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.
ASAI HIKARI
AZEYANAGI SATORU
JPS52156896A | 1977-12-27 | |||
JPS5039679A | 1975-04-11 | |||
JPS4886889A | 1973-11-15 | |||
JPS4972286A | 1974-07-12 | |||
JPS4985088A | 1974-08-15 |
Next Patent: 7-(2-(CHROMONE-3-CARBOXAMIDE)-2-PHENYLACETAMIDE) CEPHEM DERIVATIVE AND ITS PREPARATION