous manner. A substituted acetylpyridine derivative represented by the general formula (9) is reduced by enantioselective reduction to produce an optically active hydroxyethylpyridine derivative represented by the general formula (10) (wherein * represents an asymmetric carbon atom), and it is further derivatized to an intermediate of an optically active beta-3 adrenaline receptor agonist, such as an optically active dihydroxyethylpyridine derivative represented by the general formula (14) or an optically active oxirane derivative represented by the general formula (16) .

摘要翻译： 它是在一个安全，有效和工业上有利的方式生产光学活性的β-3肾上腺素受体激动剂的中间体从原料易得的目标。 甲substituiertem acetylpyridines衍生物由通式（9）表示由对映选择性还原还原以产生由通式（10）（worin * darstellt不对称碳原子。）表示的光学活性hydroxyethylpyridine衍生物，和它在中间体进一步衍生化，以 激动剂光学活性的β-肾上腺素3受体，如在光学活性衍生物dihydroxyethylpyridine测试通过或由通式（16）表示的光学活性环氧乙烷衍生物的通式（14）表示。

公开(公告)号：EP1078919A1

公开(公告)日：2001-02-28

申请号：EP00907964.1

申请日：2000-03-09

申请人： KANEKA CORPORATION

发明人： NISHIYAMA, Akira ,  INOUE, Kenji

IPC分类号： C07C269/06 ,  C07C271/18 ,  C07C271/22

CPC分类号： C07C269/06 ,  C07C271/18 ,  C07C271/22

摘要： The present invention provides a commercially profitable process for producing a β-amino acid ester derivative

which comprises reacting an α-amino acid ester derivative with a base and a dihalomethane,
reacting the same with a lithium amide and an alkyllithium in succession,
and treating the reaction product with an acid in an alcohol.

摘要翻译： 本发明提供了一种商业上有利的生产β-氨基酸酯衍生物的方法，该方法包括使α-氨基酸酯衍生物与碱和二卤甲烷反应，将其与氨基锂和烷基锂连续反应， 在醇中与酸反应的产物。

公开(公告)号：EP1046634A1

公开(公告)日：2000-10-25

申请号：EP98961624.8

申请日：1998-12-28

申请人： KANEKA CORPORATION

发明人： YAMASHITA, Koki ,  INOUE, Kenji ,  KINOSHITA, Koichi ,  UEDA, Yasuyoshi ,  MURAO, Hiroshi

IPC分类号： C07C229/20 ,  C07C227/16 ,  C07C227/40 ,  C07C323/58 ,  C07C319/14 ,  C07B53/00

CPC分类号： C07C227/16 ,  C07C319/14 ,  Y02P20/55 ,  C07C323/58 ,  C07C323/59 ,  C07C229/20

摘要： An industrially advantageous method of producing β-halogeno-α-aminocarboxylic acids is provided. Methods are also provided of producing optically active N-protected-S-phenylcysteines having high optical purity and of intermediates thereof, respectively, in which the above production method is utilized.
A method of producing β-halogeno-α-aminocarboxylic acids or salts thereof is disclosed which comprises halogenating the hydroxyl group of a β-hydroxy-α-aminocarboxylic acid (in which the basicity of the amino group in α-position is not masked by the presence of a substituent on said amino group) or a salt thereof with an acid with a halogenating agent. A method of producing optically active N-protected-S-phenylcysteines represented by the general formula (3) or salts thereof is further disclosed which comprises applying the above production method to optically active serine or a salt thereof and then carrying out treatment with an amino-protecting agent and reaction with thiophenol under a basic condition.

公开(公告)号：EP1029856A1

公开(公告)日：2000-08-23

申请号：EP99940471.8

申请日：1999-08-25

申请人： Kaneka Corporation

发明人： OKURO, Kazumi ,  INOUE, Kenji

IPC分类号： C07D301/02 ,  C07D303/36

CPC分类号： C07D303/36

摘要： A process for producing (2R,3S)-3-amino-4-phenylbutane-1,2-epoxide compounds which comprises treating a (2S,3S)-3-amino-1-halo-2-hydroxy-4-phenylbutane compound or a (2S,3S)-3-amino-4-phenylbutane-1,2-epoxide with a carboxylic acid quaternary ammonium salt or a carboxylic acid metal salt a quaternary ammonium salt and a quaternary ammonium salt, to give a (2S,3S)-1-acyloxy-3-amino-2-hydroxy-4-phenylbutane compound, further treating the same with a sulfonic acid halide in the presence of an organic base to give a (2S,3S)-1-acyloxy-3-amino-2-sulfonyloxy-4-phenylbutane compound furthermore treating said compound with an inorganic base.
An intermediate for the production of an HIV protease inhibitor can be produced from L-phenylalanine.

