Tag: M.W=150-200

Hou, Hongcen; Zhao, Yongli; Pu, Shouzhi; Chen, Junmin published the artcile< Rhodium-catalyzed direct C-H bond alkynylation of aryl sulfonamides with bromoalkynes>, Application of C6H6ClNO2S, the main research area is alkynyl benzenesulfonamide preparation; aryl sulfonamide bromoalkyne mono alkynylation rhodium catalyst; benzosultam preparation; bromoalkyne aryl sulfonamide alkynylation intramol cyclization cascade rhodium catalyst.

An efficient protocol for the synthesis of ortho-(1-alkynyl)benzenesulfonamides I [R = H, 4-Me, 4-OCF3, etc.] was developed via rhodium-catalyzed direct ortho-mono-alkynylation of aryl sulfonamides with triisopropylsilyl (TIPS)-substituted bromoalkyne. While triethylsilyl or trimethylsilyl (TES or TMS)-substituted bromoalkyne was also amenable to the alkynylation, affording six membered benzosultams II [R1 = TMS, TES; R2 = H, 6-Me, 6-Et, 6-OMe] via the alkynylation/intramol. cyclization cascade reaction. The present protocol displayed high functional group tolerance and broad substrate scope under an air atm. in good to high yields. Mechanistic studies indicated that the reaction proceeded by a turnover limiting C-H activation step and a plausible mechanism was proposed.

Organic & Biomolecular Chemistry published new progress about Alkynes Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 6961-82-6 belongs to class amides-buliding-blocks, and the molecular formula is C6H6ClNO2S, Application of C6H6ClNO2S.

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

Hou, Yunlei; Wu, Shasha; Ma, Longsheng; Bai, Jinying; Liu, Zijian; Zhao, Yanfang published the artcile< Design, synthesis and antitumor activity of novel 6,7-dimethoxyquinazoline derivatives containing diaryl urea moiety>, Product Details of C9H12N2O3, the main research area is sorafenib dimethoxyquinazoline diaryl urea scaffold antitumor lung gastric cancer.

A series of 6,7-dimethoxyquinazoline derivatives connected by diaryl urea scaffolds was designed, synthesized and their in vitro antitumor activities were evaluated. Most of them showed an excellent potency against the four tested cancer cell lines as compared with sorafenib. Particularly, a promising compound 20 was identified, which showed the most potent antitumor activities with IC50 values of 0.08, 0.09, 0.16 and 0.19 μmol/L against H460, HT-29, MKN-45 and MDA-MB-231 cell lines, resp. The structure-activity relationship(SAR) anal. indicated that compounds with dimethylamino or diethylamino group at the C4 position of 6,7-dimethoxyquinazoline moiety exhibited superior activities than compounds bearing morpholino groups.

Chemical Research in Chinese Universities published new progress about Antitumor agents. 5004-88-6 belongs to class amides-buliding-blocks, and the molecular formula is C9H12N2O3, Product Details of C9H12N2O3.

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

Chen, Hui; Li, Peng; Qin, Rongfei; Yan, Hong; Li, Gang; Huang, Haihong published the artcile< DMAP-Catalyzed One-Pot Synthesis of Quinazoline-2,4-diones from 2-Aminobenzamides and Di-tert-butyl Dicarbonate>, Category: amides-buliding-blocks, the main research area is quinazolinedione preparation; aminobenzamide di tert butyl dicarbonate heterocyclization DMAP catalyst.

The one-pot synthesis of quinazoline-2,4-diones was developed in the presence of 4-dimethylaminopyridine (DMAP) by metal-free catalysis. The com. available (Boc)2O acted as a key precursor in the construction of the 2-position carbonyl of quinazolinediones. The p-methoxybenzyl (PMB)-activated heterocyclization could smoothly proceed at room temperature instead of the microwave condition. This strategy is compatible with a variety of substrates with different functional groups. Furthermore, this protocol was utilized to smoothly prepare Zenarestat with a total yield of 70%.

ACS Omega published new progress about Benzamides Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation) (amino). 5004-88-6 belongs to class amides-buliding-blocks, and the molecular formula is C9H12N2O3, Category: amides-buliding-blocks.

