Title:
PREPARATIVE METHOD OF CEPHALOSPORANIC ACID DERIVATIVE
Document Type and Number:
Japanese Patent JPS56135489
Kind Code:
A
Abstract:
PURPOSE: A 7-aminocephalosporanic acid derivative is made to react with a novel active ester to safely produce the titled derivative used as antibiotic against grampositive and -negative bacteria in high yield.
CONSTITUTION: The reaction between a 7-aminocephalosporanic acid derivative or its salt of formula I (R is halogen, azide, acetoxy) and mandelic pyridine-N-oxide- 2-yl thiol ester is conducted, preferably at a molar ratio of 1:(1W2) in a solvent of DMF at 40°W80°C to produce the objective cephalosporanic acid derivative of formula III. The compound of formula II is novel and obtained, e.g., by reaction of pyridine-N-oxide-2-thiol of formula IV or its derivative with madelic acid or its derivative in a solvent at -50°W+100°C.
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Inventors:
MURAKAMI MASAHIRO
KOBAYASHI MASATERU
YAMAMOTO KIMIYO
SHIBUYA KAZUYUKI
KOBAYASHI MASATERU
YAMAMOTO KIMIYO
SHIBUYA KAZUYUKI
Application Number:
JP3750180A
Publication Date:
October 22, 1981
Filing Date:
March 26, 1980
Export Citation:
Assignee:
ASAHI CHEMICAL IND
International Classes:
C07D501/06; (IPC1-7): C07D501/06
Previous Patent: JPS56135488
Next Patent: MANUFACTURE OF 7-(D(-)-ALPHA-AMINO-P- HYDROXYPHENYLACETAMIDE)DESACETOXYCEPHALOSPORANIC ACID
Next Patent: MANUFACTURE OF 7-(D(-)-ALPHA-AMINO-P- HYDROXYPHENYLACETAMIDE)DESACETOXYCEPHALOSPORANIC ACID