C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 503/00 (2006.01) C07D 498/047 (1990.01)
Patent
CA 2092330
Novel alkylenediammonium diclavulanate derivatives, process for the preparaiton thereof and use thereof. A novel process for the preparation of calvulanic acid and pharmaceutically acceptable salts thereof, such as potassium clavulanate, is described. According to the novel process, crude clavulanic acid is reacted with substituted alkylenediamines of the formula Image wherein the substituents R1, R2, R3 and R4 denote - a hydrogen atom, - a straight-chain or branched-chain alkyl group having 1 to 8 carbon atoms or - a hydroxyalkyl group having 2 to 4 carbon atoms and NR1R2 and/or NR3R4 jointly denote a heterocylic ring having 3 to 6 methylene groups bound to a nitrogen atom, one of these groups being optionally substituted by an oxygen or a sulphur atom or by an imino group and R5 denotes a hydrogen atom, or a methyl group and n denotes an integer from 1 to 3, to produce novel alkylenediammonium diclavulanates of the formula 16 Image The obtained compounds are optionally isolated and converted with alkali alkanoates, such as potassium 2-ethylhexanoate in isopropanol, to potassium clavulanate. Because of their high inhibitory action against beta-lactamases and because of a significant synergistic action in combination with the beta-lactam antibiotics from the group of penicillins and cephalosporins, clavulanic acid and pharmaceutically acceptable salts thereof are valuable compounds for the preparation of galenic compositions, which are active in the treatment of infectious diseases induced by numerous gram-positive and gram-negative microorganisms.
Goudreau Gage Dubuc
Lek Pharmaceuticals D.d.
Ljubljana Lek Tovarna Farmacevtskih In Kemicnih Izdelkov,d.d.
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