24 research outputs found
A novel and short convergent approach for <i style="">N</i>-aryl-5-aminomethyl-2-oxazolidinone derivatives Linezolid and DUP-721
1236-1238A new convergent and short approach for
oxazolidinone class of antibacterial agents, Linezolid and DUP-721, has been
achieved by condensing 3-chloro-2-((phenoxycarbonyl)oxy) propyl azide with aryl
amine followed by reductive acetylation. This one pot approach for N-aryl-5-azidomethyl- 2-oxazolidinone
could provide access for rapid preparation of various oxazolidinone analogues
A facile synthesis of 2-((5<i style="">R</i>)-2-oxo-5-oxazolidinyl)methyl)-1<i style="">H</i>-isoindole-1,3(2<i style="">H</i>)-dione
1264-1268Synthesis of
enantiomerically pure 2-((5R)-2-oxo-5-oxazolidinyl)
methyl)-1H-isoindole-1,3(2H)-dione, a key precursor in the
preparation of oxazolidinone class of antibacterial agents starting from (S)-epichlorohydrin has been achieved
Studies on synthesis and anti-bacterial activity of novel 4-substituted phenyl-2-oxo-1,3-oxazolidine-5-carboxylates<sup> †</sup>
957-963Regioselective
opening of glycidic esters with sodium azide gives azido alcohols, which are converted
to novel 4- substitutcd phenyl-2-oxo-1, 3-oxazolidine-5-carboxylates by various
methods. These compounds are tested for in vitro antibacterial activity against
Staphylococcus aureous, E. faecalis and E. faecium.</i
Unusual migrations and cyclization in the preparation of β-azido alcohols from β-hydroxy esters<sup>†</sup>
2719-2723Migration of TBDMS and Boc groups from 2o
alcohols to 1o alcohols during the reduction of β-hydroxy esters
has been observed.Also, unusual cyclization has been noticed during
tosylation of benzylic alcohol in tert-butyl
((2R)-2-hydroxy-2- phenyl ethyl)carbonate with SN2
in version
Studies on stereoselective synthesis of ethyl <i>anti-</i>4-substituted<i> </i>phenyl-2-oxo-1,3-oxazolidine-5-carboxylates and their anti-bacterial activity
2683-2688ethyl anti-4-substituted phenyl-2-oxo-1,3-oxazolidine-5-carboxylates
have been synthesized stereoselectively from N-Boc-β-amino alcohols by O-tosylation followed by SN2
cyclization. All the compounds prepared are tested for their in vitro anti-bacterial
activity against S. aureus, E.faecalis and E.faecium.</i
Synthesis of <i>syn</i>-<i>N</i>-aryl sulfonyl-4-substituted phenyl-2-oxo-1,3-oxazolidine-5-carboxylates and their conversion to <i>ant</i>-form using DBU
366-371Novel syn-N-arylsulfonyl-4-substituted
phenyl-2-oxo-1,3-oxazolidine-5-carboxylates have been synthesized from the
corresponding -azido alcohols and converted to their anti-form
by epimerizing C-2 proton using DBU. Studies on the stabilization energies are
done to evaluate conversion from syn-to anti-and not the
vice-versa. All the compounds have been tested for their in vitro anti-bacterial
activity against S. aureus, E. faecalis and E. faecium.</i