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	The unique impact of microwave irradiation on the chemistry of acyclic nucleoside phosphonates Jansa, Petr ; Holý, Antonín ; Dračínský, Martin ; Baszczyňski, Ondřej ; Česnek, Michal ; Janeba, Zlatko Latest improvements of the syntheses of ANPs using microwave irradiation are presented, namely a novel, efficient, and environmentally friendly synthesis of dialkyl haloalkylphosphonates via the microwave-assisted Michaelis-Arbuzov reaction and microwave-assisted hydrolysis of phosphonate diesters. Detailed record
	Efficient one-pot synthesis of polysubstituted 6-[(1H-1,2,3-triazol-1-yl)methyl]uracils through the "click" protocol Jansa, Petr ; Špaček, Petr ; Holý, Antonín ; Votruba, Ivan ; Janeba, Zlatko Synthesis of triazoloacyclic nucleosides and nucleoside phosphonates was developed as the one-pot Cu(I)-catalyzed azide alkyne Huisgen "click" cycloaddition. A novel Cu(I)-catalyzed decarboxylation reaction of 1-substituted 1H-1,2,3-triazole-4-carboxylates at room temperature was observed and used for the preparation of 1-substituted 1H-1,2,3-triazoles. Detailed record
	Use of 1,3-dioxolanes in the syntheses of alpha-branched alkyl and aryl N-9-[2-(phosphonomethoxy)ethyl]purines Pomeisl, Karel ; Holý, Antonín ; Krečmerová, Marcela Syntheses of various alkyl and aryl substituted N-9-[2-(phoshonomethoxy)ethyl]purines from a number of 2-alkyl(aryl)-1,3-dioxolanes were developed in preparative yields. The cleavage of a dioxolane ring with Lewis acids was chosen for preparation of suitable phosphonate building blocks as a key reaction step followed by their Mitsunobu reaction with purine bases. Obtained phosphonate derivatives were tested as potential HG(X)PRTase inhibitors. In contrast to previously published N-9-[2-(phosphonoethoxy)ethyl]purines, no inhibitory activity towards this enzyme was observed. Detailed record
	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. Detailed record
	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. Detailed record
	Studium chemické stability antivirově aktivních 5-azacytosin acyklických nukleosidfosfonátů pomocí NMR spektroskopie Dračínský, Martin ; Krečmerová, Marcela ; Holý, Antonín Hydrolytic decomposition of four 5-azacytosine acyclic nucleoside phosphonates was studied. Products of the decomposition are carbamoylguanidine derivatives. Stability and decomposition products of HPMP-5-azaC (a 5-azacytosine derivative with strong antiviral activity) differ from the other derivatives. Detailed record
	Syntézy látek mimikujících acyklické nukleosiddifosfáty Doláková, Petra ; Dračínský, Martin ; Holý, Antonín A series of acyclic nucleoside diphosphate mimics bearing purine and pyrimidine bases was prepared by Mitsunobu reaction of protected heterocyclic bases with appropriate alcohol containing stable diphosphate analogue. Detailed record
	Snadné syntézy pyrimidinových acyklických nukleosidfosfonátů a jejich potenciál v biomedicinálních aplikacích Pomeisl, Karel ; Holý, Antonín ; Votruba, Ivan ; Nencka, Radim ; Pohl, Radek The presented syntheses using a nucleophilic fluorination, Suzuki–Miyaura coupling reactions and phosphorylation were successfully applied for the preparation of a number of pyrimidine acyclic nucleoside phosphonates in connection of finding of potential bioactive compounds. Detailed record
	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. Detailed record
	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. Detailed record

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1	Holý, Adam

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