295-37-4Relevant articles and documents
C-substituted cyclams from cyclotetrapeptides [1]
Lang, Markus A.,Beck, Wolfgang
, p. 447 - 450 (2003)
The reduction of cyclotetrapeptides cyclo(X-β-Ala-X-β-Ala) (X = Gly, (S)-Ala, (S)-Leu, (S)-Val, (S)-Phe) 1a - 1e with LiAlH4 in THF gives the C-substituted cyclams 2a - 2e.
ARENE CONNECTED POLYAMINE MACRORING DERIVATIVES, PREPARATION METHODS AND PHARMACEUTICAL USES THEREOF
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Page/Page column 18-19, (2010/04/24)
Abstract: The present invention relates to arene connected polyamine macrocyclic derivatives represented by general formula I, pharmaceutically acceptable salts or hydrates thereof which have anti-HIV activities, in which the definitions of substituents are as defined in the description; to preparation methods of the compounds of formula I; to pharmaceutical compositions containing the compounds of formula I or their pharmaceutically acceptable salts or hydrates; to the use of the compounds of formula I or their pharmaceutically acceptable salts or hydrates for the preparation of a medicament for the treatment and prevention of HIV-associated diseases.
Cyclohexanedione bisaminals as intermediates for cyclen, homocyclen, and cyclam synthesis
Prokhorov, Anton,Le Bris, Nathalie,Bernard, Helene,Claudon, Geraldine,Handel, Henri
, p. 3271 - 3282 (2007/10/03)
A new easy-to-run route to cyclen, homocyclen, and cyclam is proposed, based on the cyclization with dibromo- or ditosyloxy-derivatives of bisaminal intermediates obtained by condensation of the appropriate linear tetraamine with cyclohexanedione. In the cyclization step, the use of cesium carbonate instead of potassium carbonate as proton trapper caused a remarkable increase of yields. Copyright Taylor & Francis Group, LLC.
Selective protection of 1,4,8,11-tetraazacyclotetradecane (cyclam) in position 1,4 with the phosphonothioyl group and synthesis of a cyclam-1,4-bis(methylphosphonic acid). Crystal structures of several cyclic phosphonothioamides
Vitha, Tomas,Kotek, Jan,Rudovsky, Jakub,Kubicek, Vojtech,Cisarova, Ivana,Hermann, Petr,Lukes, Ivan
, p. 337 - 367 (2007/10/03)
A new cyclam-based ligand, 1,4,8,11-tetraazacyclotetradecane-1,4- bis(methylphosphonic acid) (1,4-H4te2p), was synthesized. Cyclam was protected by the reaction with PhP(S)Cl2 to form exclusively five-membered cyclic phenylphosphonothioic diamide 2 in a moderate yield. The solid-state structures of 2 and several by-products were determined. Compound 2 was isolated as two stable conformers differing in a mutual position of benzene ring and sulfur atom with respect to the cyclam ring. Compound 2 was used for the synthesis of 1,4-dibenzylcyclam. However, the deprotection of the thiophosphoryl-protected bis(methyl-phosphonate diester) with aqueous HCl under non-optimized conditions led to a mixture of cyclam derivatives differently substituted with methylphosphonic acid groups. The crystal structures of the target product, 1,4-H4te2p, and also 1,4,8,11- tetraazacyclotetradecane-1,4,8,11-tetrakis(methylphosphonic acid) (H 8tetp) were determined. A similar reaction with cyclen (1,4,7,10-tetraazacyclododecane) led only to hardly purifiable mixtures.
Coloring agent comprising transition metals
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, (2008/06/13)
The present invention relates to a composition for coloring keratin fibers and a method of using the same. The composition of the present invention contains at least one dye precursor, and one or more clathrate compounds that contain transition metal complexes.
