U.S. patents available from 1976 to present.
U.S. patent applications available from 2005 to present.

Novel process for the synthesis of amikacin

Patent 4902790 Issued on February 20, 1990. Estimated Expiration Date: Icon_subject February 20, 2007. Estimated Expiration Date is calculated based on simple USPTO term provisions. It does not account for terminal disclaimers, term adjustments, failure to pay maintenance fees, or other factors which might affect the term of a patent.

Patent References

Process of selectively blocking amino functions in aminoglycosides using transition metal salts and intermediates used thereby
Patent #: 4136254
Issued on: 01/23/1979
Inventor: Nagabhushan ,   et al.

Aminoglycoside antibiotic compounds
Patent #: 4230847
Issued on: 10/28/1980
Inventor: Nagabhushan ,   et al.

Production of a selectively protected N-acylated derivative of an aminoglycosidic antibiotic
Patent #: 4297485
Issued on: 10/27/1981
Inventor: Umezawa ,   et al.

2-N-Acylated and 2-N-alkylated derivatives of 4-O-substituted-2-deoxystreptamine aminoglycosides and process
Patent #: 4424344
Issued on: 01/03/1984
Inventor: Kirst ,   et al.

2'-N-Acylated and 2'-N-alkylated derivatives of 4-O-substituted-2-deoxystreptamine aminoglycosides Patent #: 4468513
Issued on: 08/28/1984
Inventor: Kirst ,   et al.

Inventors

Assignee

Application

No. 914451 filed on 10/02/1986

US Classes:

536/13.7, Kanamycin or derivative536/13.8Carbonyl bonded directly to kanamycin nitrogen

Examiners

Primary: Griffin, Ronald W.
Assistant: Webber, Pamela S.

Attorney, Agent or Firm

International Classes

C07H 015/20
C07H 015/22

Foreign Application Priority Data

1985-10-10 IT

Abstract

A novel process for the synthesis of amikacin starting from kanamycin A protected at the positions 3 and 6' is described comprising the reaction of kanamycin A with a salt of a bivalent metal cation selected from zinc, nickel, iron, cobalt, manganese, copper and cadmium in the presence of water as the solvent or co-solvent followed by the in situ reaction of the resulting complex with a reactive derivative of L-amino-2-hydroxy-butyric acid, removal of the metal cation of the protecting groups and purification of the thus obtained raw product. The acylation under these conditions is extremely selective.

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