National Repository of Grey Literature 4 records found  Search took 0.01 seconds. 
Příprava 8-C-substituovaných acyklických nukleosidfosfonátů odvozených od 2,6 diaminopurinu s využitím Negishiho cross-couplingu
Sedláček, Ondřej ; Pohl, Radek ; Holý, Antonín
8-Allyl-, cyclopropyl-, trifluoromethyl-, cyano-, carbethoxy- and acetaldehydo-2,6-diamino- 9-[2-(phosphonomethoxy)ethyl]purine (PMEDAP) were prepared by Negishi cross-coupling of the 8-bromo-PMEDAP under catalysis with Pd2dba3 with various phosphine ligands followed by deprotection.
Nukleosidy a nukleotidy obsahující 8-aza-7,9-dideazaxanthin
Mařák, David ; Otmar, Miroslav ; Dračínský, Martin ; Votruba, Ivan ; Holý, Antonín
The described preparation of 8-aza-7,9-dideazaxanthine from 1,3-dibenzyluracil and TosMIC was improved by using AlCl3 for final debenzylation. Treatment of 6-dibromomethyl- 5-formyluracil with benzyl-, 4-methoxybenzyl-, and 1-adamantylamine gave the corresponding 8-alkyl-8-aza-7,9-dideazaxanthines. N1- and N8-(8-phosphonooctyl)-8-aza-7,9-dideazaxanthines were prepared and found as inhibitors of thymidine phosphorylase (V79 cells, human placenta, Escherichia coli). IC50 values ranged at 3–27 .mu.M.
Efektivní syntézy acyklických nukleosidfosfonátů s jedním otevřeným a jedním nově uzavřeným kruhem
Jansa, Petr ; Dračínský, Martin ; Holý, Antonín
In order to study the SAR, we prepared new 6-[2-(phosphonomethoxy)ethoxy]-2,4-diaminopyrimidine (PMEO-DAPy) analogues substituted by another ring between positions 4 and 5.
Příprava N9-(3-fluoro-2-phosphonomethoxypropyl) (FPMP) derivátů N6-substituovaných adeninů a 2,6-diaminopurinů
Baszczyňski, Ondřej ; Holý, Antonín ; Dračínský, Martin ; Klepetářová, Blanka
An efficient method of the synthesis N9-(3-fluoro-2-phosphonomethoxypropyl) (FPMP) derivatives of purine bases was developed. A series of N6-substituted FPMP dervatives of purine and 2-aminopurine were prepared by using this method.

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