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    NOVEL PRODUCTION OF ALPHA-ASPARTYL-PHENYLALANINE ESTER
    2.
    发明专利
    NOVEL PRODUCTION OF ALPHA-ASPARTYL-PHENYLALANINE ESTER 失效

    公开(公告)号：JPS62145100A

    公开(公告)日：1987-06-29

    申请号：JP28304885

    申请日：1985-12-18

    申请人： NIPPON KAYAKU KK

    发明人： FUJII TADASHI ,  YANAGIUCHI KOJI ,  MITSUNOBU SHIYOUICHI ,  AOKI SHIGERU ,  TSUDA MAKOTO

    IPC分类号： C07K1/06 ,  B01J31/02 ,  C07B61/00 ,  C07K5/06 ,  C07K5/075

    摘要： PURPOSE:To obtain the titled compound useful as a sweetening agent in high yield without producing a by-product, by catalytically reducing an N-protected- N-hydroxymethyl-alpha-aspartylphenylalanine ester with hydrogen gas in the presence of an aromatic primary amine. CONSTITUTION:An N-protected-N-hydroxymethyl-phenylalanine ester expressed by formula I (R represents organic group reductively substituted by H, preferably benzyloxycarbonyl; R' represents 1-4C alkyl) (example; N- benzyloxycarbonyl-N-hydroxymethyl-alpha-aspartyl-phenylalani-ne methyl ester, etc.) is catalytically reduced with hydrogen gas using a catalyst such as palladium-carbon, etc. (preferably at 0-40 deg.C, for 0.5-3hr) in the presence of preferably 0.5-1.5 equivalents aromatic primary amine (preferably aniline), usually in a solvent such as methanol to obtain the aimed compound expressed by formula II.

    NEW PROCESS FOR PRODUCING 1-(4-TRIFLUOROMETHYLPHENYL)-1-PROPANONE
    4.
    发明专利
    NEW PROCESS FOR PRODUCING 1-(4-TRIFLUOROMETHYLPHENYL)-1-PROPANONE 失效

    公开(公告)号：JPS6419033A

    公开(公告)日：1989-01-23

    申请号：JP17394787

    申请日：1987-07-14

    申请人： NIPPON KAYAKU KK

    发明人： SUGIMURA HIDEO ,  SHIOZAWA AKIRA ,  YANAGIUCHI KOJI ,  NARITA KAZUHISA

    IPC分类号： C07C49/233 ,  C07C45/00 ,  C07C45/29 ,  C07C49/80 ,  C07C67/00

    摘要： PURPOSE:To obtain the title compound which is a synthetic intermediate of a compound having muscle relaxant action, without problems on bad small, industrial waste and operability, by allowing a specific oxidizing agent to act on 1-(4-trifluoromethylphenyl)-1-propanol. CONSTITUTION:The subject compound is prepared by oxidizing 1-(4- trifluoromethylphenyl)-1-propanol with an oxidizing agent of the formula (M is alkali metal, alkaline earth metal; X is halogen; n is 1-3), preferably sodium hypochlorite, calcium hypochlorite, sodium hypobromite from an industrial point of view, in a solvent such as acetone at 0-50 deg.C. The amount of the oxidizing agent used is 0.8-10, preferably 1-6 equivalents based on the starting substance. If is preferred that the addition of a phosphate or acetic acid is added to effect the reaction, after the oxidizing agent is added to the starting material in the solvent.

    RECOVERY OF PROPANONE DERIVATIVE
    5.
    发明专利
    RECOVERY OF PROPANONE DERIVATIVE 失效

    公开(公告)号：JPS63310878A

    公开(公告)日：1988-12-19

    申请号：JP14330087

    申请日：1987-06-10

    申请人： NIPPON KAYAKU KK

    发明人： SUGIMURA HIDEO ,  YANAGIUCHI KOJI ,  NARITA KAZUHISA ,  YAMAMOTO HIROTAKA

    IPC分类号： C07D295/10

    摘要： PURPOSE:To recover a propanone derivative in high yield, by adding pyrrolidine to filtrate or a treated solution obtained after optical resolution of 2-methyl-1-(4- trifluoromethylphenyl)-3-pyrrolidino-1-propan-one. CONSTITUTION:In optically resolving 2-methyl-1-(4-trifluoromethylphenyl)-3- pyrrolidino-1-propan-one useful as a central muscle relaxant and the recovering the propanone derivative thereof remaining in a filtrate, the filtrate or a treated solution thereof is mixed with 0.1-2 equivalents based on the propanone derivative of pyrrolidine and the propanone is collected. The propanone derivative as a raw material is reusable for producing an optically active propanone derivative and this process is suitable for mass production of the optically active propanone derivative.

