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Title:
PREPARATION OF 3-SUBSTITUTED THIOMETHYLCEPHALOSPORIN DERIVATIVE
Document Type and Number:
Japanese Patent JPS5818388
Kind Code:
A
Abstract:

PURPOSE: To prepare the titled compound useful as a synthetic intermediate of cefatrizine (a medicine), in high yield, by reacting a 3-halomethyl-cephalosporin derivative or its 1-sulforxide with 5-mercapto-1, 2, 3-triazole.

CONSTITUTION: 3-Halomethylcephalosporin derivative of formulaI(R1 is amino or substituted amino; R2 is H or carbocy-protecting group; X is halogen) or its 1-sulfoxide is made to react with 5-mercapto-1, 2, 3-triazole or its metal salt or the hydrate of the metal salt, in an organic solvent such as benzene, acetone, methanol, etc. at -20W+80°C for 0.5W5hr, if necessary in the presence of a base such as ammonia, triethylamine, etc. to obtain the 3-(1, 2, 3-triazol-5-ylthiomethyl)-cephaloshorin derivative of formula II or its 1-sulfoxide.


Inventors:
SHIMIZU KUNIMITSU
ASAI HIKARI
AZEYANAGI SATORU
Application Number:
JP11709281A
Publication Date:
February 02, 1983
Filing Date:
July 28, 1981
Export Citation:
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Assignee:
BANYU PHARMA CO LTD
International Classes:
C07D501/04; C07D501/36; (IPC1-7): C07D501/04
Domestic Patent References:
JPS52156896A1977-12-27
JPS5039679A1975-04-11
JPS4886889A1973-11-15
JPS4972286A1974-07-12
JPS4985088A1974-08-15