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  • Simple solid-phase synthesis of 3,10-dihydro-2H-benzo[e]imidazothiadiazin-2-one 5,5-dioxides is described, with Fmoc-?-amino acids and 2-nitrobenzenesulfonylchlorides (2-NosCls) being the key building blocks. Fmoc-?-amino acids were immobilized on Wang resin and transformed to the corresponding 2-nitrobenzenesulfonamides in two steps. After reduction of the nitro group, Fmoc-thioureas were synthesized followed by cyclization of the 1,2,4-benzothiadiazine-1,1-dioxide scaffold with diisopropylcarbodiimide (DIC). Cleavage of the Fmoc protecting group followed by spontaneous cyclative cleavage gave the target products in excellent crude purity.
  • Simple solid-phase synthesis of 3,10-dihydro-2H-benzo[e]imidazothiadiazin-2-one 5,5-dioxides is described, with Fmoc-?-amino acids and 2-nitrobenzenesulfonylchlorides (2-NosCls) being the key building blocks. Fmoc-?-amino acids were immobilized on Wang resin and transformed to the corresponding 2-nitrobenzenesulfonamides in two steps. After reduction of the nitro group, Fmoc-thioureas were synthesized followed by cyclization of the 1,2,4-benzothiadiazine-1,1-dioxide scaffold with diisopropylcarbodiimide (DIC). Cleavage of the Fmoc protecting group followed by spontaneous cyclative cleavage gave the target products in excellent crude purity. (en)
Title
  • Solid-Phase Synthesis of Anagrelide Sulfonyl Analogues
  • Solid-Phase Synthesis of Anagrelide Sulfonyl Analogues (en)
skos:prefLabel
  • Solid-Phase Synthesis of Anagrelide Sulfonyl Analogues
  • Solid-Phase Synthesis of Anagrelide Sulfonyl Analogues (en)
skos:notation
  • RIV/61989592:15110/14:33151916!RIV15-MSM-15110___
http://linked.open...avai/riv/aktivita
http://linked.open...avai/riv/aktivity
  • I, P(ED0030/01/01), P(EE2.3.20.0009), P(EE2.4.31.0130)
http://linked.open...iv/cisloPeriodika
  • 5
http://linked.open...vai/riv/dodaniDat
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  • 45894
http://linked.open...ai/riv/idVysledku
  • RIV/61989592:15110/14:33151916
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http://linked.open.../riv/klicovaSlova
  • Cyclative cleavage; Solid-phase synthesis; 2-Nitrobenzenesulfonylchlorides; Fmoc-amino acids; Cyclic guanidines; Anagrelide analogues (en)
http://linked.open.../riv/klicoveSlovo
http://linked.open...odStatuVydavatele
  • US - Spojené státy americké
http://linked.open...ontrolniKodProRIV
  • [E3B9C6649FB2]
http://linked.open...i/riv/nazevZdroje
  • ACS Combinatorial Science
http://linked.open...in/vavai/riv/obor
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http://linked.open...vavai/riv/projekt
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http://linked.open...v/svazekPeriodika
  • 16
http://linked.open...iv/tvurceVysledku
  • Soural, Miroslav
  • Popa, Igor
  • Grepl, M.
  • Fülöpová, Veronika
  • Mcmaster, Claire Suzanne
issn
  • 2156-8952
number of pages
http://localhost/t...ganizacniJednotka
  • 15110
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