反应详情

3.0 g of 3-[4-(N-benzoylamidino)phenyl]-5-methanesulfonyloxymethyl-2-oxazolidinone [obtainable by reacting 4-(5-oxo-1,2,4-oxadiazolin-3-yl)aniline with 2,3-epoxypropan-1-ol to give N-[4-(5-oxo-1,2,4-oxadiazolin-3-yl)phenyl]-2,3-dihydroxypropylamine, reacting with diethyl carbonate in the presence of tert-butoxide to give 3-[4-(5-oxo-1,2,4-oxazolin-3-yl)phenyl]-5-hydroxymethyl-2-oxazolidinone, reductive cleavage of the 5-oxo-1,2,4-oxadiazoline group, reacting with benzoyl chloride and subsequently esterifying with methanesulfonyl chloride) dissolved in 10 ml of DMF, are added to a solution of 1.2 g of 4-ethoxycarbonylmethylpiperazine (“A”) in 20 ml of DMF, and the mixture is stirred at room temperature for 60 min. Removal of the solvent and the usual working up result in 3-[4-(N-benzoylamidino)phenyl]-5-(4-ethoxycarbonylmethylpiperazinomethyl)-2-oxazolidinone, m.p. 114°.