    PRODUCTION OF N-PROTECTED-N-HYDROXYMETHYL-ALPHA-ASPARTYL-PHENYLALANINE ESTER
    6.
    发明专利
    PRODUCTION OF N-PROTECTED-N-HYDROXYMETHYL-ALPHA-ASPARTYL-PHENYLALANINE ESTER 失效

    公开(公告)号：JPS6339897A

    公开(公告)日：1988-02-20

    申请号：JP18186186

    申请日：1986-08-04

    申请人： NIPPON KAYAKU KK

    发明人： TSUDA MAKOTO ,  YANAGIUCHI KOJI ,  FUJII TADASHI ,  MITSUNOBU SHIYOUICHI ,  AOKI SHIGERU

    IPC分类号： C07K1/06 ,  B01J31/00 ,  B01J31/02 ,  C07K5/06 ,  C07K5/075

    摘要： PURPOSE:To obtain the titled compound useful for an intermediate for producing a low-caloric edulcorant in high yield, by condensing an alpha-[3-substituted-5- oxooxazolidinyl-(4)]-acetic acid with a phenylalanine ester in the presence of a basic catalyst. CONSTITUTION:(A) An alpha-[3-sublstituted-5-oxooxazolidinyl-(4)]-acetic acid expressed by formula I (R represents amino protecting group) {example; alpha-[3- benzyloxycarbonyl-5-oxooxazolidinyl-(4)]-acetic acid, etc.} is condensed with (B) a phenylalanine ester expressed by formula II (R' represents 1-4C alkyl) in the presence of a basic catalyst in an equimolar amount, based on the components A, equivalent to afford the aimed compound expressed by formula III.

    OPTICAL PURIFICATION OF SALT OF 2-METHYL-1-(4- TRIFLUOROMETHYLPHENYL)-3-PYRROLIDINO-1-PROPANONE
    7.
    发明专利
    OPTICAL PURIFICATION OF SALT OF 2-METHYL-1-(4- TRIFLUOROMETHYLPHENYL)-3-PYRROLIDINO-1-PROPANONE 失效

    公开(公告)号：JP2000290271A

    公开(公告)日：2000-10-17

    申请号：JP9949499

    申请日：1999-04-07

    申请人： NIPPON KAYAKU KK

    发明人： SUGIMURA HIDEO ,  YANAGIUCHI KOJI ,  NARITA KAZUHISA ,  YAMAMOTO HIROTAKA

    IPC分类号： C07D295/10 ,  C07B57/00

    摘要： PROBLEM TO BE SOLVED: To carry out an optical purification of the salt of 2-methyl-1-(4- trifluoromethylphenyl)-3-pyrrolidino-1-propanone in a high yield and purity without causing recemization during the purification process by suspending a mixture of a specific racemic salt of methyltrifluoromethylphenyl-pyrrolidinopropanone and an optically active isomer of the salt in an organic solvent. SOLUTION: A mixture of (A) a racemic salt of 2-methyl-1-(4- trifluoromethylphenyl)-3-pyrrolidino-1-propanone and (B) an optically active isomer of the salt is suspended in an organic solvent (preferably ketones, especially acetone, etc.), to collect the component B as the crystal and the component A as the solution. The salt is preferably hydrochloride. For example, acetone is added to (-)-2-methyl-1-(4-trifluoromethylphenyl)-3-pyrrolidino-1-propanone hydrochloride having an optical purity of 80% and the precipitated crystal is filtered to obtain the purified salt having an optical purity of 99.4%.

    NEW PRODUCTION OF AMINOKETONE DERIVATIVE
    8.
    发明专利
    NEW PRODUCTION OF AMINOKETONE DERIVATIVE 失效

    公开(公告)号：JPH07179446A

    公开(公告)日：1995-07-18

    申请号：JP30014294

    申请日：1994-11-10

    申请人： NIPPON KAYAKU KK

    发明人： YANAGIUCHI KOJI ,  MITSUNOBU SHIYOUICHI ,  IMAIZUMI YOSHIHIRO ,  OGAWA YUTAKA

    IPC分类号： C07D295/10

    摘要： PURPOSE:To obtain an aminoketone derivative having central muscular relaxing actions in high yield while suppressing the formation of by-products having an irritant smell by reacting a specific ketone with (para)formaldehyde and a specified amine (salt). CONSTITUTION:This method for producing a beta-aminoketone derivative (salt) expressed by formula III [R1 is a halogeno-lower alkyl; R2 is a lower alkyl; (n) is 0 or 1] is to react (A) a ketone expressed by formula I with (B) (para) formaldehyde and (C) an amine (salt) expressed by formula II in the presence of an acid or a base in a nonpolar solvent such as an aromatic hydrocarbon or a uniform mixed solvent consisting essentially of the solvent. For example, 2-methyl-1-(4-trmfluoromethylphenyl)-3-pyrrolidino-1-propanone (salt) is cited as the compound.