- On the important transition of sugar-based surfactant as a microreactor for C-S coupling in water: From micelle to vesicle
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A reversible, temperature-induced micelle-to-vesicle transition of a sugar-based pseudogemini surfactant (C11D12) was employed for copper-catalyzed C-S coupling in water. The phase behavior and morphology of the C11D12 aqueous solution were investigated by DLS and cryo-TEM. The aggregates undergo a series of transitions upon increasing the temperature: spherical micelles were initially transformed into large vesicles, but they eventually transformed into smaller vesicles. The vesicular catalytic protocol accommodates an excellent substrate scope with moderate to high yields. The mechanisms of temperature-induced aggregate transition and vesicular catalysis were elucidated by experimental results and DFT calculations. It was revealed that the charge layer of the vesicle grants stronger nucleophilicity to the PhSO2-Cu-D12Ga intermediate. Furthermore, the aqueous reaction medium can be recycled and reused several times after easily separating the precipitated product.
- Ge, Xin,Lei, Qiuyun,Liao, Xiong,Liu, Xuemin,Song, Weili,Wu, Lei,Wu, Siyuan,Zhou, Shaodong
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- Synthesis method of 4-benzenesulfonylbenzoic acid
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The invention discloses a synthesis method of 4-benzenesulfonylbenzoic acid. The synthesis method comprises the synthesis route as followings: a benzene sulfinic acid sodium salt and p-halogenated benzaldehyde are utilized as raw materials, inorganic matt
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Paragraph 0036-0038
(2019/11/20)
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- Design, synthesis, characterization and antimicrobial evaluation of some heterocyclic condensed systems with bridgehead nitrogen from thiazolotriazole class
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In the present study, a series of new heterocyclic condensed systems with bridgehead nitrogen from the thiazolo[3,2-b][1,2,4]triazoles class was synthesized starting from some 4-(4-X-phenylsulfonyl)phenyl)-4H-1,2,4-triazole-3-thioles 1a-c (X=H, Cl, Br). The intermediates of S-alkylated 1,2,4-triazoles, 2-(5-(4-(4-X-phenylsulfonyl)phenyl)-2H-1,2,4-triazol-3-ylthio)-1-(4-fluorophenyl)ethanones 2a-c, were obtained by treatment of triazoles 1a-c with 2-bromo-4'-fluoroacetophenone. The 2-(4-(4-X-phenylsulfonyl)phenyl)-6-(4-fluorophenyl)thiazolo[3,2-b][1,2,4]triazoles 3a-c were obtained by cyclization of S-alkylated 1,2,4-triazoles 2a-c in sulfuric acid media, at 0°C. For the synthesis of 2-(4-(4-X-phenylsulfonyl)phenyl)-5-(4-fluorobenzylidene)-thiazolo[3,2-b][1,2,4]triazol-6(5H)-ones 4a-c, the triazoles 1a-c were treated with 4-fluorobenzaldehyde, chloroacetic acid and anhydrous sodium acetate, in the presence of acetic acid and acetic anhydride. The structures of the newly synthesized compounds have been confirmed by elemental analysis and spectral methods (IR, 1H-NMR,13C-NMR, MS). The antimicrobial activity of all new compounds has been screened against some bacteria and yeasts.
- Barbuceanu, Stefania-Felicia,Draghici, Constantin,Barbuceanu, Florica,Bancescu, Gabriela,Saramet, Gabriel
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p. 694 - 700
(2015/11/27)
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- 4- { [ ( PYRIDIN- 3 - YL -METHYL) AMINOCARBONYL] AMINO} BENZENE - SULFONE DERIVATIVES AS NAMPT INHIBITORS FOR THERAPY OF DISEASES SUCH AS CANCER
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The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes. An embodiment of the invention is the provision of a compound of Formula IIIA.
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Page/Page column 241
(2012/03/26)
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- New heterocyclic compounds from 1,2,4-triazole and 1,3,4-thiadiazole class bearing diphenylsulfone moieties. Synthesis, characterization and antimicrobial activity evaluation
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Some new 5-(4-(4-X-phenylsulfonyl)phenyl)-4-(R)-2H-1,2,4-triazol-3(4H)- thiones 4a,b; 5a,b and 5-(4-(4-X-phenylsulfonyl)phenyl)-N-(R)-1,3,4-thiadiazol- 2-amines 6a,b; 7a,b were obtained by cyclization of new N1-[4-(4-X- phenylsulfonyl)benzoyl]-N4-(R)-thiosemicarbazides 2a,b; 3a,b (X = H, Br). The 1,2,4-triazoles were synthesized by intramolecular cyclization of acylthiosemicarbazides, in basic media. On the other hand, 1,3,4-thiadiazoles were obtained from same acylthiosemicarbazides, in acidic media. These new intermediates from thiosemicarbazide class were afforded by the reaction of 4-(4-X-phenylsulfonyl)benzoic acids hydrazides (X = H, Br) 1a,b with 4-trifluoromethoxyphenyl or 3,4,5-trimethoxyphenyl isothiocyanate. The newly synthesized compounds were characterized by IR, 1H NMR, 13C NMR, MS and elemental analysis. All the new compounds were screened for their antimicrobial activity against some bacteria (Staphylococcus aureus ATCC 25923, Bacillus cereus ATCC 13061, Escherichia coli ATCC 25922, Enterobacter cloacae ATCC 49141, Acinetobacter baumannii ATCC 19606 and Pseudomonas aeruginosa ATCC 27853) and yeasts (Candida albicans ATCC 90028 and Candida parapsilosis ATCC 22019).
