公开(公告)号：EP0902011A4

公开(公告)日：2002-03-20

申请号：EP98902203

申请日：1998-02-13

Applicant: KANEKA CORP

Inventor： YAMADA MASAHIKO ,  NAGASHIMA NOBUO ,  HASEGAWA JUNZO

IPC: B01J23/44 ,  C07B53/00 ,  C07B61/00 ,  C07C227/08 ,  C07C227/18 ,  C07C229/36 ,  C07C253/30 ,  C07C255/58 ,  C07C319/20 ,  C07C323/63

CPC classification number: C07C227/18 ,  C07C227/08 ,  C07C229/36

Abstract: A highly economical and efficient process for producing optically active homophenylalanine derivatives represented by general formula (IV); and intermediates therefor and a process for producing the same. The process comprises reacting a β-benzoylacrylic acid derivative represented by general formula (II) with a 1-arylethylamine derivative represented by general formula (III) and reducing the resultant η-oxo-homophenylalanine derivative represented by general formula (I).

公开(公告)号：EP1604975A4

公开(公告)日：2006-11-02

申请号：EP04721366

申请日：2004-03-17

Applicant: KANEKA CORP

Inventor： TANAKA TATSUYOSHI ,  SUGAWARA MASANOBU ,  MAEDA HIROFUMI ,  NISHIYAMA AKIRA ,  YASOHARA YOSHIHIKO ,  NAGASHIMA NOBUO

IPC: C07C231/02 ,  C07C231/10 ,  C07C231/18 ,  C07C235/16 ,  C07C237/06 ,  C07C237/52 ,  C07C303/28 ,  C07C309/66 ,  C07C309/73 ,  C07D205/08 ,  C07C269/06 ,  C07C269/04 ,  C07C271/64 ,  C07C303/44

CPC classification number: C07C309/73 ,  C07C231/02 ,  C07C231/10 ,  C07C231/18 ,  C07C235/16 ,  C07C303/28 ,  C07C309/66 ,  C07D205/08 ,  C07C237/06 ,  C07C237/52

Abstract: The invention provides processes by which (R)-3-[4- (trifluoromethyl)phenylamino]pentanamide derivatives useful as intermediates of drugs, particularly, cholesteryl ester transfer protein (CETP) inhibitor can be easily and simply produced from easily available starting materials. According to the invention, (S)-N-[4-(trifluoromethyl)- phenyl]-3-hydroxypentanamide is produced from easily available raw materials and converted into (R)-3-[4-(trifluoromethyl)- phenylamino]pentanamide through (R)-4-ethyl-1-[4-(trifluoro- methyl)phenyl]-2-azetidinone. Further, (R)-3-[4-(trifluoro- methyl)phenylamino]pentanamide derivatives are produced by reacting (R)-4-ethyl-1-[4-trifluoromethyl]phenyl]-2- azetidinone with a carbamic acid ester.

公开(公告)号：EP1193253A4

公开(公告)日：2006-01-11

申请号：EP00927758

申请日：2000-05-15

Applicant: KANEKA CORP

Inventor： HONDA TATSUYA ,  NAGASHIMA NOBUO

IPC: C07C227/16 ,  C07C227/22 ,  C07C229/20 ,  C07D205/04 ,  C07D207/26 ,  C07D207/273 ,  C07C227/26

CPC classification number: C07D207/273 ,  C07C227/16 ,  C07C227/22 ,  C07C229/20 ,  C07D205/04

Abstract: A compound (5) can be produced by preparing a compound (3) by subjecting compound (1) to halogenation with inversion to obtain a compound (2) and hydrolyzing the compound (2), by subjecting a compound (6) to halogenation with inversion to obtain a compound (7) and hydrolyzing the compound (7), or by subjecting a compound (6) to halogenation with inversion to obtain a compound (7), cyclizing the compound (7) into a compound (2) and hydrolyzing the compound (2), cyclizing the compound (3) prepared above, and treating the obtained product with an amino-protective agent. The compound (5) thus produced can be further improved in the optical purity by recrystallization.