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

Chinn, Alex J.; Sedillo, Kassandra; Doyle, Abigail G. published the artcile< Phosphine/Photoredox Catalyzed Anti-Markovnikov Hydroamination of Olefins with Primary Sulfonamides via α-Scission from Phosphoranyl Radicals>, Quality Control of 6961-82-6, the main research area is secondary sulfonamide preparation; primary sulfonamide alkene antiMarkovnikov hydroamination phosphine iridium photocatalyst.

A dual phosphine and photoredox catalytic system that enables direct formation of sulfonamidyl radicals from primary sulfonamides RSO2NH2 (R = 4-tert-butylphenyl, Me, cyclopropyl, thiophen-2-yl, etc.) was reported. Mechanistic investigations support that the N-centered radical is generated via α-scission of the P-N bond of a phosphoranyl radical intermediate, formed by sulfonamide nucleophilic addition to a phosphine radical cation. As compared to the recently well-explored β-scission chem. of phosphoranyl radicals, this strategy is applicable to activation of N-based nucleophiles and is catalytic in phosphine. The application of this activation strategy to an intermol. anti-Markovnikov hydroamination of unactivated olefins (such as cyclohexene, hex-1-ene, styrene, etc.) with primary sulfonamides RSO2NH2 is highlighted. A range of structurally diverse secondary sulfonamides [such as 4-(tert-butyl)-N-hexylbenzenesulfonamide, 4-(tert-butyl)-N-(3-phenylpropyl)benzenesulfonamide, 2-chloro-N-cyclohexylbenzenesulfonamide, etc.] can be prepared in good to excellent yields under mild conditions.

Journal of the American Chemical Society published new progress about Alkenes Role: RCT (Reactant), RACT (Reactant or Reagent). 6961-82-6 belongs to class amides-buliding-blocks, and the molecular formula is C6H6ClNO2S, Quality Control of 6961-82-6.

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

Ogita, H.; Isobe, Y.; Takaku, H.; Sekine, R.; Goto, Y.; Misawa, S.; Hayashi, H. published the artcile< Synthesis and structure-activity relationship of diarylamide derivatives as selective inhibitors of the proliferation of human coronary artery smooth muscle cells>, Recommanded Product: 2-Amino-4,5-dimethoxybenzamide, the main research area is diarylamide derivative antiproliferative SAR preparation coronary artery.

A series of diarylamide derivatives were synthesized and evaluated for their inhibitory activities against human coronary artery smooth muscle cells (SMCs) and human coronary artery endothelial cells (ECs). I was superior to the lead compound, tranilast, in terms of the potency of the activity and cell selectivity. A series of diarylamide derivatives were synthesized and evaluated for their inhibitory activities against the proliferation of human coronary artery smooth muscle cells (SMCs) and human coronary artery endothelial cells (ECs).

Bioorganic & Medicinal Chemistry Letters published new progress about Arterial endothelium, coronary artery endothelium. 5004-88-6 belongs to class amides-buliding-blocks, and the molecular formula is C9H12N2O3, Recommanded Product: 2-Amino-4,5-dimethoxybenzamide.

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

Meng, Chong; Liu, Peng; Nguyen, Thanh Tung; Han, Xingyou; Li, Feng published the artcile< N-Methylation of Amines with Methanol in Aqueous Solution Catalyzed by a Water-Soluble Metal-Ligand Bifunctional Dinuclear Iridium Catalyst>, Product Details of C6H6ClNO2S, the main research area is sulfonamide methanol iridium catalyst methylation green chem; methylsulfonamide preparation; amine methanol iridium catalyst methylation; methylamine preparation green chem.

The N-methylation of amines with methanol in aqueous solution was proposed and accomplished by using a water-soluble metal-ligand bifunctional dinuclear iridium catalyst. In the presence of [(Cp*IrCl)2(thbpym)][Cl]2 (1 mol%), a range of desirable products were obtained in high yields under environmentally benign conditions. Notably, this research exhibited the potential of transition metal-catalyzed the activation of methanol as a C1 source for the construction of C-N bond in aqueous solution

Journal of Organic Chemistry published new progress about Amines Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 6961-82-6 belongs to class amides-buliding-blocks, and the molecular formula is C6H6ClNO2S, Product Details of C6H6ClNO2S.

