About: Solid-Phase Synthesis of 4,7,8-Trisubstituted 1,2,3,4-Tetrahydro-benzo[e][1,4]diazepin-5-ones     Goto   Sponge   NotDistinct   Permalink

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Description
  • Solid-phase synthesis of 1,2,3,4-tetrahydro-benzo[e][1,4]diazepin-5-ones with use of polystyrene resin is described. The starting material was polymer supported 1,2-diaminoethane and as a key synthon, 4-chloro-2-fluoro-5-nitrobenzoic acid was used. The synthetic approach allows the preparation of derivatives with variable substitution at positions 4 and 8. Additionally, a skeletal diversity was increased when the nitro group was reduced and some benzene fused heterocycles were prepared. An expansion of a diazepinone to a benzodiazocinone scaffold was also successful although some limitations in a diversity of target derivatives were observed.
  • Solid-phase synthesis of 1,2,3,4-tetrahydro-benzo[e][1,4]diazepin-5-ones with use of polystyrene resin is described. The starting material was polymer supported 1,2-diaminoethane and as a key synthon, 4-chloro-2-fluoro-5-nitrobenzoic acid was used. The synthetic approach allows the preparation of derivatives with variable substitution at positions 4 and 8. Additionally, a skeletal diversity was increased when the nitro group was reduced and some benzene fused heterocycles were prepared. An expansion of a diazepinone to a benzodiazocinone scaffold was also successful although some limitations in a diversity of target derivatives were observed. (en)
Title
  • Solid-Phase Synthesis of 4,7,8-Trisubstituted 1,2,3,4-Tetrahydro-benzo[e][1,4]diazepin-5-ones
  • Solid-Phase Synthesis of 4,7,8-Trisubstituted 1,2,3,4-Tetrahydro-benzo[e][1,4]diazepin-5-ones (en)
skos:prefLabel
  • Solid-Phase Synthesis of 4,7,8-Trisubstituted 1,2,3,4-Tetrahydro-benzo[e][1,4]diazepin-5-ones
  • Solid-Phase Synthesis of 4,7,8-Trisubstituted 1,2,3,4-Tetrahydro-benzo[e][1,4]diazepin-5-ones (en)
skos:notation
  • RIV/61989592:15310/12:33141463!RIV13-MSM-15310___
http://linked.open...avai/predkladatel
http://linked.open...avai/riv/aktivita
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  • P(ED0030/01/01)
http://linked.open...iv/cisloPeriodika
  • 12
http://linked.open...vai/riv/dodaniDat
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  • 169119
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  • RIV/61989592:15310/12:33141463
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  • Benzodiazepinones, Benzodiazocinones, Thiazines, Thiazepines, Bisheterocycles, Solid-phase synthesis (en)
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  • US - Spojené státy americké
http://linked.open...ontrolniKodProRIV
  • [4FA75D89F541]
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  • ACS Combinatorial Science
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  • 14
http://linked.open...iv/tvurceVysledku
  • Soural, Miroslav
  • Lemrová, Barbora
http://linked.open...ain/vavai/riv/wos
  • 000312122500003
issn
  • 2156-8952
number of pages
http://bibframe.org/vocab/doi
  • 10.1021/co300121d
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  • 15310
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