- PROCESS TO PREPARE PROPYLENE AMINES AND PROPYLENE AMINE DERIVATIVES
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The present invention relates to a process to prepare propylene amines of the formula NH2-(A-NH-)pR, wherein R is a hydrogen atom or an alkyl group, p is at least 1 when R is an alkyl group, and at least 2 when R is a hydrogen atom, or derivatives or precursors thereof wherein one or more units -NH-A-NH-may be present as a cyclic urea unit. (I) or a cyclic unit (ll) or between two units –NH-A-NH-a carbonyl bond is present, each unit –A-can be independently an alkylene unit and at least one unit –A-is a -C3H6- unit, wherein each -C3H6- unit can be linear or branched, by reacting (i) at least one of a hydroxy-functional compound chosen from the alkanolamine-functional compounds, and dihydroxyalkylene compounds, with (ii) an amine-functional compound,in the presence of (iii) a carbon oxide delivering agent, wherein at least one of the alkanolamine-functional compound, the amine-functional compound and/or the carbon oxide delivering agent contains at least one alkylene unit (A) that is a propylene unit
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Page/Page column 35; 39; 40
(2019/02/25)
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- Inhibitors of aminoglycoside 6'-N-acetyltransferases, compositions and uses thereof
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The present invention relates to inhibitors of aminoglycoside 6''-N-acetyltransferases of Formula I: R-X-Y-Z Formula I wherein: R is selected from the group consisting of: R1 is selected from the group consisting of OH and R2 is selected from the group consisting of OH and R3 is selected from the group consisting of NH2 and OH; R4 is selected from the group consisting of NH2 and R5 is selected from the group consisting of OMe, OEt OPr, and O-iPr; X is selected from the group consisting of NH and O; Y is selected from the group consisting of: R6 is selected from the group consisting of OH, CH3, and OCH3; n is an integer ranging from 1 to 10; and Z is selected from the group consisting of: and R7 is selected from the group consisting of OH, OMe, OEt OPr, O-iPr, O-tBu and
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Page/Page column 17
(2008/06/13)
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- Synthesis and structure-activity relationships of truncated bisubstrate inhibitors of aminoglycoside 6′-N-acetyltransferases
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Truncated aminoglycoside-coenzyme A bisubstrate analogues were efficiently prepared using a convergent approach where the amine and the thiol are coupled in one pot with the addition of a linker, without the need for protecting groups. These derivatives were tested for their effect on the activity of the resistance-causing enzyme aminoglycoside 6′-N-acetyltransferase Ii, and key structure-activity relationships are reported. Moreover, one of the inhibitors is able to block aminoglycoside resistance in cells expressing this enzyme.
- Gao, Feng,Yan, Xuxu,Shakya, Tushar,Baettig, Oliver M.,Ait-Mohand-Brunet, Samia,Berghuis, Albert M.,Wright, Gerard D.,Auclair, Karine
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p. 5273 - 5281
(2007/10/03)
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- NUCLEOPHILIC CLEAVAGE AND FORMATION OF SATURATED HETEROCYCLES. XII. REACTIVITY OF SMALL HETEROCYCLES TOWARD AMINOLYSIS AND HYDROLYSIS
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The cleavage of four-membered saturated heterocycles proceeds via a more product-like transition state than that of three-membered rings.General acid catalysis is characteristic of oxygen heterocycles, but in the case of nitrogen heterocycles catalysis is specific.The reactivity of amines in the cleavage of azetidines is linearly dependent on their pKa values, primary and secondary amines comprising separate reaction series.
- Bobylev, V. A.,Veselkov, N. Yu.,Dalin, A. R.,Sharikov, F. Yu.
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p. 1700 - 1713
(2007/10/02)
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