Category: 25999-04-6

Appel, Rolf; Montenarh, Mathias published the artcile< Addition reaction of N,N-dialkylsulfamides, tertiary amines, and phosphines with fluorosulfonyl isocyanate>, Category: amides-buliding-blocks, the main research area is addition sulfamide fluorosulfonyl isocyanate; amine fluorosulfonyl isocyanate reaction; phosphine fluorosulfonyl isocyanate reaction; urea fluorosulfonyl sulfamoyl.

Addition of RSO2NH2 to FSO2NCO gave 72-98% RSO2NHCONHSO2F (R = Me2N, piperidino, morpholino, MeO), thermal decomposition of which gave 20-48% RSO2F (R = Me2N, piperidino, morpholino). The reaction of FSO2NCO with amines and phosphines gave 91-99% 1:1 adducts RR12E+CON-SO2F (RR12E = Et3N, pyridine, Me3P, PhEt2P, MePh2P, Ph3P).

Chemische Berichte published new progress about Addition reaction. 25999-04-6 belongs to class amides-buliding-blocks, and the molecular formula is C4H10N2O3S, Category: amides-buliding-blocks.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Jiang, Yutong; Andrews, Steven W.; Condroski, Kevin R.; Buckman, Brad; Serebryany, Vlad; Wenglowsky, Steve; Kennedy, April L.; Madduru, Machender R.; Wang, Bin; Lyon, Michael; Doherty, George A.; Woodard, Benjamin T.; Lemieux, Christine; Do, Mary Geck; Zhang, Hailong; Ballard, Joshua; Vigers, Guy; Brandhuber, Barbra J.; Stengel, Peter; Josey, John A.; Beigelman, Leonid; Blatt, Lawrence; Seiwert, Scott D. published the artcile< Discovery of Danoprevir (ITMN-191/R7227), a Highly Selective and Potent Inhibitor of Hepatitis C Virus (HCV) NS3/4A Protease>, Safety of Morpholine-4-sulfonamide, the main research area is danoprevir macrocyclic peptidomimetic acylsulfonamide preparation inhibitor HCV NS3 protease.

HCV serine protease NS3 represents an attractive drug target because it is not only essential for viral replication but also implicated in the viral evasion of the host immune response pathway through direct cleavage of key proteins in the human innate immune system. Through structure-based drug design and optimization, macrocyclic peptidomimetic mols. bearing both a lipophilic P2 isoindoline carbamate and a P1/P1′ acylsulfonamide/acylsulfamide carboxylic acid bioisostere were prepared that possessed subnanomolar potency against the NS3 protease in a subgenomic replicon-based cellular assay (Huh-7). Danoprevir (compound 49) was selected as the clin. development candidate for its favorable potency profile across multiple HCV genotypes and key mutant strains and for its good in vitro ADME profiles and in vivo target tissue (liver) exposures across multiple animal species. X-ray crystallog. studies elucidated several key features in the binding of danoprevir to HCV NS3 protease and proved invaluable to the iterative structure-based design strategy of the authors.

Journal of Medicinal Chemistry published new progress about Antiviral agents. 25999-04-6 belongs to class amides-buliding-blocks, and the molecular formula is C4H10N2O3S, Safety of Morpholine-4-sulfonamide.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Lohaus, Gerhard published the artcile< Preparation and reactions of aryloxysulfonyl isocyanates>, Electric Literature of 25999-04-6, the main research area is aryloxysulfonyl isocyanate; piperazine sulfamoyl; morpholine sulfamoyl; heterocyclo sulfamide.

Reaction of phenols ROH (e.g. R = Ph, p-MeC6H4, m-ClC6H4, 2,4,6-Cl3C6H2, p-NCC6H4) with ClSO2NCO gave 40-79% ROSO2NCO (I). Hydrolysis of I yielded nearly quant. ROSO2NH2 (II). I are highly active compounds and the reactivity corresponded to the acidity of the starting phenols. II was useful for the transfer of SO2NH2 groups, e.g. to amines.

