The aminoglycoside antibiotics are a valuable therapeutic class of antibiotics which include the kanamycins, gentamicins, streptomycins and the more recently discovered fortimicins. While the naturally produced parent antibiotics are, in themselves valuable entities, chemical modifications have been found to improve the activity, either intrinsic activity or activity against resistant strains, or reduce the toxicity of the parent antibiotics. And, because of the development of aminoglycoside resistant strains and inactivation of the parent antibiotics by R-mediated factors which can develop, the search for new entities continues.
One such entity has been discovered in the fortimicin family of antibiotics, 3-O-demethylfortimicin A. 3-O-demethylfortimicin B is also of interest because of its usefulness in preparing fortimicin derivatives. The 3-O-demethylfortimicins are disclosed in U.S. Pat. No. 4,124,756, issued November 7, 1979.
Previously known methods for producing O-demethylfortimicins have resulted in inefficient, slow synthesis and resulted in yields that are not satisfactory for commercial production, although satisfactory for laboratory synthesis. Thus there has been a need for improved processes to improve the yield of 3-O-demethylfortimicin production. The present invention provides one such method.
USPTO Backgrounds
USPTO Backgrounds