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Title:
MANUFACTURING METHOD AND PURIFICATION METHOD OF (S)-2-(4-METHOXY-BENZENESULFONYLAMINO)-N-(METHOXYPOLYETHOXYETHYL)-SUCCINAMIC ACID-t-BUTYL ESTER
Document Type and Number:
Japanese Patent JP2011057584
Kind Code:
A
Abstract:

To provide a manufacturing method and a purification method, which are industrially advantageous, high yielding and safe, of high-purity (S)-2-(4-methoxy-benzenesulfonylamino)-N-(methoxypolyethoxyethyl)-succinamic acid-t-butyl ester as an intermediate required for the manufacture of an inhibitor of thrombin, a blood coagulation protease.

(S)-2-(4-methoxy-benzenesulfonylamino)-succinic acid-1-t-butyl ester is caused to react with a specific chloroformate ester in the presence of an organic solvent and a base to form a mixed acid anhydride, which is then caused to react with a specific polyethylene glycol-aminoethyl-methyl ether to give (S)-2-(4-methoxy-benzenesulfonylamino)-N-(methoxypolyethoxyethyl)-succinamic acid-t-butyl ester represented by formula (1) (wherein n is an integer of 20-200) without using expensive HBTU.


Inventors:
MAEHARA AKIRA
NOJIMA AKIKO
Application Number:
JP2009206800A
Publication Date:
March 24, 2011
Filing Date:
September 08, 2009
Export Citation:
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Assignee:
TAOKA CHEMICAL CO LTD
International Classes:
C07C303/40; C07C303/44; C07C311/29