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.