Alkylenediammonium diclavulanate derivatives, a process for the

Details Alkylenediammonium diclavulanate derivatives, a process for the Alkylenediammonium diclavulanate derivatives, a process for the

1993-03-25

1994-05-10

Berch, Mark L.

Organic compounds -- part of the class 532-570 series

Organic compounds

Unsubstituted hydrocarbyl chain between the ring and the -c-...

A61K 3142, C07D498047, C07B 6302

Patent

active

053108981

ABSTRACT:
A novel process for the preparation of calvulanic acid and pharmaceutically acceptable salt thereof, such as potassium clavulanate, is described. According to the novel process, crude clavulanic acid, which is present in the form of an extract in an organic solvent, such as ethyl acetate, the extract having been obtained in known manner upon fermentation with a calvulanic acid producing microorganism, is reacted with substituted alkylenediamines of the formula II ##STR1## wherein the substituents R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 and n have the meanings as defined in claim 1, e.g. with N,N'-diisopropylethylenediamine, to the novel alkylenediammonium diclavulanates of the formula I ##STR2## wherein the substituents R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 and n have the meanings as defined in claim 1, e.g. to N,N'-diisopropylethylenediammonium diclavulanate. The obtained compounds of the formula I 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 grampositive and gram-negative microorganisms.

REFERENCES:
patent: 4454069 (1984-06-01), Cook et al.
patent: 4525353 (1985-06-01), Cole
patent: 4647659 (1987-03-01), Cook et al.
patent: 4650795 (1987-03-01), Liberman
An Encyclopedia of Chemicals, Drugs, and Biologicals, The Merck Index, 11th Edition, 1989, Nos. 1072, 7037, 7047.

Affiliated with

Also associated with

Rating

Alkylenediammonium diclavulanate derivatives, a process for the does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Alkylenediammonium diclavulanate derivatives, a process for the , we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Alkylenediammonium diclavulanate derivatives, a process for the will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-2413207