公开(公告)号：EP1179530A4

公开(公告)日：2005-07-27

申请号：EP01904517

申请日：2001-02-16

Applicant: KANEKA CORP

Inventor： SUGAWARA MASANOBU ,  FUJII AKIO ,  OKURO KAZUMI ,  SAKA YASUHIRO ,  NAGASHIMA NOBUO ,  INOUE KENJI ,  TAKEDA TOSHIHIRO ,  KINOSHITA KOICHI ,  MOROSHIMA TADASHI ,  FUSE YOSHIHIDE ,  UEDA YASUYOSHI

IPC: C07C227/10 ,  C07C227/32 ,  C07C227/42 ,  C07C229/26 ,  C07C229/30 ,  C07C303/36 ,  C07C311/19 ,  C07D203/08 ,  C07D203/20 ,  C07D203/24 ,  C07B53/00 ,  C07C227/04

CPC classification number: C07D203/08 ,  C07B2200/07 ,  C07C227/10 ,  C07C227/32 ,  C07C227/42 ,  C07C229/30 ,  C07C303/36 ,  C07D203/20 ,  C07D203/24 ,  C07C311/19 ,  C07C229/26

Abstract: An optically active amino acid derivative is prepared either by subjecting an optically active 3-haloalanine derivative (1) to N-protection followed by cyclization or cyclization followed by N-protection to prepare an optically active aziridinecarboxylic acid derivative (3) whose imino group is protected with 2- and/or 4-nitrated benzenesulfonyl and treating this derivative (3) with an organometallic reagent or by subjecting an optically active 3-haloalanine derivative to N-protection to obtain an optically active 3-haloalanine derivative (4) whose amino group is protected with 2- and/or 4-nitrated benzenesulfonyl and treating this derivative (4) with an organometallic reagent. According to such processes, natural and nonnatural optically active amino acids can be prepared from inexpensive raw materials through simple and easy operation. In said derivatives, X is halogen; R?1 and R2¿ are each hydrogen or the like; * represents an asymmetric carbon atom; and P1 is 2- and/ or 4- nitrated benzenesulfonyl.

公开(公告)号：EP1253140A4

公开(公告)日：2003-03-26

申请号：EP01902737

申请日：2001-02-02

Applicant: KANEKA CORP

Inventor： SAKA YASUHIRO ,  HONDA TATSUYA ,  NAGASHIMA NOBUO

IPC: C07D205/04

CPC classification number: C07D205/04

Abstract: A process for preparing optically active azetidine -2-carboxylic acid efficiently, easily, simply, and industrially advantageously by cyclizing an optically active 4-amino- 2-halogenobutyric acid in an optical yield of as high as 90 % or above. Specifically, a process for preparing optically active azetidine-2-carboxylic acid of formula (2) (wherein * represents an asymmetric carbon atom) by cyclizing an optically active 4-amino-2-halogenobutyric acid of the general formula (1) (wherein X is halogeno and * represents an asymmetric carbon atom) in the presence of an alkaline earth metal oxide, an alkaline earth metal hydroxide except barium hydroxide, or an organic amine.

公开(公告)号：EP1170287A4

公开(公告)日：2002-08-07

申请号：EP01946848

申请日：2001-01-25

Applicant: KANEKA CORP

Inventor： NAGASHIMA NOBUO

IPC: C07C271/22 ,  C07C303/38 ,  C07C311/19 ,  C07D205/04 ,  C07C269/04

CPC classification number: C07C311/19 ,  C07B2200/07 ,  C07C271/22 ,  C07C303/38 ,  C07D205/04 ,  Y02P20/55

Abstract: A process for preparing optically active N-substituted azetidine-2-carboxylic acids of the general formula (2) efficiently, simply, easily and industrially advantageously by subjecting an optically active 4-(substituted amino)-2= halogenobutyric acid of the general formula (1) to cyclization in the presence of a base; and novel compounds of the general formula (3) wherein R is a substituted oxycarbonyl type protective group or a substituted sulfonyl type protective group; X is halogeno; and * represents an asymmetric carbon atom.

