96800-34-9Relevant academic research and scientific papers
Synthesis of oxazolidinones by a solid-phase/activation cycloelimination (sp/ace) methodology
Ten Holte, Peter,Van Esseveldt, Bart C. J.,Thijs, Lambertus,Zwanenburg, Binne
, p. 2965 - 2969 (2007/10/03)
A versatile method for the solid-phase synthesis of oxazolidinones is described. An appropriate 1,2-diol is attached to immobilized sulfonyl chloride, resulting in the selective activation of one of the alcohol functions. The subsequent reaction of the ot
Polymer-aided stereodivergent synthesis (PASS): A new concept for the discrete preparation of optical antipodes
Ten Holte, Peter,Thijs, Lambertus,Zwanenburg, Binne
, p. 1093 - 1095 (2007/10/03)
A new concept to the discrete prepartion of optical antipodes is reported. The approach makes use of a cyclization/cleavage procedure that has been applied to polymer-supported quasi-meso compound 1, containing a polymeric leaving group and a regular leaving group. Two-directional cyclization leads to the formation and separation of quasi-enantiomers 2 and 3 simultaneously, with one being immobilized and on free in solution. Treatment of 2 and 3 with appropriate nucleophiles gives discrete enantiomers 4 and 5.
A short synthesis of oxazolidinone derivatives linezolid and eperezolid: A new class of antibacterials
Lohray, Braj B.,Baskaran, Sundarababu,Rao, B. Srinivasa,Reddy, B. Yadi,Rao, I. Nageswara
, p. 4855 - 4856 (2007/10/03)
Oxazolidinone derivatives such as Linezolid and Eperazolid, which are a new class of antibacterials, have been synthesized from 1,2,5,6-dianhydro- 3,4-isopropylidine-D-mannitol in good yield.
Antibacterials. Synthesis and structure-activity studies of 3-aryl-2-oxooxazolidines. 1. The 'B' group
Gregory,Brittelli,Wang,Wuonola,McRipley,Eustice,Eberly,Bartholomew,Slee,Forbes
, p. 1673 - 1681 (2007/10/02)
The synthesis and structure/activity studies of the effect of varying the 'B' group in a series of oxazolidinone antibacterials (I) are described. Two synthetic routes were used: (1) alkylation of aniline with glycidol followed by dialkyl carbonate heterocyclization to afford I (A = H, B = OH), whose arene ring was further elaborated by using electrophilic aromatic substitution methodology; (2) cycloaddition of substituted aryl isocyanates with epoxides to give A and B with a variety of values. I with B = OH or Br were converted to other 'B' functionalities by using S(N)2 methodology. Antibacterial evaluation of compounds I with A = acetyl, isopropyl, methylthio, methylsulfinyl, methylsulfonyl, and sulfonamido and a variety of different 'B' groups against Staphylococcus aureus and Enterococcus faecalis concluded that the compounds with B = aminoacyl, and particularly acetamido, were the most active of those examined in each A series, possessing MICs in the range of 0.5-4 μg/mL for the most active compounds described.
