2,3-dioxopiperazine derivatives

Details 2,3-dioxopiperazine derivatives 2,3-dioxopiperazine derivatives

C - Chemistry, Metallurgy

07

D

260/266.1, 260/2

C07D 241/08 (2006.01)

Patent

CA 1078384

ABSTRACT OF THE DISCLOSURE The present invention provides 2,3-dioxopiperazine deri- vatives useful as intermediates of penicillins and cephalosporins, and having the formula Image (I) wherein R represents .alpha.-amino acid residue represented by the formula Image , wherein R5 is an alkyl, cycloalkyl, cyclo- alkenyl, cycloalkadienyl, aryl, aralkyl, aryloxy, alkylthioalkyl or heterocyclic group which may be substituted by a substituent selected from halogen, hydroxyl, nitro, alkyl, alkoxy, alkylthio, acyl or alkylsulfonylamino; R6 represents a hydrogen atom; and R5 and R6 together with a common carbon atom may form a cyclo- alkyl, cycloalkenyl or cycloalkadienyl ring, R2 represents a hydrogen atom or an alkyl group, A represents an alkyl, alkenyl, alkadienyl, cycloalkyl, aryl or aralkyl group which may be sub- stituted by a substituent selected from halogen, hydroxyl, alkyl, alkoxy, alkylthio, nitro, cyano, dialkylamino, cyclic amino, acyl, carboxyl or alkoxycarbonyl, n represents 0 or 1, and B represents a carboxyl group, a salt thereof or a reactive deriva- tive of a carboxyl group selected from the residues of acid halide, acid anhydride, mixed acid anhydride with organic or inorganic acids,active ester, active acid amide and acid cyanide, and when n represents O, B represents only a reactive derivative of a car- boxyl group selected from the residues of acid halide, acid an- hydride, mixed acid anhydride with organic or inorganic acids active ester, active acid amide and acid cyanide.

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