Phenylglyoxal for polyamines modification and cyclam synthesis
Tripier, Rapha?l,Chuburu, Fran?oise,Le Baccon, Michel,Handel, Henri
, p. 4573 - 4579 (2007/10/03)
The bis-aminals obtained by tetraamine and phenylglyoxal condensation display various behaviours such as equilibrium between different configurations, rearrangements that lead to lactam derivatives, or amine deprotection. Our investigations about them were focused on three different linear amines, and then extended to polyazacycloalkanes cyclen and cyclam. Cyclam was also synthesised with the bis-aminals issued from condensation of linear polyamines with phenylglyoxal. The lactam derivatives described here were moreover, employed for the mono-N-functionalisation of tetraamines by phenyl-acetic acid group.
Studies on biologically potent tetraazamacrocyclic complexes of bivalent tin
Chaudhary, Ashu,Singh
, p. 615 - 626 (2007/10/03)
Fourteen- to eighteen-membered tetraamide macrocyclic ligands N4L1-N4L4 have been prepared by the condensation of 1,2-diaminoethane or 1,3-diaminopropane with malonic or succinic acid in the presence of condensing reagents dicyclohexylcarbodiimide and 4-dimethylaminopyridine. On reduction, these macrocyclic ligands give a new series of tetraazamacrocycles MacL1-MacL4 which form complexes with tin(II) chloride. The ligands and their complexes were characterized by elemental analyses, molecular weight determinations, infrared and 1H NMR spectral studies. The hexacoordinated state for tin has been confirmed by spectral studies. An octahedral geometry for these complexes has been proposed as the binding sites are the nitrogen atoms of the macrocycles. On the basis of the chemical composition the representation of the complexes as [Sn(MacLn)Cl2] (n = 1-4) has been established. The ligands and their complexes also have been screened for their antifungal and antibacterial activities and the findings have been reported and explained.
Process for preparing 1,4,8,11-tetraazacyclotetradecane
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, (2008/06/13)
An improved process for preparing 1,4,8,11-tetraazacyclotetradecane comprising the bisacylation of an acyclic diamine to obtain a dichlorodiamide compound in a first step, the cyclization of said diamide compound to obtain dioxocyclam in a second step, and the reduction of dioxocyclam in a third step to obtain the desired 1,4,8,11-tetraazacyclotetradecane.
Studies on the interaction of iron(II), nickel(II), copper(II) and zinc(II) with tetraazamacrocycles
Shakir, Mohammad,Varkey, Saji P.,Nasman, Omar S. M.
, p. 671 - 676 (2007/10/03)
The condensation of aliphatic diamines H2N(CH2)nNH2 (n = 2-3) with dicarboxylic acid HOOC - (CH2)n - COOH (n=1-2) in the presence of dicyclohexyl-carbodiimide and 4-(dimethylamino)pyridine results in new types of 14-18 membered tetraamide macrocyclic ligands 1a-1d. These compounds on reduction with LiAlH4 yield a series of tetraazamacrocycles 2a-2d which form complexes with Fe(II), Ni(II), Cu(II) and Zn(II). The ligands and their complexes have been characterized by elemental analyses, mass, IR, 1H NMR, UV/Vis, EPR spectroscopic, molar conductance and magnetic moment data. An octahedral geometry around the metal ion is suggested for [M2aCl2][M2dCl2], where M = Fe(II) and Ni(II) while a square-planar and a tetrahedral geometry is proposed for [M2a]Cl2-[M2d]Cl2 for M = Cu(II) and Zn(II).
Process for the synthesis of cyclic polynitrogenated compounds
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, (2008/06/13)
A method for the synthesis of cyclic polyamines preceeds by reaction of a diamine with the acrylonitrile wherein the reduction steps are carried out with Raney alloy instead of using hydrogen under pressure in the presence of Raney nickel. Compounds so prepared have the formula: STR1 wherein A and B are: an alkyl chain --(CH2)-- in which x is an integer of 2 to 4, substituted or not by an alkyl group of 1 to 5 carbon atoms, which may be substituted or not by an aromatic ring, heterocyclic ring, amine ketone, carboxylic acid, amide, cyano, alkyl, alkoxy, hydroxy, nitro or halogen and R1 and R2 are the same moieties as those substituting the alkyl claim above.
