摘要 |
<p>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(R<1> is amino or substituted amino; R<2> 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 -20-+80 deg.C for 0.5-5hr, 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.</p> |