Chemische Berichte published new progress about 25999-04-6. 25999-04-6 belongs to class amides-buliding-blocks, and the molecular formula is C4H10N2O3S, Electric Literature of 25999-04-6.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Belhani, Billel; Berredjem, Malika; Le Borgne, Marc; Bouaziz, Zouhair; Lebreton, Jacques; Aouf, Nour-Eddine published the artcile< A one-pot three-component synthesis of novel α-sulfamidophosphonates under ultrasound irradiation and catalyst-free conditions>, Safety of Morpholine-4-sulfonamide, the main research area is alpha sulfamidophosphonate preparation green chem; benzaldehyde sulfamide trialkylphosphite sonication three component reaction.

An efficient and convenient one-pot synthesis of novel α-sulfamidophosphonates was described via a three-component reaction. This reaction was carried out through a three component condensation reaction of sulfamide, an aromatic aldehyde and trialkylphosphite under conventional/ultrasonic techniques, catalyst-free and solvent-free conditions. This methodol. was established with many advantages, including mild reaction conditions, short reaction times, good yields, simple work-up procedures and environmental friendliness.

RSC Advances published new progress about Condensation reaction. 25999-04-6 belongs to class amides-buliding-blocks, and the molecular formula is C4H10N2O3S, Safety of Morpholine-4-sulfonamide.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Cheloufi, H.; Belhani, B.; Ouk, T. S.; Zerrouki, R.; Aouf, N.-E.; Berredjem, M. published the artcile< Synthesis and antitumor evaluation of novel sulfonylcycloureas derived from nitrogen mustard>, Product Details of C4H10N2O3S, the main research area is sulfonylcyclourea derive nitrogen mustard; Antitumor; Cancer; Nitrogen mustard; Sulfonamides; Sulfonylcycloureas.

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 (2a-m) with Et bis(2-chloroethyl)carbamate (1a). The relative cytotoxicity of these new derivatives in comparison to chlorambucil is reported.

Molecular Diversity published new progress about Antitumor agents. 25999-04-6 belongs to class amides-buliding-blocks, and the molecular formula is C4H10N2O3S, Product Details of C4H10N2O3S.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Alcaraz, Lilian; Bennion, Colin; Morris, James; Meghani, Premji; Thom, Stephen M. published the artcile< Novel N-aryl and N-heteroaryl sulfamide synthesis via palladium cross-coupling>, Quality Control of 25999-04-6, the main research area is sulfonamide aryl halide cross coupling palladium phosphine ligand; aryl sulfonamide preparation; phosphine palladium cross coupling catalyst.

An efficient synthesis of N-aryl and N-heteroaryl sulfamides, e.g., I, via an intermol. palladium-catalyzed coupling process has been developed. The reactions proceeded with good to excellent yields and tolerated a wide range of functional groups.

Organic Letters published new progress about Arenesulfonamides Role: SPN (Synthetic Preparation), PREP (Preparation). 25999-04-6 belongs to class amides-buliding-blocks, and the molecular formula is C4H10N2O3S, Quality Control of 25999-04-6.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Hedayatullah, Mir; Hugueny, Jean Claude published the artcile< Regioselective transfer of the sulfamoyl group on aminopyrimidines and -purines>, Application of C4H10N2O3S, the main research area is sulfamoylation aminopyrimidine aminopurine regioselectivity; pentachlorophenyl sulfamate sulfamoylating agent.

The regioselective transfer of the sulfamoyl group, to the exocyclic NH2 group of cytosine, thiamine, adenine and guanine is carried out in 86-98% yield by reaction with C6Cl5O3SNH2 in pyridine at 100°.

Phosphorus and Sulfur and the Related Elements published new progress about Regiochemistry. 25999-04-6 belongs to class amides-buliding-blocks, and the molecular formula is C4H10N2O3S, Application of C4H10N2O3S.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Appel, Rolf; Montenarh, Mathias published the artcile< Reactions of N,N-dialkyl- and N,N-diarylsulfamides with chlorosulfonyl isocyanate>, Product Details of C4H10N2O3S, the main research area is sulfamide reaction chlorosulfonyl isocyanate; urea sulfamoyl.

