摘要 |
alpha -Phosphono-(3 beta -amino or 3 alpha -alkylazetidin-2-one-1-yl)acetic acids and esters thereof are provided via cyclization process comprising the reaction of a beta -hydroxy phosphonomethyl acid amide with triphenylphosphine-di-(C1-C3 alkyl)azodicarboxylate in an anhydrous aprotic solvent. The azetidinones obtained are useful intermediates to carbapenems and carbacephems and monocyclic antibacterials, e.g., alpha -(dialkylphosphono)-[[3 beta -[2-(2-aminothiazol-4-yl)-2-(syn)methoxyiminoace tylamino]azetidin-2-one-1-yl]]acetic acid and pharmaceutically acceptable salts thereof. |