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    12.
    发明专利
    未知

    公开(公告)号：AT231125T

    公开(公告)日：2003-02-15

    申请号：AT97943179

    申请日：1997-10-13

    Applicant: KANEKA CORP

    Inventor： KINOSHITA KOICHI ,  KANOU FUMIHIKO ,  OKUBO TAKAHIRO ,  UEDA YASUYOSHI

    IPC: A61K31/40 ,  A61K31/401 ,  A61P9/12 ,  C07D207/16

    Abstract: A process for producing captopril of the following formula (1) comprising subjecting a substrate compound of the following general formula (2) to hydrolysis reaction in aqueous medium to remove RCO group and isolating, said hydrolysis reaction in aqueous medium being conducted in the presence of a strong acid at pH not over 1 and a reaction temperature not below 40 DEG C.

    Process for producing high purity N-(D-alpha-methyl-beta-acylthiopropionyl) L-proline
    13.
    发明专利
    Process for producing high purity N-(D-alpha-methyl-beta-acylthiopropionyl) L-proline 未知

    公开(公告)号：IN182217B

    公开(公告)日：1999-02-06

    申请号：IN1754CA1996

    申请日：1996-10-04

    Applicant: KANEKA CORP

    Inventor： OEDA YASUYOSHI ,  KANO FUMIHIKO ,  KINOSHITA KOISHI ,  OKUBO TAKAHIRO

    IPC: A61K31/00 ,  C07D207/16 ,  A61K31/40

    Abstract: A highly convenient and efficient process for economically producing in a high yield high-quality captopril which is remarkably reduced in the content of impurities and has a high melting point and intermediates for synthesizing the same which contain only a small amount of precursors as impurities and have excellent qualities. The process comprises subjecting an acid halide and an L-proline to the Schotten-Baumann reaction and eliminating the impurities formed as the by-products in the form of the precursors represented by general formula (5) or (6) by treating, during or after the Schotten-Baumann reaction, the aqueous medium solution with active carbon or crystallization followed by deacylation. In the formula, R represents acyl and n represents an integer of from 2 to 4.

    PROCESS FOR PRODUCING N-(D-ALFA-METHYL-BETA-MERCAPTOPROPIONYL)-L-PROLINE AND INTERMEDIATES THEREOF
    14.
    发明专利
    PROCESS FOR PRODUCING N-(D-ALFA-METHYL-BETA-MERCAPTOPROPIONYL)-L-PROLINE AND INTERMEDIATES THEREOF 未知

    公开(公告)号：HU9801362A2

    公开(公告)日：1998-09-28

    申请号：HU9801362

    申请日：1996-10-07

    Applicant: KANEKA CORP

    Inventor： KANOU FUMIHIKO ,  KINOSHITA KOICHI ,  OKUBO TAKAHIRO ,  UEDA YASUYOSHI

    IPC: A61K31/00 ,  C07D207/16

    Abstract: A highly convenient and efficient process for economically producing in a high yield high-quality captopril which is remarkably reduced in the content of impurities and has a high melting point and intermediates for synthesizing the same which contain only a small amount of precursors as impurities and have excellent qualities. The process comprises subjecting an acid halide and an L-proline to the Schotten-Baumann reaction and eliminating the impurities formed as the by-products in the form of the precursors represented by general formula (5) or (6) by treating, during or after the Schotten-Baumann reaction, the aqueous medium solution with active carbon or crystallization followed by deacylation. In the formula, R represents acyl and n represents an integer of from 2 to 4.

    SIMPLE PROCESS FOR PRODUCING HIGH-QUALITY CAPTOPRIL
    15.
    发明专利
    SIMPLE PROCESS FOR PRODUCING HIGH-QUALITY CAPTOPRIL 未知

    公开(公告)号：CA2249543A1

    公开(公告)日：1998-04-23

    申请号：CA2249543

    申请日：1997-10-13

    Applicant: KANEKA CORP

    Inventor： OKUBO TAKAHIRO ,  KANO FUMIHIKO ,  UEDA YASUYOSHI ,  KINOSHITA KOICHI

    IPC: A61K31/40 ,  A61K31/401 ,  A61P9/12 ,  C07D207/16

    Abstract: An extremely simple process in which by-product impurities difficult to remove by purification are prevented from generating and high-quality captopril, represented by formula (1), can be inexpensively produced in a high yield. The process comprises hydrolyzing a substrate represented by general formula (2) (wherein R represents alkyl or alkoxyl) in an aqueous medium to eliminate the RCO group and then isolating the reaction product. The hydrolysis is conducted in the presence of a strong acid at 40 ~C or higher and a pH of 1 or lower.

