- Synthesis method of plazomicin or salt of plazomicin
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The invention relates to a synthesis method of plazomicin or salt of the plazomicin. Specifically, the synthesis method uses a compound 6 as a raw material, six steps of exchange reaction, amino protection reaction, PNZ protecting group removal reaction, reductive amination reaction, degradation reaction and amino-protecting group removal reaction are sequentially performed, and finally the plazomicin or the salt of the plazomicin is prepared. The details of specific steps are described in the description. The synthesis method has the advantages of being few in steps, high in reaction selectivity, simple in operation, low in material cost and the like, and is very suitable for industrial application.
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Paragraph 0026-0029
(2020/01/14)
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- Preparation method of pradimicin antibiotics
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The invention provides a preparation method of pradimicin antibiotics, belonging to the field of pharmaceutical chemistry and pharmaceutical engineering. The preparation method comprises the followingsteps: freeing of sisomicin, protection of amino, selective introduction of protective groups, deprotection of amino, and the like. The preparation method is suitable for industrial production, thushaving good market prospects.
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Paragraph 0081-0083; 0125; 0128; 0148; 0151; 0154; 0160
(2019/01/08)
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- TREATMENT OF URINARY TRACT INFECTIONS WITH ANTIBACTERIAL AMINOGLYCOSIDE COMPOUNDS
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A method for treating a urinary tract infection in a mammal in need thereof is disclosed, the method comprising administering to the mammal an effective amount of an antibacterial aminoglycoside compound.
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Page/Page column 51
(2010/12/17)
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- ANTIBACTERIAL AMINOGLYCOSIDE ANALOGS
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Compounds of structure (I): having antibacterial activity are disclosed, including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein Q1, Q2, Q3, R8 and R9 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
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Page/Page column 48
(2009/06/27)
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- Process for the preparation of purified aminoglycoside antibiotics
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The invention relates to an improved process for the isolation and purification of aminoglycoside antibiotics of Formula (I) as defined herein combining selective lipophilization of the compound of Formula (I) in the crude product obtained by fermentation with controlled liquid/liquid extraction.
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- Semisynthetic Aminoglycoside Antibacterials. Part 9. Synthesis of Novel 1- and 3-Substituted and 1- and 3-epi-Substituted Derivatives of Sisomicin and Gentamicin from the 1- and 3-Oxo-derivatives
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The conversion of selectively protected gentamicin and sisomicin derivatives into the 1- and 3-oxo-compounds by reaction with 3,5-di-t-butyl-1,2-benzoquinone is described.By application of suitable reductive techniques these oxo-aminoglucosides have been converted into novel 1- and 3-epi-, 1- and 3-deamino-1- and -3-hydroxy-, 1- and 3-deamino-1- and -3-epi-hydroxy, and 1-deamino-derivatives.A study of the 13C n.m.r. parameters of the 1-epi- and 1-deamino-derivatives has led to the assignment of novel solution conformations for these new aminoglycosides.
- Boxler, Dena L.,Brambilla, Raymond,Davies, D. Huw,Mallams, Alan K.,McCombie, Stuart W.,at al.
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p. 2168 - 2185
(2007/10/02)
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- Semisynthetic aminoglycoside antibacterials. 6. Synthesis of sisomicin, antibiotic G-52, and novel 6'-substituted analogues of sisomicin from aminoglycoside 66-40C
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The discovery of aminoglycoside 66-40C, a novel dimeric, unsaturated imine produced by Micromonospora inyoensis, afforded a versatile intermediate for the synthesis of a variety of sisomicin analogues modified at the 6' position. The conversion of 66-40C into sisomicin, antibiotic G-52, and a series of novel 6'-substituted analogues of sisomicin is described, and the biological activity of the products is discussed.
- Davies,Mallams,Counelis,Loebenberg,Moss Jr.,Waitz
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p. 189 - 193
(2007/10/05)
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- Aminoglycoside 66-40C, method for its manufacture, method for its use as an intermediate in the preparation of known antibiotics and novel antibacterials
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Aminoglycoside 66-40C, a minor product produced by the fermentation of Micromonospora inyoensis, is separated from said fermentation mixture, and is used as an intermediate in preparing the known antibiotic, sisomicin, as well as 6' -N-alkylsisomicins having antibacterial activity. Claimed are Aminoglycoside 66-40C as well as 6' -N-t-alkylsisomicins having a tertiary carbon bonded to the 6' -nitrogen.
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- Di-N-alkylaminoglycosides, methods for their manufacture and novel intermediates useful therein, method for their use as antibacterial agents and pharmaceutical compositions useful therefor
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1,2'-di-N-4,6-di-O-(aminoglycosyl)-1,3-diaminocyclitols and 1,6'-di-N-alkyl-4,6-di-O-(aminoglycosyl)-1,3-diaminocyclitols and their acid addition salts are valuable as antibacterial agents. Also disclosed are 2'-N-alkyl-4,6-di-O-(aminoglycosyl)-1,3-diaminocyclitol antibacterial agents which are also useful as intermediates in the preparation of the 1,2'-di-N-alkyl-4,6-di-O-(aminoglycosyl)-1,3-diaminocyclitols. Preferred compounds of this invention include 1,2'-di-N-ethylsisomicin and 1,6'-di-N-ethylsisomicin.
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