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Statements

Subject Item
n2:RIV%2F61989592%3A15110%2F14%3A33151916%21RIV15-MSM-15110___
rdf:type
n12:Vysledek skos:Concept
dcterms:description
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.
dcterms:title
Solid-Phase Synthesis of Anagrelide Sulfonyl Analogues Solid-Phase Synthesis of Anagrelide Sulfonyl Analogues
skos:prefLabel
Solid-Phase Synthesis of Anagrelide Sulfonyl Analogues Solid-Phase Synthesis of Anagrelide Sulfonyl Analogues
skos:notation
RIV/61989592:15110/14:33151916!RIV15-MSM-15110___
n3:aktivita
n15:I n15:P
n3:aktivity
I, P(ED0030/01/01), P(EE2.3.20.0009), P(EE2.4.31.0130)
n3:cisloPeriodika
5
n3:dodaniDat
n10:2015
n3:domaciTvurceVysledku
n7:4012240 n7:1759256 Mcmaster, Claire Suzanne
n3:druhVysledku
n16:J
n3:duvernostUdaju
n18:S
n3:entitaPredkladatele
n17:predkladatel
n3:idSjednocenehoVysledku
45894
n3:idVysledku
RIV/61989592:15110/14:33151916
n3:jazykVysledku
n11:eng
n3:klicovaSlova
Cyclative cleavage; Solid-phase synthesis; 2-Nitrobenzenesulfonylchlorides; Fmoc-amino acids; Cyclic guanidines; Anagrelide analogues
n3:klicoveSlovo
n6:Cyclative%20cleavage n6:Fmoc-amino%20acids n6:Cyclic%20guanidines n6:2-Nitrobenzenesulfonylchlorides n6:Anagrelide%20analogues n6:Solid-phase%20synthesis
n3:kodStatuVydavatele
US - Spojené státy americké
n3:kontrolniKodProRIV
[E3B9C6649FB2]
n3:nazevZdroje
ACS Combinatorial Science
n3:obor
n5:CC
n3:pocetDomacichTvurcuVysledku
3
n3:pocetTvurcuVysledku
5
n3:projekt
n4:EE2.3.20.0009 n4:EE2.4.31.0130 n4:ED0030%2F01%2F01
n3:rokUplatneniVysledku
n10:2014
n3:svazekPeriodika
16
n3:tvurceVysledku
Grepl, M. Fülöpová, Veronika Popa, Igor Soural, Miroslav Mcmaster, Claire Suzanne
s:issn
2156-8952
s:numberOfPages
4
n9:organizacniJednotka
15110