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Syntéza (purin-6-yl)acetátů a jejich transformace
Hasník, Zbyněk ; Hocek, Michal
A novel approach to the synthesis of (purin-6-yl)acetates was developed based on Pd-catalysed cross-coupling reactions of 6-chloropurines with the Reformatsky agent. These intermediates were converted into various products by functional group transformations. Amides were prepared by amidation of ester group with amines, 6-(hydroxyethyl)purines by reduction by NaBH4, and beta-substituted 6-ethylpurines by mesylation of 6-(hydroxyethyl)purines and subsequent nucleophilic substitution.
Purinové báze a nukleosidy nesoucí funkcionalizované C-substituenty v pozici 6. Syntéza a biologická aktivita
Hocek, Michal ; Šilhár, Peter ; Kuchař, Martin ; Hasník, Zbyněk ; Bambuch, Vítězslav
Purine bases and nucleosides bearing diverse functionalized C-substituents have been prepared either via cross-coupling reactions of 6-halopurines with protected functionalized organometallic reagents or via conjugate additions of nucleophiles to 6-vinyl- or 6-ethynylpurines. Other types of substituents have been prepared by further functional group transformations of 6-(mesyloxymethyl)purines. Systematic biological activity screening revealed several new types of cytostatic and anti-HCV purine nucleosides.
Syntéza C-5 substituovaných derivátů HPMPC (Cidofoviru)
Krečmerová, Marcela ; Holý, Antonín
The series of N4-alkyl derivatives of (S)-1-[3-hydroxy-2-(phosphonomethoxy)propyl]-5-ethylcytosine was prepared from the corresponding 5-ethyl-4-methoxypyrimidin-2-(1H )-one intermediates by the action of primary amines. Sonogashira coupling was used for the preparation of 5-ethynyl HPMPC.
N6-methyl-AMP-hydrolasa aktivuje N6-substituované purinové ANPs
Schinkmanová, Markéta ; Votruba, Ivan ; Holý, Antonín
Identification and characterization of a new enzyme, N6-methyl-AMP aminohydrolase, that is responsible for the conversion of N6-cyclopropyl-PMEDAP to biologically active PMEG.

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