Reaction of RR1NSO2NH2 with ClSO2NCO gave RR1NSO2NHCONHSO2Cl [R = R1 = Me, Et, or Ph; NRR1 = piperidino or morpholino], which were hydrolyzed to give RR1NSO2NHCONH2.

Chemische Berichte published new progress about 25999-04-6. 25999-04-6 belongs to class amides-buliding-blocks, and the molecular formula is C4H10N2O3S, Product Details of C4H10N2O3S.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Lange, Jos H. M.; Van Stuivenberg, Herman H.; Veerman, Willem; Wals, Henri C.; Stork, Bob; Coolen, Hein K. A. C.; McCreary, Andrew C.; Adolfs, Tiny J. P.; Kruse, Chris G. published the artcile< Novel 3,4-diarylpyrazolines as potent cannabinoid CB1 receptor antagonists with lower lipophilicity>, Application In Synthesis of 25999-04-6, the main research area is aminosulfonyl isothiocyanate diarylpyrazoline addition; aminosulfonylcarbamoyl diarylpyrazoline preparation chlorination amination; diarylpyrazoline derivative cannabinoid CB1 receptor antagonist.

3,4-Diarylpyrazolines as potent CB1 receptor antagonists with lipophilicity lower than that of SLV319 are described. The key change was the replacement of the arylsulfonyl group in the original series by a dialkylaminosulfonyl moiety. The absolute configuration (4S) of enantiomer I was established by X-ray diffraction anal. and I showed a close mol. fit with rimonabant in a CB1 receptor-based model. II exhibited the highest CB1 receptor affinity (Ki = 24 nM) in this series, as well as very potent CB1 antagonistic activity (pA 2 = 8.8) and a high CB1/CB2 subtype selectivity (∼147-fold).

Bioorganic & Medicinal Chemistry Letters published new progress about Cannabinoid receptor 1 Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 25999-04-6 belongs to class amides-buliding-blocks, and the molecular formula is C4H10N2O3S, Application In Synthesis of 25999-04-6.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Karatas, Mehmet; Chaikuad, Apirat; Berger, Bianca; Kubbutat, Michael H. G.; Totzke, Frank; Knapp, Stefan; Kunick, Conrad published the artcile< 7-(2-Anilinopyrimidin-4-yl)-1-benzazepin-2-ones designed by a ""cut and glue"" strategy are dual Aurora A/VEGF-R kinase inhibitors>, Related Products of 25999-04-6, the main research area is anilinopyrimidinyl benzazepinone AuroraA VEGFR kinase inhibitor; Aurora kinase; X-ray structure analysis; anilinopyrimidine; benzazepinone; molecular docking; protein kinase inhibitor; sulfamide.

Although overexpression and hyperactivity of protein kinases are causative for a wide range of human cancers, protein kinase inhibitors currently approved as cancer drugs address only a limited number of these enzymes. To identify new chemotypes addressing alternative protein kinases, the basic structure of a known PLK1/VEGF-R2 inhibitor class was formally dissected and reassembled. The resulting 7-(2-anilinopyrimidin-4-yl)-1-benzazepin-2-ones were synthesized and proved to be dual inhibitors of Aurora A kinase and VEGF receptor kinases. Crystal structures of two representatives of the new chemotype in complex with Aurora A showed the ligand orientation in the ATP binding pocket and provided the basis for rational structural modifications. Congeners with attached sulfamide substituents retained Aurora A inhibitory activity. In vitro screening of two members of the new kinase inhibitor family against the cancer cell line panel of the National Cancer Institute (NCI) showed antiproliferative activity in the single-digit micromolar concentration range in the majority of the cell lines.

Molecules published new progress about Antiproliferative agents. 25999-04-6 belongs to class amides-buliding-blocks, and the molecular formula is C4H10N2O3S, Related Products of 25999-04-6.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics