| Summary: | SYNTHESIS OF UNSYMMETRICAL DERIVATES OF AZAPHTALOCYANINES II. Slajsova Dana Department of Pharmaceutical Chemistry and Drug Control, Faculty of Pharmacy in Hradec Králové, Charles University in Prague Magnesium complexes of unsymmetrical azaphtalocyanines (AzaPc) of tetrapyrazinoporphyrazine type with one carboxylic acid were synthesized using statistical condensation of 5,6-bis(tert-butylsulfanyl)pyrazine-2,3-dicarbonitrile (A) and 6-(3-tert-butylsulfanyl-5,6-dicyanopyrazine-2-ylamino)hexanoic acid (B). These two products were chosen because each of them takes advantage of suitable properties to application of AzaPc in photodynamic therapy. These properties are demonstrated in final product too. Bulky tert-butylsulfanyl ensures good monomerisation of planar moleculs of AzaPc in a solution and consequently allows efficient separation and purification. Positive influence of alkylsulfanyl substituent on singlet oxygen production has been already shown earlier. Carboxy group, that can be converted in other reactions (esterification, conjugation with biomoleculs) brings into the AzaPc the modifiable moiety. The standard cyclization process in butanol in the presence of magnesium butanolate was applied. 2,2-dimethylpropane-1-thiol was liberated during the reaction. Probably, it was due to nucleophilic attack of...
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