Patent ID: 6281364
Filing Date: 2001-08-28
Classification: C07C,C07D,Y02P

Abstract:
Process for the preparation of a .gamma.-lactam of the general formula I and a salt thereof ##STR16##whereinR.sup.1 may represent H, (C.sub.1 -C.sub.8)-alkyl, (C.sub.2 -C.sub.8)-alkenyl, (C.sub.2 -C.sub.8)-alkynyl, (C.sub.2 -C.sub.8)-alkoxyalkyl, (C.sub.1 -C.sub.8)-acyl, which are optionally linear or branched and may be mono- or poly-substituted by halogens, by radicals having N, O, P, S atoms,(C.sub.3 -C.sub.7)-cycloalkyl, which may be saturated or unsaturated and mono- or poly-substituted by linear or branched (C.sub.1 -C.sub.8)-allyl, (C.sub.2 -C.sub.8)-alkenyl, (C.sub.2 -C.sub.8)-alkynyl, (C.sub.1 -C.sub.8)-acyl, (C.sub.1 -C.sub.8)-alkoxy, (C.sub.2 -C.sub.8)-alkoxyalkyl, by halogens, by radicals having N, O, P, S atoms, and/or may have hetero atoms selected from the group consisting of N, O, P, and S in the ring, aryl, heteroaryl, heteroaralkyl, wherein the rings just mentioned may optionally be mono- or poly-substituted by linear or branched (C.sub.1 -C.sub.8)-alkyl, (C.sub.2 -C.sub.8)-alkenyl, (C.sub.2 -C.sub.8)-alkynyl, (C.sub.1 -C.sub.8)-acyl, (C.sub.1 -C.sub.8)-alkoxy, (C.sub.2 -C.sub.8)-alkoxyalkyl, by halogens, by radicals having N, O, P, S atoms, and N-bonded amino acid or peptide residue,R.sup.2 may represent H, (C.sub.1 -C.sub.8)-alkyl, (C.sub.2 -C.sub.8)-alkenyl, (C.sub.2 -C.sub.8)-alkynyl, (C.sub.2 -C.sub.8)-alkoxyalkyl, which are optionally linear or branched and may be mono- or poly-substituted by halogens, by radicals having N, O, P, S atoms, (C.sub.3 -C.sub.7)-cycloalkyl, which may be saturated or unsaturated and mono- or poly-substituted by linear or branched (C.sub.1 -C.sub.8)-alkyl, (C.sub.2 -C.sub.8)-alkenyl, (C.sub.2 -C.sub.8)-alkynyl, (C.sub.1 -C.sub.8)-acyl, (C.sub.1 -C.sub.8)-alkoxy, (C.sub.2 -C.sub.8)-alkoxyalkyl, by halogens, by radicals having N, O, P, S atoms, and/or may have hetero atoms selected from the group consisting of N, O, P, and S in the ring, aryl, aralkyl, heteroaryl, heteroaralkyl, wherein the rings just mentioned may optionally be mono- or poly-substituted by linear or branched (C.sub.1 -C.sub.8)-alkyl, (C.sub.2 -C.sub.8)-alkenyl, (C.sub.2 -C.sub.8)-alkyl, (C.sub.1 -C.sub.8)-acyl, (C.sub.1 -C.sub.8)-alkoxy, (C.sub.2 -C.sub.8)-alkoxyalkyl, by halogens, and by radicals having N, O, P, S atoms,R.sup.3 may represent H, ClCO, (C.sub.1 -C.sub.8)-acyl, which may optionally be linear or branched, a C-bonded amino acid or a peptide residue or a conventional peptide-protecting groupwherein a derivative compound of the general formula II ##STR17##wherein R.sup.1, R.sup.2, R.sup.3 are as defined above and X represents a substituent selected from the group halogen and sulfonic acid ester, are cyclised to form a compound of the general formula I.