295-37-4Relevant articles and documents
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Bounsall,Koprich
, p. 1481,1487 (1970)
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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.
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.
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.
