PROCESS FOR PRODUCTION OF NEW DERIVATIVES OF 1-SULPHA-2-AZETIDINON AND MEDICAL PREPARATIVES CONTAINING THESE COMPOUNDS

摘要

A 1-sulfo-2-oxoazetidine derivative of the formula wherein R is -COQ<0> (Q<0> is an amino group which may optionally be protected or substituted), -COQ<5> (Q<5> is a hydroxyl group which may optionally be protected), -(CH2)na- R<4a> (n is an integer of 1 to 3; R<4a> is a hydrogen atom or a carbamoylamino, N-sulfocarbamoylamino, carbamoyl, carbamoyloxy, N-sulfocarbamoyloxy, haloalkylcarbonylcarbamoyloxy, alkylsulfonyloxy, pyridinio, alkoxy, alkylsulfinyl, alkylsulfonyl, halogenoalkylcarbonyloxy, hydroxyl, alkoxycarbonyl, acyloxy, 1-alkoxyiminoalkyl, alkylcarbony or acylamino group) or a nitrogen-containing heterocyclic group; R<1> is an amino group which may optionally be acylated or protected; and X is a hydrogen atom or a methoxy group, or a salt or ester thereof, and methods of producing said compound (I) which may be shown as follows wherein the symbols have the same meanings as respectively defined above, and intermediates for preparing the compound (I) and methods of producing them. The compound (I) has improved antimicrobial and beta -lactamase-inhibitory activities and is of value as drugs for human beings and domesticated animals.