- Barbuceanu, Stefania-Felicia,Saramet, Gabriel,Almajan, Gabriela Laura,Draghici, Constantin,Barbuceanu, Florica,Bancescu, Gabriela
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scheme or table
p. 417 - 423
(2012/04/10)
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- DIHYDROOROTATE DEHYDROGENASE INHIBITORS
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The invention relates to compounds of formula (I) wherein R1, R2, X1, X2, Y, Ra, Rb, Q have the meanings given in claim 1. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis and also in the treatment of cancer disorders.
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Page/Page column 109
(2010/11/03)
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- Copper(II) and uranyl(II) complexes with acylthiosemicarbazide: Synthesis, characterization, antibacterial activity and effects on the growth of promyelocytic leukemia cells HL-60
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New chelates of N1-[4-(4-X-phenylsulfonyl)benzoyl]-N4-butyl-thiosemicarbazide (X = H, Cl, Br) with Cu2+ and UO22+ have been prepared and characterized by analytical and physico-chemical techniques such as magnetic susceptibility measurements, elemental and thermal analyses, electronic, ESR and IR spectral studies. Room temperature ESR spectra of Cu(II) complexes yield {g} values characteristic of distorted octahedral and pseudo-tetrahedral geometry. Infrared spectra indicate that complexes contain six-coordinate uranium atom with the ligand atoms arranged in an equatorial plane around the linear uranyl group. Effects of these complexes on the growth of human promyelocytic leukemia cells HL-60 and their antibacterial activity (against Staphylococcus epidermidis ATCC 14990, Bacillus subtilis ATCC 6633, Bacillus cereus ATCC 14579, Pseudomonas aeruginosa ATCC 9027 and Escherichia coli ATCC 11775 strains) were studied comparatively with that of free ligands.
- Angelusiu, Madalina Veronica,Almajan, Gabriela Laura,Rosu, Tudor,Negoiu, Maria,Almajan, Eva-Ruxandra,Roy, Jenny
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scheme or table
p. 3323 - 3329
(2009/12/01)
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- Flow-vacuum pyrolysis of polycyclic compounds. 251. Pyrolysis of some 3-mercapto-5-substituted-1,2,4-triazoles
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The flow-vacuum pyrolysis (FVP) of the 3-mercapto-5-substituted-1,2,4- triazoles 5a-c, between 475°C - 750°C, at 2 mm Hg, in inert atmosphere (4mL/min argon flow rate) and quartz pyrolysis tube (60 cm length, 1 cm internal diameter, quartz chips filling 30 mm long) afforded a complex mixture with cyano-diphenyl-sulphones 12a-c and corresponding diphenylsulphones 13a-c as main products. The reaction products were identified by GC/MS. A radical mechanism is suggested in order to explain the formation of the main reaction products.
- Istrati, Daniela,Popescu, Angela,Mihaiescu, Dan,Saramet, Ioana,Bala?u, Mihaela C.
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scheme or table
p. 497 - 503
(2009/05/11)
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- Gonadotropin releasing hormone receptor antagonists
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The present invention relates to Gonadotropin Releasing Hormone (“GnRH”) (also known as Leutinizing Hormone Releasing Hormone) receptor antagonists.
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Page/Page column 77
(2010/02/15)
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- Synthesis and Biological Activity of a Series of Diaryl-Substituted α-Cyano-β-hydroxypropenamides, a New Class of Anthelmintic Agents
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A series of α-cyano-β-hydroxypropenamides was prepared and tested for anthelmintic activity. α-Cyano-β-hydroxy-N--3-propenamide (1) showed good activity against the nematode Nematospirodes dubius in a mixed parasite infection in mice; several of the analogues were also effective against the cestode Hymenolepis nana.In sheep trials, 1 caused 100percent reduction of the hematophagous nematode Haemonchus contortus after a single dose of 20 mg/kg but did not show satisfactory control of Trichostrongylus colubriformis or Ostertagia circumcincta.Against the liver fluke Fasciola hepatica, 1 suppressed egg production but only temporarily, suggesting that the adult flukes were not eliminated.Mechanism of action studies on 1 using Ascaris mitochondria showed it to be an uncoupler of oxidative phosphorylation.
- Sjogren, Eric B.,Rider, Michael A.,Nelson, Peter H.,Bingham, Stanford,Poulton, Anthony L.,et al.
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p. 3295 - 3301
(2007/10/02)
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