ACIC ADDITION SALT OF ARBEKACIN WITH (-)-CIS-1,2-EPOXYPROPYLPHOSPHONIC ACID, ITS PRODUCTION AND ANTIMICROBIAL AGENT

Japanese Patent JP3213687

B2

PROBLEM TO BE SOLVED: To produce the subject new acid addition salt having high antimicrobial activities and low nephrotoxicity by reacting arbekacin with (-)-cis-1,2-epoxypropylphosphonic acid in an aqueous solution and then freeze- drying the aqueous layer of the reactional solution.
SOLUTION: This new acid addition salt of an arbekacin represented by formula I [one to five of five groups X are groups, added to amino groups of the arbekacin and represented by formula II (M is H, Na+, K+, ammonium cation, etc.)] with (-)-cis-1,2-epoxypropylphosphonic acid (salt). Since the acid addition salt has high antimicrobial activities and low nephrotoxicity, it is useful as an antimicrobial agent, etc. The new acid addition salt is obtained by reacting a free salt of the arbekacin with a hemi-amine salt of (-)-cis-1,2- epoxypropylphosphonic acid in an amount of 1-5mol hemi-amine salt of the epoxypropylphosphonic acid, described above and based on 1mol arbekacin in an aqueous medium, producing the acid addition salt and then freeze-drying or concentrating and evaporating the aqueous layer after the reaction to dryness.

Seiji Shibahara
Usui Takayuki
Tetsutaro Niisato
Shinei Reihide
Shuichi Gomi
Shigeharu Inoue
Shinichi Kondo
Tomio Takeuchi

JP26182295A

October 02, 2001

October 09, 1995

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Foundation for Microbial Chemistry
Meiji Seika Co., Ltd.

C07H1/00; A61K31/665; A61K31/7028; A61K31/7034; A61K31/7036; A61K31/7042; A61K31/7048; A61P31/04; C07H15/234; C07H15/26; C07H17/04; (IPC1-7): C07H15/234; A61K31/7036; A61P31/04

JP55164696A
JP645574B2

Shigeru Yagita (2 outside)

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