1393813-40-5Relevant academic research and scientific papers
Simple, rapid, and clean condensation of sulfonamide and maleic anhydride derivatives: Synthesis of novel 1H- Pyrrole-2,5-diones under heterogeneous conditions
Bougheloum, Chafika,Guezane Lakoud, Samia,Belghiche, Robila,Messalhi, Abdelrani
, p. 1344 - 1350 (2016)
H6P2W18O62is used as an efficient catalyst for the synthesis of novel N-substituted sulfonyl maleimides (1H-Pyrrole-2,5-diones) via the condensation of sulfonamide and maleic anhydride derivatives. The Dawson heteropolyacid was used with a catalytic amount of 2?mmol% in acetonitrile at reflux. The reuse of H6P2W18O62as heterogeneous catalyst several times without decrease in their activity, short reaction times, easy isolation of desired products with good to excellent yields shows the advantages of this novel methodology.
PYRIMIDINE SULFAMIDE DERIVATIVE AND PREPARATION METHOD AND MEDICAL APPLICATION THEREOF
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Paragraph 0102-0104, (2020/09/22)
Disclosed are a series of pyrimidine sulfamide compounds and applications thereof in preparing a drug for a disease related to an ETA receptor antagonist. In particular, disclosed is a derived compound represented by formula (I) or a tautomer or pharmaceutically acceptable composition thereof.
Synthesis and antitumor evaluation of novel sulfonylcycloureas derived from nitrogen mustard
Cheloufi,Belhani,Ouk,Zerrouki,Aouf,Berredjem
, p. 399 - 405 (2016/04/20)
A new series of sulfonylcycloureas derivatives have been synthesized and evaluated in vitro for their antitumor activity against four cancer cell lines (A431, Jurkat, U266, and K562). These compounds were prepared by the condensation of several sulfonamides (2am) with ethyl bis(2-chloroethyl)carbamate (1a). The relative cytotoxicity of these new derivatives in comparison to chlorambucil is reported.
Synthesis of new substituted N-sulfonyl pyrrolidine-2,5-dione using dawson-type heteropolyacid as catalyst
Bougheloum, Chafika,Belghiche, Robila,Messalhi, Abdelrani
supporting information, p. 269 - 276 (2015/04/27)
The synthesis of new series of pyrrolidine-2,5-diones having sulfonamide moieties is described. These compounds are synthesized in good yield in three steps (carbamoylation-sulfamoylation, deprotection and condensation) using a catalytic amount of H6P2W18O62 in acetonitrile under refluxing conditions.
An efficient method for the synthesis of novel n-acylsulfonamides using tin (IV) chloride as catalysts
Bouchareb, Fouzia,Boufas, Wahida,Cheloufi, Hadjer,Berredjem, Malika,Aouf, Nour-Eddine
, p. 587 - 595 (2014/06/09)
A series of novel N-acylsulfonamides derivatives were synthesized via direct condensation of parent sulfonamide with ethyl lactate as an acylating agent in the presence of tin (IV) chloride (SnCl4) as a Lewis acid catalyst. The sulfonamides were prepared, starting from chlorosulfonyl isocyanate (CSI), in three steps (carbamoylation, sulfamoylation, and deprotection) with excellent yields. Copyright
The discovery of N -[5-(4-bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy] ethoxy]-4-pyrimidinyl]- N ′-propylsulfamide (macitentan), an orally active, potent dual endothelin receptor antagonist
Bolli, Martin H.,Boss, Christoph,Binkert, Christoph,Buchmann, Stephan,Bur, Daniel,Hess, Patrick,Iglarz, Marc,Meyer, Solange,Rein, Josiane,Rey, Markus,Treiber, Alexander,Clozel, Martine,Fischli, Walter,Weller, Thomas
, p. 7849 - 7861 (2012/10/29)
Starting from the structure of bosentan (1), we embarked on a medicinal chemistry program aiming at the identification of novel potent dual endothelin receptor antagonists with high oral efficacy. This led to the discovery of a novel series of alkyl sulfamide substituted pyrimidines. Among these, compound 17 (macitentan, ACT-064992) emerged as particularly interesting as it is a potent inhibitor of ETA with significant affinity for the ET B receptor and shows excellent pharmacokinetic properties and high in vivo efficacy in hypertensive Dahl salt-sensitive rats. Compound 17 successfully completed a long-term phase III clinical trial for pulmonary arterial hypertension.
