公开(公告)号：DE69718450T2

公开(公告)日：2003-11-20

申请号：DE69718450

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.

公开(公告)号：DE69718450D1

公开(公告)日：2003-02-20

申请号：DE69718450

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.

公开(公告)号：AT248144T

公开(公告)日：2003-09-15

申请号：AT96932825

申请日：1996-10-07

Applicant: KANEKA CORP

Inventor： UEDA YASUYOSHI ,  KANOU FUMIHIKO ,  KINOSHITA KOICHI ,  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 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.

公开(公告)号：ES2191200T3

公开(公告)日：2003-09-01

申请号：ES97943179

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.

公开(公告)号：DE69629661T2

公开(公告)日：2004-06-24

申请号：DE69629661

申请日：1996-10-07

Applicant: KANEKA CORP

Inventor： UEDA YASUYOSHI ,  KANOU FUMIHIKO ,  KINOSHITA KOICHI ,  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 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.

公开(公告)号：DE69629661D1

公开(公告)日：2003-10-02

申请号：DE69629661

申请日：1996-10-07

Applicant: KANEKA CORP

Inventor： UEDA YASUYOSHI ,  KANOU FUMIHIKO ,  KINOSHITA KOICHI ,  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 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.

公开(公告)号：HRP960449A2

公开(公告)日：1998-02-28

申请号：HRP960449

申请日：1996-10-03

Applicant: KANEKA CORP A COMPANY IN JAPAN

Inventor： UEDA YASUYOSHI ,  KANO FUMIHIKO ,  KINOSHITA KOICHI ,  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 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.

公开(公告)号：ES2206593T3

公开(公告)日：2004-05-16

申请号：ES96932825

申请日：1996-10-07

Applicant: KANEKA CORP

Inventor： UEDA YASUYOSHI ,  KANOU FUMIHIKO ,  KINOSHITA KOICHI ,  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 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.

公开(公告)号：IN185170B

公开(公告)日：2000-12-02

申请号：IN2193CA1998

申请日：1998-12-18

Applicant: KANEKA CORP

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

IPC: C07D207/28 ,  C07D207/36

公开(公告)号：SI9720012A

公开(公告)日：1998-12-31

申请号：SI9720012

申请日：1997-10-13

Applicant: KANEKA CORP

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

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

Abstract: A process of production of captopryl of the following formula (1), comprising exposure of the substrate compound of the following general formula (2) to the hydrolysis reaction in a water medium to remove the RCO group, and isolation of the product, where the hydrolysis reaction is led in a water medium at the presence of a strong acid at pH not above 1 and at a reaction temperature not below 40 degrees Celsius.