A Cs 2 CO 3 -catalyzed azide-acetonitrile [3+2]-cycloaddition reaction of monosubstituted acetonitriles with aryl azides has been developed for the synthesis of 5-amino-1,2,3-triazoles.
Functionalized five-membered spirooxindoles were furnished in good yields and excellent stereoselectivities by using an effective Tomita zipper cyclization (TZC) reaction through organophosphine catalysis.
We present herein for the first time the asymmetric synthesis of drug-like spiranes through reflexive-Michael reaction by using 2-aminobuta-1,3-enyne catalysis under mild conditions.
Organocatalytic azide-ketone [3+2] cycloaddition (OrgAKC) of a variety of 1-aryl-2-(arylthio)ethanones and 1-alkyl-2-(alkylthio)ethanones with different aryl or alkyl azides is reported in dimethyl sulfoxide or solvent-free under ambient conditions to furnish 1,5-disubstituted 4-thio-1,2,3-triazoles in a regiospecific manner, which are further converted into useful 1,5-disubstituted 1,2,3-triazoles by treatment with Raney Ni at 25 °C for 1-3 h. Notable features of the OrgAKC reaction include high rate and selectivity, solvent-free conditions, easily available substrates and catalysts, a wide range of synthetic and medicinal applications, and excellent yields generating a vast library of triazoles.
An asymmetric organocatalytic arylideneacetone-olefin[ 4 + +2] cycloaddition reactiono favarietyo fa rylideneacetones and 1,3-indandione with different aldehydes is reported in toluenea ta mbient conditions to furnish the optically pure spiro compounds, whicha re further converted into medicinally usefuls piromentins by the Suzukir eaction. This asymmetric reaction has advantageous features such as high rate ands electivity,u ses easily availables ubstrates/catalysts,h as many synthetic/ medicinal applications,a nd gives excellent yields for generating av ast libraryo fc hiral spiro compounds.
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