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Title:
PRODUCTION OF SIALIC ACID DERIVATIVE
Document Type and Number:
Japanese Patent JPH1059994
Kind Code:
A
Abstract:

To obtain a sialic acid derivative for remedying disturbance of memory involved in senile dementia, by reaction of a specific carboxyl-bearing sialic acid derivative with an amine derivative in the presence of a phosphorus- based condensation agent and an organic base.

This sialic acid derivative of formula III is obtained easily at low cost in high yield and purity by amidation between a carboxyl-bearing sialic acid derivative of formula I [R2 is H or an acyl; R3 is a 1-15C alkyl or (substituted) aryl group-substituted 1-8C alkyl; R5 is acetamido group or alkyl group-substituted amino group; X is O or S] and an amine derivative of formula II (R1 is a steroid compound residue; R4 is H or a 1-4C alkyl) (e.g. aminocholestane) in the presence of a phosphorus-based condensation agent (e.g. phosphorus oxychloride) and an organic base (e.g. triethylamine). This sialic acid derivative is useful as e.g. a medicine for remedying disturbance of memory involved in senile dementia including Alzheimer's disease.


Inventors:
IWAMURA HIROSHI
SHIRASAKA TADASHI
Application Number:
JP21369096A
Publication Date:
March 03, 1998
Filing Date:
August 13, 1996
Export Citation:
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Assignee:
MITSUBISHI CHEM CORP
International Classes:
C07H15/04; (IPC1-7): C07H15/04
Attorney, Agent or Firm:
Hasegawa Moji