公开(公告)号：EP2039689A4

公开(公告)日：2011-12-28

申请号：EP07743869

申请日：2007-05-22

Applicant: KANEKA CORP

Inventor： MORI KOHEI ,  NISHIYAMA AKIRA ,  TAOKA NAOAKI ,  MORIYAMA DAISUKE ,  NAGASHIMA NOBUO

IPC: C07D263/16 ,  C07B53/00 ,  C07B61/00 ,  C07C67/31 ,  C07C69/675 ,  C07C231/12 ,  C07C231/16 ,  C07C237/04 ,  C07C237/22 ,  C07D301/24 ,  C07D303/16 ,  C07D303/48 ,  C12P7/42 ,  C12P7/62

CPC classification number: C07B53/00 ,  C07B2200/07 ,  C07C67/31 ,  C07C231/18 ,  C07C237/04 ,  C07C237/22 ,  C07C2601/02 ,  C07D263/16 ,  C07D301/24 ,  C07D303/16 ,  C07D303/48 ,  C12P7/42 ,  C12P13/02 ,  C12P41/002 ,  C07C69/675

公开(公告)号：EP1715054A4

公开(公告)日：2010-10-06

申请号：EP05703812

申请日：2005-01-19

Applicant: KANEKA CORP

Inventor： NISHIYAMA AKIRA ,  TAOKA NAOAKI ,  KISHIMOTO NARUMI ,  NAGASHIMA NOBUO

IPC: C12P7/18 ,  C07C303/28 ,  C07C309/66 ,  C12N15/53 ,  C12P11/00 ,  C12P17/10 ,  C12P41/00

CPC classification number: C12P17/10 ,  C07C303/28 ,  C12P7/18 ,  C12P11/00 ,  C07C309/66

公开(公告)号：EP1512677A4

公开(公告)日：2007-06-20

申请号：EP03733239

申请日：2003-06-02

Applicant: KANEKA CORP

Inventor： NISHIYAMA AKIRA ,  KISHIMOTO NARUMI ,  NAGASHIMA NOBUO

IPC: C07C45/63 ,  C07C49/84 ,  C07C213/00 ,  C07C215/28 ,  C07C215/30 ,  C07C221/00 ,  C07C225/16 ,  C07B57/00

CPC classification number: C07C49/84 ,  C07B2200/07 ,  C07C45/63 ,  C07C213/00 ,  C07C215/28 ,  C07C221/00 ,  C07C215/30 ,  C07C225/16

Abstract: A process for easily producing, from an easily available inexpensive starting material, an optically active ß-amino alcohol useful as an intermediate for medicines. An easily available alpha-substituted ketone is reacted with an optically active amine to produce a mixture of diastereomers of an optically active alpha-substituted aminoketone. One of the diastereomers is separated optionally after the diastereomers are converted to a salt with an acid. The optically active alpha-substituted aminoketone or salt thereof thus isolated is subjected to stereoselective reduction to produce an optically active ß-substituted amino alcohol, which is then subjected to hydrogenolysis. Thus, an optically active ß-amino alcohol or a salt thereof is produced.

公开(公告)号：EP1321454A4

公开(公告)日：2005-11-02

申请号：EP01965626

申请日：2001-09-13

Applicant: KANEKA CORP

Inventor： NAGASHIMA NOBUO

IPC: C07C209/62 ,  C07C211/27 ,  C07C213/02 ,  C07C227/18 ,  C07C229/36 ,  C07C269/04 ,  C07C271/20 ,  C07D205/04 ,  C07D207/40 ,  C07D207/416 ,  C07C215/30 ,  C07C227/06 ,  C07C229/22 ,  C07C231/02 ,  C07C233/00 ,  C07C271/22 ,  C07D207/16

CPC classification number: C07D207/416 ,  C07C209/62 ,  C07C213/02 ,  C07C227/18 ,  C07C269/04 ,  C07D205/04 ,  C07C211/27 ,  C07C229/36 ,  C07C271/20

Abstract: A process which comprises reacting a 2- or 4-nitro- benzenesulfonamide with an alkali metal alkoxide to remove the nitrobenzenesulfonyl group and thereby obtain an amine corresponding to the amide, and, if necessary, reacting this amine without isolation with an activated substituted oxycarbonyl compound or an activated acyl compound to obtain an amine derivative. According to this process, free amines and substituted derivatives thereof can be easily and simply prepared with industrial advantage from 2- or 4-nitrobenzenesulfonamides without using any thiol compound.