摘要翻译： 一种制备（2R，3S）-3-氨基-4-苯基丁烷-1,2-环氧化物化合物的方法，包括（2S，3S）-3-氨基-1-卤代-2-羟基-4-苯基丁烷化合物 或（2S，3S）-3-氨基-4-苯基丁烷-1,2-环氧化物与羧酸季铵盐或羧酸金属盐季铵盐和季铵盐反应，得到（2S， 3S）-1-酰氧基-3-氨基-2-羟基-4-苯基丁烷化合物，在有机碱的存在下，用磺酸卤化物进一步处理，得到（2S，3S）-1-酰氧基-3 - 氨基-2-磺酰氧基-4-苯基丁烷化合物，此外用无机碱处理所述化合物。 用于生产HIV蛋白酶抑制剂的中间体可由L-苯丙氨酸制备。

公开(公告)号：EP0969000A1

公开(公告)日：2000-01-05

申请号：EP98923095.8

申请日：1998-06-03

申请人： KANEKA CORPORATION

发明人： MATSUO, Kazuhiko ,  MATSUMOTO, Shingo ,  INOUE, Kenji

IPC分类号： C07C269/06 ,  C07C271/16 ,  C07C323/44 ,  C07C271/22 ,  C07B41/02

CPC分类号： C07C269/06 ,  C07C271/16 ,  C07C271/22

摘要： The present invention has its objects to provide a method for reducing α-aminoketone derivatives under mild conditions with high stereoselectivity.
This invention is a method for reducing α-aminoketone which comprises reacting an α-aminoketone derivative of general formula (1) with a compound prepared from an organoaluminum compound of general formula (4), a sulfonic acid derivative of general formula (5), and an alcohol compound of general formula (6) to give an α-aminoalcohol derivative of general formula (7).

摘要翻译： 本发明的目的在于提供一种在高立体选择性的温和条件下还原α-氨基酮衍生物的方法。 本发明是一种还原α-氨基酮的方法，该方法包括使通式（1）的α-氨基酮衍生物与由通式（4）的有机铝化合物，通式（5）的磺酸衍生物， 和通式（6）的醇化合物反应，得到通式（7）的α-氨基醇衍生物。

公开(公告)号：EP0670305A1

公开(公告)日：1995-09-06

申请号：EP94927066.4

申请日：1994-09-20

申请人： KANEKA CORPORATION

发明人： INOUE, Kenji ,  AWAJ, Hiroshi ,  TAKAHASHI, Satomi

IPC分类号： C07C271/16 ,  C07D263/24 ,  B01J27/135

CPC分类号： C07D263/24 ,  C07C271/16 ,  Y02P20/55

摘要： An economically excellent and efficient process for producing a 3-amino-2-hydroxy-1-propanol derivative, represented by general formula (2), useful as an intermediate for producing medicines, such as an HIV protease inhibitor, and an oxazolidinone derivative derived therefrom, wherein R¹ represents alkyl, aralkyl or aryl; and R² and R³ represent each independently hydrogen or an amino-protecting group, provided the case where both of R² and R³ represent hydrogen is excluded.

摘要翻译： 用于生产由通式（2）表示的3-氨基-2-羟基-1-丙醇衍生物的经济优良和有效的方法，其可用作生产药物的中间体，例如HIV蛋白酶抑制剂和衍生的恶唑烷酮衍生物 其中R 1表示烷基，芳烷基或芳基; R 2和R 3各自独立地表示氢或氨基保护基，只要R 2和R 3均代表氢即可。

公开(公告)号：EP1647551A1

公开(公告)日：2006-04-19

申请号：EP04747351.7

申请日：2004-07-05

申请人： KANEKA CORPORATION

发明人： OKURO, Kazumi ,  TANAKA, Tatsuyoshi ,  MITSUDA, Masaru ,  INOUE, Kenji

IPC分类号： C07D301/24 ,  C07D303/14 ,  C07D249/08 ,  C07D309/12 ,  C07D405/06 ,  C07C33/46 ,  C07C29/10 ,  C07C43/178 ,  C07C41/26 ,  C07C69/28 ,  C07C67/29 ,  C07F7/08 ,  C07B53/00

CPC分类号： C07C67/29 ,  C07B2200/07 ,  C07C29/10 ,  C07D301/24 ,  C07C33/46

摘要： The present invention provides an industrially safe, easily operable process for producing an optically active epoxy alcohol derivative useful as an intermediate for pharmaceuticals from inexpensively available materials, and also provides a novel halohydrin derivative serving as an important intermediate for the epoxyalcohol derivative. Furthermore, the present invention provides a process for producing an intermediate for a triazole antifungal agent by allowing a halohydrin to react with a triazole sulfonamide, the process including a small number of steps. A process for producing an optically active epoxy alcohol derivative includes allowing an optically active α-substituted propionate derivative to react with a haloacetic acid derivative in the presence of a base to prepare an optically active haloketone derivative, allowing the resulting haloketone derivative to react with an aryl metal compound to stereoselectively prepare a halohydrin derivative, eliminating a substituent for the hydroxy group of the halohydrin derivative, and performing epoxidation with a base. Furthermore, a process for producing an intermediate for a triazole antifungal agent includes allowing a halohydrin derivative to react with a triazole sulfonamide, the process including a small number of steps.

摘要翻译： 本发明提供工业上上安全，易于操作处理，用于光学活性环氧醇衍生物可用作在中间从廉价地获得的材料制备药物，并且因此提供了一种新型的卤代醇在重要中间体衍生物用作用于环氧醇衍生物。 进一步地，本发明提供了用于通过允许卤代醇与三唑磺酰胺，该方法包括少量步骤反应在中间为三唑类抗真菌剂的制造方法。 一种用于在光学活性环氧醇衍生物的制造方法包括：允许向旋光±取代丙酸酯衍生物在碱的存在下，卤代乙酸衍生物反应来制备光学活性的卤代酮衍生物，使所得卤代酮衍生物与在反应 芳金属化合物立体选择性地制备卤代醇衍生物，消除了对卤代醇衍生物的羟基的取代基，并用碱进行环氧化作用。 进一步，在中间制造用于三唑类抗真菌剂的方法包括：允许卤代醇衍生物与三唑磺酰胺，该方法包括少量步骤反应。