- pyrrole Shalom intermediates
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The invention particularly relates to an amine phosphate binder bixalomer intermediate and a preparation method thereof. The preparation method comprises the following steps: reacting a raw material 3,3'-diamidodipropyl amine under the action of benzyl chloroformate to obtain 3,3'-dibenzyloxyamidodipropyl amine, carrying out substitution reaction on the 3,3'-dibenzyloxyamidodipropyl amine and 1,4-dibromobutane or 1,4-dichlorobutane to obtain N,N,N',N'-tetra(3-dibenzyloxyamido)-1,4-butanediamine, and carrying out deprotection by pressure hydrogenation under the action of Pd-C to obtain N,N,N',N'-tetra(3-aminopropyl)-1,4-butanediamine. The method has the advantages of cheap and accessible raw materials, operable reaction, high yield and fewer three wastes, and thus, has excellent industrial prospects.
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Paragraph 0028; 0029; 0030; 0031; 0032; 0033-0041
(2017/07/23)
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- Design, synthesis and evaluation of novel uracil acetamide derivatives as potential inhibitors of Plasmodium falciparum dUTP nucleotidohydrolase
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The ubiquitous enzyme dUTP nucleotidohydrolase (dUTPase) catalyses the hydrolysis of dUTP to dUMP and can be considered as the first line of defence against incorporation of uracil into DNA. Inhibition of this enzyme results in over-incorporation of uraci
- McCarthy, Orla,Musso-Buendia, Alex,Kaiser, Marcel,Brun, Reto,Ruiz-Perez, Luis M.,Johansson, Nils Gunnar,Pacanowska, Dolores Gonzalez,Gilbert, Ian H.
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experimental part
p. 678 - 688
(2009/09/27)
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- Synthesis of peptide dendrimers based on a β-cyclodextrin core with guest binding ability
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The synthesis of three first-order dendrimers based on a β-cyclodextrin core containing fourteen Val, Phe and Val-Phe residues is described. The guest binding ability of the tetradecavalent peptidyl β-cyclodextrin derivative has been tested by calorimetric titration and the thermodynamic parameters for the complex formation with adamantanecarboxylic acid were obtained.
- Muhanna, Abdullah M. A.,Ortiz-Salmerón, Emilia,García-Fuentes, Luis,Giménez-Martínez, Juan J.,Vargas-Berenguel, Antonio
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p. 6125 - 6128
(2007/10/03)
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- Selective synthesis of carbamate protected polyamines using alkyl phenyl carbonates
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Utilising alkyl phenyl carbonates, an economical, practical and versatile method for selective Boc, Cbz and Alloc protection of polyamines has been developed. This method allows Boc, Cbz and Alloc protection of primary amines in the presence of secondary amines by reaction of the polyamines with the alkyl phenyl carbonates. Also, this method allows mono carbamate protection of simple symmetrical aliphatic α,ω-alkanediamines in high yields with respect to the diamine. Finally, the method allows selective carbamate protection of a primary amine located on a primary carbon in the presence of a primary amine located on a secondary or a tertiary carbon in excellent yields.
- Pittelkow, Michael,Lewinsky, Rasmus,Christensen, Jorn Bolstad
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p. 2195 - 2202
(2007/10/03)
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- Synthesis of new α-thiosialodendrimers and their binding properties to the sialic acid specific lectin from Limax flavus
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Carbohydrate-protein binding interactions can be greatly amplified using the cluster or multivalent effect. In previous studies, sialylated multibranched L-lysine dendrimers were found to be potent inhibitors of the hemagglutination of human erythrocytes
- Zanini, Diana,Roy, René
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p. 2088 - 2095
(2007/10/03)
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- Multivalent neoglycoconjugates: Solid-phase synthesis of N-linked α-sialodendrimers
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A series of N-linked α-sialodendrimers with valencies of 2, 4 and 8 has been scaffolded on an N,N-bis(3-aminopropyl)succinamic acid core using Wang resin and 9-fluorenylmethoxycarbonyl and 2-(1H-benzotriazol-1-yl)1,1,3,3-tetramethyluronium tetrafluorobora
- Llinares, Muriel,Roy, Rene
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p. 2119 - 2120
(2007/10/03)
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- Novel dendritic α-sialosides: Synthesis of glycodendrimers based on a 3,3′-iminobis(propylamine) core
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The cluster or multivalent effect has been recognized as an effective means by which to increase binding interactions between carbohydrates and proteins. In fact, it has been demonstrated that sialylated multibranched L-lysine dendrimers were potent inhibitors of hemagglutination of human erythrocytes by Influenza viruses. In a continuation of these studies, the synthesis of novel glycodendrimers with even valencies from 2 to 16 and ending with equidistant thiosialoside residues is described. These symmetrical dendrimers were more readily characterized by standard NMR spectral techniques than previously reported nonsymmetrical dendrimers of this general type. The synthesis of the dendritic core was based on the regioselective protection of the primary amines of 3,3′-iminobis(propylamine) (4) using benzyl cyanoformate. The resulting secondary amine 5 was alkylated with tert-butyl bromoacetate to provide divalent core structure 6 with Cbz protected amines and acid protected tert-butyl ester. Sequential deprotection by trifluoroacetolysis or hydrogenation afforded acid 7 or diamine 8 as key precursors, respectively. The two fragments were coupled using HOBt/DIC strategy to provide Cbz-protected dendrimers with valencies of 2, 4, 8, and 16 in the first, second, third, and fourth generations, respectively, in reasonable to good yields (42-82%). Cbz-protected precursors were efficiently transformed into N-chloroacetylated dendrimers by hydrogenolysis and treatment of the resulting amines with chloroacetic anhydride (82-91%). N-Chloroacetylated dendrimers were then treated with an excess of 2-thiosialic acid derivative 3 to give fully protected sialodendrimers in 76-96% yields. Deprotection of sialodendrimers under Zemplen conditions followed by methyl ester saponification and purification by gel permeation chromatography afforded symmetrical dendritic α-thiosialosides 21, 23, 25, and 27 in fair yields (47-58%). These novel sialodendrimers, in keeping with their design, are currently being evaluated as inhibitors of human erythrocyte hemagglutination by Influenza viruses.
- Zanini, Diana,Roy, Rene
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p. 7348 - 7354
(2007/10/03)
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