Organic compounds -- part of the class 532-570 series – Organic compounds – Carbohydrates or derivatives
Patent
1982-09-07
1984-08-28
Brown, Johnnie R.
Organic compounds -- part of the class 532-570 series
Organic compounds
Carbohydrates or derivatives
536 133, 536 136, 536 166, 424180, C07H 1522
Patent
active
044685122
ABSTRACT:
Zinc salts are used to effect the regio-selective acylation and alkylation of the 1-amino group of 4-O-substituted-2-deoxystreptamine-containing aminoglycosides. The 1-N-substituted derivatives of apramycin, 3'-hydroxyapramycin, certain .alpha. or .beta.-(lower alkyl)aprosaminides and certain .alpha. or .beta.-(substituted lower alkyl)-aprosaminides are new. The 1-N-substituted-4-O-substituted-2-deoxystreptamine aminoglycosides produced by the process of this invention are antibacterial agents.
REFERENCES:
patent: 4002608 (1977-01-01), Wright et al.
patent: 4166114 (1979-08-01), Igarashi
patent: 4169197 (1979-09-01), Magerlein
patent: 4199570 (1980-04-01), Igarashi et al.
patent: 4200628 (1980-04-01), Igarashi et al.
patent: 4230847 (1980-10-01), Nagabhushan et al.
patent: 4297485 (1981-10-01), Umezawa et al.
patent: 4360665 (1982-11-01), Kirst
patent: 4362866 (1982-12-01), Igarashi et al.
patent: 4380625 (1983-04-01), Stadler et al.
Y. Abe et al., "Aminoglycoside Antibiotics. XIV. etc.", J. Antibiotics (Tokyo), 34, 1434 (1981).
J. Davies and S. O'Connor, "Enzymatic Modification of Aminoglycoside Antibiotics etc.", Antimicrob. Agents Chemother., 14, 69, (1978).
S. O'Connor et al., "Apramycin, a Unique Aminocyclitol Antibiotic", J. Org. Chem., 41, 2087 (1976).
H. A. Kirst, B. A. Truedell, and J. E. Toth, "Control of Site-Specific Substitution, etc.", Tet. Letters, vol. 22, p. 295 (1981, approximately the 1st quarter of the year).
Partial Program of 20th Interscience Conference on Antimicrobial Agents and Chemotherapy (Sep. 23, 1980).
Kirst Herbert A.
Truedell Brenda A.
Brown Johnnie R.
Eli Lilly and Company
Harrison Nancy J.
Steinhardt Paul C.
Whale Arthur R.
LandOfFree
1-N-Acylated and 1-N-alkylated derivatives of 4-O-substituted-2- does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with 1-N-Acylated and 1-N-alkylated derivatives of 4-O-substituted-2-, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and 1-N-Acylated and 1-N-alkylated derivatives of 4-O-substituted-2- will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-878119