"2156-8952" . "Benzodiazepines, Solid-phase synthesis, Aminoketones, Nitrobenzoic acids, Haloketones"@en . . . "Solid-Phase Synthesis of Trisubstituted Benzo[1,4]-Diazepin-5-one Derivatives" . "000312122500004" . "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." . "12" . "F\u00FCl\u00F6pov\u00E1, Veronika" . "4"^^ . "Guck\u00FD, Tom\u00E1\u0161" . . . . "RIV/61989592:15310/12:33141460!RIV13-MSM-15310___" . . . "15310" . . . "14" . "US - Spojen\u00E9 st\u00E1ty americk\u00E9" . . . . . "6"^^ . . "10.1021/co300124q" . "Grepl, Martin" . "[0CC36A59F590]" . "169118" . . "P(ED0030/01/01)" . "ACS Combinatorial Science" . . . . . "RIV/61989592:15310/12:33141460" . "Solid-Phase Synthesis of Trisubstituted Benzo[1,4]-Diazepin-5-one Derivatives"@en . "Soural, Miroslav" . . . "Solid-Phase Synthesis of Trisubstituted Benzo[1,4]-Diazepin-5-one Derivatives"@en . "Solid-Phase Synthesis of Trisubstituted Benzo[1,4]-Diazepin-5-one Derivatives" . "4"^^ . "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 .