Práca sa venuje syntéze, overeniu štruktúry a štúdiu fyzikálno-chemických vlastností derivátov aryloxyaminopropanolu, 2-hydroxy-3-[4-(2-fluórfenyl)-piperazín-1-yl]-propyl-4-[(alkoxykarbonyl)amino] benzoátov, ich solí s kyselinou chlorovodíkovou, s jedným až štyrmi atómami uhlíka v alkoxy skupine karbamoylovej skupiny. Štruktúra zlúčenín bola potvrdená elementárnou analýzou, IČ, UV a hmotnostnými spektrami. V rámci štúdia bola stanovená teplota topenia, rozpustnosť, povrchová aktivita, disociačná konštanta, ako aj parametre lipofility, t.j. rozdeľovací koeficient P, hodnoty RM z reverznej chromatografie na tenkej vrstve a retenčný faktor k pomocou vysokoúčinnej kvapalinovej chromatografie.

The paper deals with the synthesis, structure confirmation, and study of physicochemical properties of some aryloxyaminopropanol derivatives, compounds of 2-hydroxy-3-[4-(2-fluorophenyl)-piperazine-1-yl]-propyl-4-[(alkoxycarbonyl)amino]benzoates, their salts with hydrochloric acid, with one to four carbon atoms in the alkoxy group of the carbamoyl group. Their structure was confirmed by elemental analysis, IR, UV and mass spectra. The melting point, solubility, surface activity, dissociation constant, and some lipophilicity parameters, i.e. partition coefficient P, RM values from reversed phase thin-layer chromatography, and retention factor k obtained from HPLC of the substances under study were determined.

Comenius University Faculty of Pharmacy Department of Pharmaceutical Chemistry Bratislava

Synthesis, identification and physicochemical properties of novel potential ultrashort-acting beta-adrenergic blockers

Lit.: 10