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Title:
PRODUCTION OF PENICILLANIC ANTIBIOTIC
Document Type and Number:
Japanese Patent JPH0327386
Kind Code:
A
Abstract:

PURPOSE: To obtain the title antibiotic of high purity extremely low in toxity in high yield by acylating an amino group of specific penicillanic acid by an acid halide in the presence of nicotin or the like.

CONSTITUTION: An amino group substd. at the 6-position of penicillanic acid wherein a carboxy group represented by formula I (wherein X is H or -OCOCH3) is protected (A) is acylated by an acid halide represented by formula II (wherein R is H or OH) (C) in the presence of a nicotin or isonicotine compd. as an acid receptor (B) to obtain the objective antibiotic represented by formula III. The acylation is pref. performed in the presence of compds. represented by formulae IV, V [wherein R1 is a group represented by formula VI or COOS (R2 and R3 are each H or 1-5C alkyl)].


Inventors:
VALCAVI UMBERTO (IT)
MAROTTA VITTORIO (IT)
FARINA PAOLO (IT)
Application Number:
JP12704190A
Publication Date:
February 05, 1991
Filing Date:
May 18, 1990
Export Citation:
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Assignee:
ISTITUTO BIOCHIMICO ITALIANO (IT)
International Classes:
A61K31/43; A61P31/04; C07D499/68; C07D499/00; C07D499/12; C07D499/64; C07D501/06; (IPC1-7): A61K31/43; C07D499/68
Domestic Patent References:
JPS51149296A1976-12-22
JPS5572194A1980-05-30
JPS5069092A1975-06-09
Attorney, Agent or Firm:
Aoki Akira (4 outside)