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| Description
| - The project will deal with regioselective cross-coupling reactions of 2,6- and 6,8-dihalopurines (9- substituted or protected bases and protected nucleosides) with organometallic reagents (boronic acids, organozinc and organoaluminium reagents) in order to introduce C-substituents into these position. Depending on the nature of dihalopurine, nature and amount of organometallic reagent and conditions, products of mono- or disubstitution will be obtained. The mono-C-substituted halopurines will serve as starting compounds for further transformations: aminolyses, alcoholyzes and cross-couplings. By this approach, a large series of title purine bases and nucleosides bearing C-substituent in position 2,6 or 8 in combination with another substituent (C-, N- or O-) in other positions. Final title disubstituted purine bases and nucleosides will be tested not only on cytostatic activity, but also on antimycobacterial and antivital activity. (en)
- Projekt bude zaměřen na studium regioselektivních cross-coupling reakcí 2,6- a 6,8-dihalogenpurinů (9-substituovaných či chráněných bází a chráněných nukleosidů) s organokovovými činidly (boronovými kyselinami, organozinečnatými a organohlinitými činidly), pomocí kterých budou zaváděny do těchto poloh C-substituenty. V závislosti na typu dihalogenpurinu, typu a množství organokovového činidla a podmínkách budou získávány produkty mono- či disubstituce. Mono-C-substituované halogenpuriny budou použity k dalším substitučním reakcím: aminolýzám, alkoholýzám a cross-coupling reakcím. Touto metodikou bude připravena velká serie purinových bází a nukleosidů nesoucí C-substituenty v polohách 2,6 či 8 v kombinaci s dalším substituentem (C-, N- nebo O-) v dalších polohách. U výsledných disubstituovaných purinových bází a nukleosidů bude studována zejména jejich cytostatická aktivita, ale i např. antimykobakteriální a protivirový účinek.
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| Title
| - Synthesis and cytostatic activity studies of novel 2,6- and 6,8-disubstituted purine bases and nucleosides (en)
- Syntéza nových 2,6- a 6,8-disubstituovaných purinových bází a nukleosidů a studium jejich cytostatické aktivity
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| skos:notation
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| http://linked.open...avai/cep/aktivita
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| http://linked.open...kovaStatniPodpora
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| http://linked.open...ep/celkoveNaklady
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| http://linked.open...datumDodatniDoRIV
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| http://linked.open...i/cep/druhSouteze
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| http://linked.open...ep/duvernostUdaju
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| http://linked.open.../cep/fazeProjektu
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| http://linked.open...ai/cep/hlavniObor
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| http://linked.open...hodnoceniProjektu
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| http://linked.open...vai/cep/kategorie
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| http://linked.open.../cep/klicovaSlova
| - purines; nucleosides; cross-coupling reactions; cytostatic activity (en)
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| http://linked.open...ep/partnetrHlavni
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| http://linked.open...inujicichPrijemcu
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| http://linked.open...cep/pocetPrijemcu
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| http://linked.open...ocetSpoluPrijemcu
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| http://linked.open.../pocetVysledkuRIV
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| http://linked.open...enychVysledkuVRIV
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| http://linked.open...okUkonceniPodpory
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| http://linked.open...okZahajeniPodpory
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| http://linked.open...iciPoslednihoRoku
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| http://linked.open...atUdajeProjZameru
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| http://linked.open.../vavai/cep/soutez
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| http://linked.open...usZobrazovaneFaze
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| http://linked.open...ai/cep/typPojektu
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| http://linked.open...jektu+dodavatelem
| - Regioselect.cross-coupling reactions of 2,6-a 6,8-dihalopurines and 2,6,8-trichloropurines with one equivalent of an organometal.reagent were studied. Mono-substituted halopurines were used in other reactions, the methodology was applied in the synthesis (en)
- Regioselektivní cross-coupling reakce 2,6- a 6,8-dihalogenpurinů a 2,6,8-trichlorpurinů s jedním ekvivalentem organokov. činidla. Získané monosubstituované halogenpuriny využity k dalším reakcím a metodika aplikována na syntézu modifik.bází a nukleosidů. (cs)
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| http://linked.open...tniCyklusProjektu
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| http://linked.open.../cep/klicoveSlovo
| - purines
- nucleosides
- cross-coupling reactions
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| is http://linked.open...vavai/riv/projekt
of | - Dichotomy in Regioselective Cross-Coupling Reactions of 6,8-Dichloropurines with Phenylboronic Acid and Methylmagnesium Chloride: Synthesis of 6,8-Disubstituted Purines
- Regioselective cross-coupling reactions in the synthesis of multisubstituted purine bases and nucleosides
- Biological activity of selected guanidinopurines
- Cytostatic 6-arylpurine nucleosides V. Synthesis of 8-substituted 6-phenylpurine ribonucleosides.
- An efficient synthesis of 2-substituted 6-methylpurine bases and nucleosides by Fe- or Pd-catalyzed Cross-coupling reactions of 2,6-dichloropurines.
- Ferrocene-modified purines as potential electrochemical markers: synthesis, crystal structures, electrochemistry and cytostatic activity of (ferrocenylethynyl)-and (ferrocenylethyl)purines
- Cytostatic 6-arylpurine nucleosides IV. Synthesis of 2-substituted 6-phenylpurine ribonucleosides.
- Synthesis of carba-analogues of myoseverin by regioselective cross-coupling reactions of 2,6-dichloro-9-isopropylpurine.
- Syntheses of purines bearing carbon substituents in positions 2,6 or 8 by metal- or organometal-mediated C-C bond-forming reactions.
- Regioselectivity in cross-coupling reactions of 2,6,8-trichloro-9-(tetrahydropyran-2-yl)purine: Synthesis of 2,6,8-trisubstituted purine bases
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| is http://linked.open...vavai/cep/projekt
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