| 摘要 |
<p>PURPOSE:A reaction product from a specific aminothiazoliminoacetic acid amide and boron trifluoride is allowed to react with a cephem compound under specific conditions to enable industrially simple and high-efficiency production of the title compound which is used as an antibacterial. CONSTITUTION:(A) A compound resulting from reaction between a compound of formula (R<1> is lower alkyl)(syn-isomer) such as 2-(2-aminothiazol-4-yl)-2-(syn)- methoxyiminoacetic acid amide and boron trifluoride or its complex is allowed to react with a compound of formula II R<2a> is carboxyl-protecting group; R<3> is (substituted) heterocyclic group bonding via C-N bond to exomethylene in the 3-position] in an organic solvent at -50-0 deg.C. Then, the reaction is continued in a mixed solvent of water and an organic solvent at a pH of 4.5-6.7 at 0-50 deg.C, when needed, the carboxyl is deprotected or converted into its salt to give the objective compound (syn-isomer) or formula III (R<2> is H, carboxyl- protecting group).</p> |