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

Raffa, Demetrio; Maggio, Benedetta; Plescia, Fabiana; Cascioferro, Stella; Raimondi, Maria Valeria; Cancemi, Gabriella; D’Anneo, Antonella; Lauricella, Marianna; Cusimano, Maria Grazia; Bai, Ruoli; Hamel, Ernest; Daidone, Giuseppe published the artcile< Synthesis, antiproliferative activity and possible mechanism of action of novel 2-acetamidobenzamides bearing the 2-phenoxy functionality>, Formula: C9H12N2O3, the main research area is preparation acetamido benzamide derivative cancer; 2-(2-Phenoxyacetamido)benzamides; Antiproliferative activity; Apoptosis; G0/G1 arrest; Pro-caspase 3.

Several new 2-(2-phenoxyacetamido)benzamides 17a-v, 21 and 22 were synthesized by stirring in pyridine the acid chlorides 16a-e and the appropriate5-R-4-R1-2-aminobenzamide 15a-e and initially evaluated in vitro for antiproliferative activity against the K562 (human chronic myelogenous leukemia) cell line. Some of synthesized compounds were evaluated for their in vitro antiproliferative activity against the full NCI tumor cell line panel derived from nine clin. isolated cancer types (leukemia, non-small cell lung, colon, CNS, melanoma, ovarian, renal, prostate and breast). The most active compounds caused an arrest of K562 cells in the G0-G1 phase of cell cycle and induction of apoptosis, which was mediated by caspase activation.

Bioorganic & Medicinal Chemistry published new progress about Antiproliferative agents. 5004-88-6 belongs to class amides-buliding-blocks, and the molecular formula is C9H12N2O3, Formula: C9H12N2O3.

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

Dugad, L. B.; Cooley, C. R.; Gerig, J. T. published the artcile< NMR studies of carbonic anhydrase-fluorinated benzenesulfonamide complexes>, Computed Properties of 1524-40-9, the main research area is carbonic anhydrase fluorobenzenesulfonamide complex NMR.

19F NMR was used to examine complexes formed by 2-fluoro-, 3-fluoro-, and 2,5-difluorobenzenesulfonamide and human carbonic anhydrase (CA) isoenzymes I and II. The results showed that all 3 inhibitors formed complexes with both isoenzymes that had 2:1 inhibitor/enzyme stoichiometry. The 19F spectra observed for all inhibitor-isoenzyme combinations were consistent either with rapid rotation of the aromatic ring of the inhibitor in the complexes or with preferential binding of only 1 of the 2 possible conformations of the inhibitors that were isomeric by virtue of rotation about the C1-C4 bond of the fluoro aromatic ring. Because ring rotation is slow in the case of the pentafluorobenzenesulfonamide-CA I complex, selective binding of rotamers is the explanation of these observations presently favored. A computer graphics study showed that formation of 2:1 complexes of CA I is feasible without the appreciable distortion of the protein tertiary structure found in the crystalline state.

Biochemistry published new progress about NMR (nuclear magnetic resonance). 1524-40-9 belongs to class amides-buliding-blocks, and the molecular formula is C6H6FNO2S, Computed Properties of 1524-40-9.

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

Whalley, David M.; Duong, Hung A.; Greaney, Michael F. published the artcile< Alkene Carboarylation through Catalyst-Free, Visible Light-Mediated Smiles Rearrangement>, Safety of o-Chlorobenzenesulfonamide, the main research area is aliphatic ester preparation carboarylation arenesulfonamide alkene Truce Smiles rearrangement; acetamide preparation tandem photoredox carboarylation Truce Smiles rearrangement; aromatic substitution; arylation; photochemistry; radical reactions; rearrangement.

A light-mediated Truce-Smiles arylative rearrangement is described that proceeds in the absence of any photocatalyst. The protocol creates two C-C bonds from simple starting materials, with the installation of an aryl ring and a difluoroacetate moiety across unactivated alkenes. The reaction proceeds via a radical mechanism, utilizing a light-mediated reduction of Et bromodifluoroacetate by N,N,N’,N’-tetramethylethylenediamine (TMEDA) to set up intermol. addition to an unactivated alkene, followed by Truce-Smiles rearrangement.

Chemistry – A European Journal published new progress about Acetamides Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 6961-82-6 belongs to class amides-buliding-blocks, and the molecular formula is C6H6ClNO2S, Safety of o-Chlorobenzenesulfonamide.

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