- METHOD FOR SYNTHESIZING AMINES
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The invention relates to a process for preparing certain amines, wherein, in a first step, a corresponding amino alcohol is reacted with a suitable carbonyl compound and then, in a second step, the intermediate obtained in the first step is reacted with a suitable amine component to form the desired amine.
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Paragraph 0278-0280
(2021/05/28)
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- QUINOLINE DERIVATIVES AS SMO INHIBITORS
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Disclosed are quinoline derivatives as hedgehog pathway inhibitors, especially as SMO inhibitors. Compounds of the present invention can be used in treating diseases relating to hedgehog pathway including cancer.
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Paragraph 0429; 0430
(2017/02/28)
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- Iridium-catalyzed condensation of amines and vicinal diols to substituted piperazines
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A straightforward procedure is described for the synthesis of piperazines from amines and 1,2-diols. The heterocyclization is catalyzed by [Cp*IrCl2]2 and sodium hydrogen carbonate and can be achieved with either toluene or water as solvent. The transformation does not require any stoichiometric additives and only produces water as the byproduct. The reaction can be performed between a 1,2-diamine and a 1,2-diol or by a double condensation between a primary alkylamine and a 1,2-diol. At least one substituent is required on the piperazine ring to achieve the cyclization in good yield. The mechanism is believed to involve dehydrogenation of the 1,2-diol to the α-hydroxy aldehyde, which condenses with the amine to form the α-hydroxy imine. The latter rearranges to the corresponding α-amino carbonyl compound, which then reacts with another amine followed by reduction of the resulting imine. Piperazines are prepared by [Cp*IrCl 2]2-catalyzed heterocyclization of 1,2-diols with either 1,2-diamines or primary alkylamines. The reaction is performed in toluene or water and requires no stoichiometric additive. The key step in the mechanism is believed to be the isomerization of an α-hydroxy imine to the corresponding α-amino carbonyl compound. Copyright
- Lorentz-Petersen, Linda L. R.,Nordstrom, Lars Ulrik,Madsen, Robert
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p. 6752 - 6759
(2013/01/15)
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- NOVEL HOMOPIPERAZINE DERIVATIVES AS PROTEIN TYROSINE KINASE INHIBITORS AND PHARMACEUTICAL USE THEREOF
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The invention relates to compounds of general formula (I) wherein R1,R2, R3, R4, m and n are defined as defined herein, and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use -alone or in
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Page/Page column 66-67
(2012/02/01)
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- Synthesis and antitubercular activity of ferrocenyl diaminoalcohols and diamines
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A total of 21 ferrocenyl and benzyl diaminoalcohols and diamines were synthesized and evaluated against Mycobacterium tuberculosis H37Rv. Interestingly, ferrocenyl diamines exhibit better activities than ferrocenyl diaminoalcohols.
- Andrianina Ralambomanana, Dimby,Razafimahefa-Ramilison, Dorothee,Rakotohova, Andry Clement,Maugein, Jeanne,Pelinski, Lydie
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experimental part
p. 9546 - 9553
(2009/04/06)
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- Iridium catalysed synthesis of piperazines from diols
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A green and atom-economical method has been developed for the synthesis of piperazines by cyclocondensation of diols and amines in aqueous media in the presence of a catalytic amount of [Cp*IrCl2]2. The Royal Society of Chemistry.
- Nordstrom, Lars Ulrik,Madsen, Robert
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p. 5034 - 5036
(2008/09/18)
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