173202-24-9Relevant academic research and scientific papers
Highly stereoselective monofluoroolefination: Facile access to (E)-α-fluorinated arylvinyl sulfones from trifluoromethyl α-fluorinated arylsulfonyl gem-diols
Fang, Xiang,Zhou, Jun,Wang, Wang,Yang, Xueyan,Wu, Fanhong
supporting information, (2020/04/28)
An excellent stereoselective direct synthesis of trisubstituted (E)-α-fluorinated arylvinyl sulfones employing trifluoromethyl α-fluorinated arylsulfonyl gem-diols and aryl aldehydes under mild reaction conditions has been developed, which affords α-fluorinated arylvinyl sulfones in high yields with E-isomer only. The desired products can be further transformed into more useful fluoroolefins through debenzenesulfonyl process.
Construction of N-Boc monofluoromethyl aryl sulfones via Mannich reaction of α-amido sulfones with trifluoromethyl α-fluorinated arylsulfonyl gem-diols
Fang, Xiang,Wang, Wang,Wu, Fanhong,Yang, Xueyan
supporting information, (2020/08/19)
A mild and efficient nucleophilic monofluoromethylation of α-amido sulfones with trifluoromethyl α-fluorinated arylsulfonyl gem-diols as new building blocks has been developed, which affords N-Boc monofluoromethyl aryl sulfones in good yields with appropriate 5:1 diastereomeric ratio.
Base-free Enantioselective C(1)-Ammonium Enolate Catalysis Exploiting Aryloxides: A Synthetic and Mechanistic Study
McLaughlin, Calum,Slawin, Alexandra M. Z.,Smith, Andrew D.
supporting information, p. 15111 - 15119 (2019/11/05)
An isothiourea-catalyzed enantioselective Michael addition of aryl ester pronucleophiles to vinyl bis-sulfones via C(1)-ammonium enolate intermediates has been developed. This operationally simple method allows the base-free functionalization of aryl esters to form α-functionalized products containing two contiguous tertiary stereogenic centres in excellent yield and stereoselectivity (all ≥99:1 er). Key to the success of this methodology is the multifunctional role of the aryloxide, which operates as a leaving group, Br?nsted base, Br?nsted acid and Lewis base within the catalytic cycle. Comprehensive mechanistic studies, including variable time normalization analysis (VTNA) and isotopologue competition experiments, have been carried out. These studies have identified (i) orders of all reactants; (ii) a turnover-limiting Michael addition step, (iii) product inhibition, (iv) the catalyst resting state and (v) catalyst deactivation through protonation.
CARBACEPHEM β-LACTAM ANTIBIOTICS
-
Page/Page column 91, (2010/04/06)
Carbacephem -lactam antibiotics having structure (I) are disclosed, including stereoisomers, pharmaceutically acceptable salts, esters and prodrugs thereof, wherein Ar1, Ar2, R1 and R2 are as defined herein. The compounds are useful for the treatment of bacterial infections, in particular those caused by methicillin-resistant Staphylococcus spp.
CARBACEPHEM BETA-LACTAM ANTIBIOTICS
-
Page/Page column 64-65; 87, (2010/11/05)
Carbacephem β-lactam antibiotics having chemical structures (I) and (II) are disclosed: including stereoisomers, pharmaceutically acceptable salts, esters and prodrugs thereof, wherein Ar2, R1, R2 and R6 are as defined herein. The compounds are useful for the treatment of bacterial infections, in particular those caused by methicillin-resistant Staphylococcus spp.
HALOALKYL HETEROARYL BENZAMIDE COMPOUNDS
-
Page/Page column 129-130, (2010/12/17)
A new class of haloalkyl heteroaryl benzamides is described. These compounds show strong activity against hepatitis viruses.
Regio- and stereo-selective synthesis of trifluoromethylated isoxazolidines by 1,3-dipolar cycloaddition of 1,1,1-trifluoro-3-phenylsulfonylpropene with nitrones, and their conversion into trifluoromethylated syn-3-amino alcohols
Tsuge, Hiroyasu,Okano, Takashi,Eguchi, Shoji
, p. 2761 - 2766 (2007/10/02)
1,1,1-Trifluoro-3-phenylsulfonylpropene 1, a useful synthetic precursor for trifluoromethylated compounds, has been prepared from methyl phenyl sulfone 2 and ethyl trifluoroacetate.The 1,3-dipolar cycloaddition of 1 with various nitrones 5a-f gave 5-trifl