    PROCESS FOR PRODUCING N-(D-ALPHA-METHYL-BETA-MERCAPTOPROPIONYL)-L-PROLINE AND ITS INTERMEDIATE
    16.
    发明专利
    PROCESS FOR PRODUCING N-(D-ALPHA-METHYL-BETA-MERCAPTOPROPIONYL)-L-PROLINE AND ITS INTERMEDIATE 未知

    公开(公告)号：SI9620018A

    公开(公告)日：1997-12-31

    申请号：SI9620018

    申请日：1996-10-07

    Applicant: KANEKA CORP

    Inventor： UEDA YASUYOSHI ,  KANOU FUMIHIKO ,  KINOSHITA KOICHI ,  OKUBO TAKAHIRO

    IPC: A61K31/00 ,  C07D207/16 ,  A61K31/40

    Abstract: A highly convenient and efficient process for economically producing in a high yield high-quality captopril which is remarkably reduced in the content of impurities and has a high melting point and intermediates for synthesizing the same which contain only a small amount of precursors as impurities and have excellent qualities. The process comprises subjecting an acid halide and an L-proline to the Schotten-Baumann reaction and eliminating the impurities formed as the by-products in the form of the precursors represented by general formula (5) or (6) by treating, during or after the Schotten-Baumann reaction, the aqueous medium solution with active carbon or crystallization followed by deacylation. In the formula, R represents acyl and n represents an integer of from 2 to 4.

    PROCESS FOR PRODUCING N-(D-.ALPHA.-METHYL-.BETA.-MERCAPTOPROPIONYL)-L-PROLINE AND INTERMEDIATES THEREOF
    17.
    发明专利
    PROCESS FOR PRODUCING N-(D-.ALPHA.-METHYL-.BETA.-MERCAPTOPROPIONYL)-L-PROLINE AND INTERMEDIATES THEREOF 未知

    公开(公告)号：CA2206396A1

    公开(公告)日：1997-04-10

    申请号：CA2206396

    申请日：1996-10-07

    Applicant: KANEKA CORP

    Inventor： KANOU FUMIHIKO ,  KINOSHITA KOICHI ,  UEDA YASUYOSHI ,  OKUBO TAKAHIRO

    IPC: A61K31/00 ,  C07D207/16

    Abstract: A highly convenient and efficient process for economically producing in a high yield high-quality captopril which is remarkably reduced in the content of impurities and has a high melting point and intermediates for synthesizing the same which contain only a small amount of precursors as impurities and have excellent qualities. The process comprises subjecting an acid halide an Lproline to the Schotten-Baumann reaction and eliminating the impurities formed as the by-products in the form of the precursors represented by general formula (5) or (6) by treating, during or after the Schotten-Baumann reaction, the aqueous medium solution with activated carbon or crystallization followed by deacylation. In the formulae, R1 represents acyl and n represents an integer of from 2 to 4.

    PROCESS FOR PRODUCING N-(D-alpha-METHYL-beta-MERCAPTOPROPIONYL)-L-PROLINE AND INTERMEDIATES THEREOF
    18.
    发明公开
    PROCESS FOR PRODUCING N-(D-alpha-METHYL-beta-MERCAPTOPROPIONYL)-L-PROLINE AND INTERMEDIATES THEREOF 失效
    PROCESS FOR N-（D-α-甲基-β-巯基丙酰基）-L-脯氨酸及其中间体的制备

    公开(公告)号：EP0802182A4

    公开(公告)日：2001-01-17

    申请号：EP96932825

    申请日：1996-10-07

    Applicant: KANEKA CORP

    Inventor： UEDA YASUYOSHI ,  KANOU FUMIHIKO ,  KINOSHITA KOICHI ,  OKUBO TAKAHIRO

    IPC: A61K31/00 ,  C07D207/16

    CPC classification number: C07D207/16

    Abstract: A highly convenient and efficient process for economically producing in a high yield high-quality captopril which is remarkably reduced in the content of impurities and has a high melting point and intermediates for synthesizing the same which contain only a small amount of precursors as impurities and have excellent qualities. The process comprises subjecting an acid halide an L-proline to the Schotten-Baumann reaction and eliminating the impurities formed as the by-products in the form of the precursors represented by general formula (5) or (6) by treating, during or after the Schotten-Baumann reaction, the aqueous medium solution with activated carbon or crystallization followed by deacylation. In the formulae, R1 represents acyl and n represents an integer of from 2 to 4.

    SIMPLE PROCESS FOR PRODUCING HIGH-QUALITY CAPTOPRIL
    20.
    发明公开
    SIMPLE PROCESS FOR PRODUCING HIGH-QUALITY CAPTOPRIL 失效
    生产高品质工艺简单CAPTROTRIL

    公开(公告)号：EP0889031A4

    公开(公告)日：2000-03-22

    申请号：EP97943179

    申请日：1997-10-13

    Applicant: KANEKA CORP

    Inventor： KINOSHITA KOICHI ,  KANOU FUMIHIKO ,  OKUBO TAKAHIRO ,  UEDA YASUYOSHI

    IPC: A61K31/40 ,  A61K31/401 ,  A61P9/12 ,  C07D207/16

    CPC classification number: C07D207/16

    Abstract: An extremely simple process in which by-product impurities difficult to remove by purification are prevented from generating and high-quality captopril, represented by formula (1), can be inexpensively produced in a high yield. The process comprises hydrolyzing a substrate represented by general formula (2) (wherein R represents alkyl or alkoxyl) in an aqueous medium to eliminate the RCO group and then isolating the reaction product. The hydrolysis is conducted in the presence of a strong acid at 40 °C or higher and a pH of 1 or lower.

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