摘要 |
PURPOSE:To obtain the titled compound useful as an intermediate for antibacterial substance in high yield without using water and catalyst, by heating an acylaminocarbamoyloxymethylcephalosporanic acid and a specific thiol in the presence of a solvent under an anhydrous condition. CONSTITUTION:(A) A 7-acylamino (or amino)-3-carbamoyloxymethyl- cephalosporanic acid shown by formula I (R is H or acyl; X is H or alkoxy), or a derivative at its carboxyl group or a salt thereof [e.g. 7beta-(D-5'-N-isobutoxycarbonylamino-5'-carboxylvaleramido)-7alpha-met hoxy-3-carbamoyloxyme thyl-3-cephem-4-carboxylic acid, etc.] is heated with (B) a thiol (e.g. 1-methyl-5- mercaptotetrazole, etc.) shown by the formula R''SH (R'' is (substituted) heterocy clic or group shown by formula II) under an anhydrous condition in the presence of 5 times as much solvent as the component A to give the aimed compound shown by formula III.
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