MANUFACTURE OF CEPHEM DERIVATIVE

A novel process for preparing cephem derivatives is characterized in that an acylating agent, wherein R is benzotriazolyl, pyridyl, succinimidyl or phthalimidyl, and n is 1 or 2, is used in esterifying 2-(2-amino-thiazol-4-yl)-2-syn-methoxyiminoacetic acid: The ester thus obtained is then reacted wi...

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Hauptverfasser: KIN HOUCHIN, RI KANJIYUN, KIN KANCHIYUU, RI TETSUKAI
Format: Patent
Sprache:eng
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Zusammenfassung:A novel process for preparing cephem derivatives is characterized in that an acylating agent, wherein R is benzotriazolyl, pyridyl, succinimidyl or phthalimidyl, and n is 1 or 2, is used in esterifying 2-(2-amino-thiazol-4-yl)-2-syn-methoxyiminoacetic acid: The ester thus obtained is then reacted with 7-aminocephalosporanic acid of formula III below to give a desired cephem derivative. Use of such an acylating agent eliminates the awkward steps of protection and then deprotection of the amino radical of the starting organic acid. wherein R' is H or alkali metal and R is H, acetoxymethyl or heterocyclicthiomethyl.