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Description
| - Solid-phase synthesis of 3,4-dihydro-benzo[e][1,4]diazepin-5-ones with three diversity positions is described. Various primary amines were used as the starting material and immobilized on the polystyrene resin equipped with different acid-labile linkers. Polymer supported amines were converted to ?-aminoketones with the use of their sulfonylation with the 4-nitrobenzensulfonylchoride (4-Nos-Cl) and subsequent alkylation with alfa-bromoketones. After the cleavage of the 4-Nos group the corresponding -aminoketones were acylated with various o-nitrobenzoic acids. Reduction of the nitro group followed by spontaneous on-resin ring closure gave the target immobilized benzodiazepines. After acid-mediated cleavage the products were obtained in very good, crude purity and satisfactory yields which makes the developed method applicable for simple library synthesis of the corresponding derivatives in a combinatorial fashion.
- Solid-phase synthesis of 3,4-dihydro-benzo[e][1,4]diazepin-5-ones with three diversity positions is described. Various primary amines were used as the starting material and immobilized on the polystyrene resin equipped with different acid-labile linkers. Polymer supported amines were converted to ?-aminoketones with the use of their sulfonylation with the 4-nitrobenzensulfonylchoride (4-Nos-Cl) and subsequent alkylation with alfa-bromoketones. After the cleavage of the 4-Nos group the corresponding -aminoketones were acylated with various o-nitrobenzoic acids. Reduction of the nitro group followed by spontaneous on-resin ring closure gave the target immobilized benzodiazepines. After acid-mediated cleavage the products were obtained in very good, crude purity and satisfactory yields which makes the developed method applicable for simple library synthesis of the corresponding derivatives in a combinatorial fashion. (en)
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Title
| - Solid-Phase Synthesis of Trisubstituted Benzo[1,4]-Diazepin-5-one Derivatives
- Solid-Phase Synthesis of Trisubstituted Benzo[1,4]-Diazepin-5-one Derivatives (en)
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skos:prefLabel
| - Solid-Phase Synthesis of Trisubstituted Benzo[1,4]-Diazepin-5-one Derivatives
- Solid-Phase Synthesis of Trisubstituted Benzo[1,4]-Diazepin-5-one Derivatives (en)
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skos:notation
| - RIV/61989592:15310/12:33141460!RIV13-MSM-15310___
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http://linked.open...avai/predkladatel
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http://linked.open...avai/riv/aktivita
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http://linked.open...avai/riv/aktivity
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http://linked.open...iv/cisloPeriodika
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http://linked.open...vai/riv/dodaniDat
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http://linked.open...aciTvurceVysledku
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http://linked.open.../riv/druhVysledku
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http://linked.open...iv/duvernostUdaju
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http://linked.open...titaPredkladatele
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http://linked.open...dnocenehoVysledku
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http://linked.open...ai/riv/idVysledku
| - RIV/61989592:15310/12:33141460
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http://linked.open...riv/jazykVysledku
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http://linked.open.../riv/klicovaSlova
| - Benzodiazepines, Solid-phase synthesis, Aminoketones, Nitrobenzoic acids, Haloketones (en)
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http://linked.open.../riv/klicoveSlovo
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http://linked.open...odStatuVydavatele
| - US - Spojené státy americké
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http://linked.open...ontrolniKodProRIV
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http://linked.open...i/riv/nazevZdroje
| - ACS Combinatorial Science
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http://linked.open...in/vavai/riv/obor
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http://linked.open...ichTvurcuVysledku
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http://linked.open...cetTvurcuVysledku
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http://linked.open...vavai/riv/projekt
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http://linked.open...UplatneniVysledku
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http://linked.open...v/svazekPeriodika
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http://linked.open...iv/tvurceVysledku
| - Soural, Miroslav
- Grepl, Martin
- Gucký, Tomáš
- Fülöpová, Veronika
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http://linked.open...ain/vavai/riv/wos
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issn
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number of pages
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http://bibframe.org/vocab/doi
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http://localhost/t...ganizacniJednotka
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is http://linked.open...avai/riv/vysledek
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