1-isothiazolidinone derivatives of azetidine-2-one,...

C - Chemistry – Metallurgy – 07 – D

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C07D 417/04 (2006.01) A61K 31/425 (2006.01) C07D 417/14 (2006.01)

Patent

CA 2256096

The object of the present invention are novel compounds of azetidine-2-one substituted in 1-position with different isothiazolidinone radicals, as analogons of a beta-lactam structure, of the general formula I Image wherein R1 represents a hydrogen or a halo atom, R2 represents a hydrogen or a halo atom or a phthalimide group, R3 represents a hydrogen or a halo atom, R4 represents a hydrogen or a halo atom, R5 represents a hydrogen atom, a lower linear or branched alkyl, aryl or aralkyl, or a radical containing a heterocycle with one or more heteroatoms, such as isoxazolyl or pyrazolyl, and n is 0, 1 or 2. The usefulness of these compounds as intermediates for the preparation of novel beta-lactam analogons or active substances in formulations for antimicrobial therapy is given.

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