- OXAZOLIDINONE DERIVATIVES AS ANTIMICROBIALS
-
The present invention relates to certain substituted phenyl oxazolidinones and to processes for the synthesis of the same. This invention also relates to pharmaceutical compositions containing the compounds of the present invention as antimicrobials. The compounds are useful antimicrobial agents, effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria, for example, multiple-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms, for example, Bacterioides spp. and Clostridia spp. species, and acid fast organisms, for example, Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp.
- -
-
Page/Page column 74
(2010/10/20)
-
- Further Studies on the Synthesis of Quinazolines from 2-Fluorobenzonitriles
-
Recently, we reported that appropriately substituted 2-fluorobenzonitriles undergo cyclization with guanidine carbonate to afford 2,4-diaminoquinazolines usually in good to excellent yield.This paper describes the preparation of a variety of new 2,4-diaminoquinazolines substituted at positions five or seven.In addition, the reactions of selected 2-fluorobenzonitriles with formamidine acetate or acetamidine acetate were examined.The results obtained demonstrate that the analogous 4-amino- and 2-methyl-4-aminoquinazolines can be prepared by this approach but that yields are considerably lower than when guanidine carbonate is employed as the cyclization reagent.
- Hynes, John B.,Tomazic, Alenka,Parrish, Christie A.,Fetzer, Oliver S.
-
p. 1357 - 1364
(2007/10/02)
-
- Displacement of Halogen of 2-Halogeno-Substituted Benzonitriles with Carbanions. Preparation of (2-Cyanoaryl)arylacetonitriles
-
(2-Cyanoaryl)arylacetonitriles are obtained by displacement of halogen of 2-halobenzonitriles with phenylacetonitrile anions.The method also applies to a number of heteroaromatics with ortho-situated halogen and cyano groups and to heteroarylacetonitrile anions.The anions were generated by using potassium tert-butoxide or potassium carbonate.Calculated electron densities of the electrophilic centers reflect the reactivity in the displacement reaction.The calculations indicate that the potassium ion complexes with the cyano group of the 2-halobenzonitriles in nonpolar solvents, thus promoting competitive addition of the anion to the cyano group.Carbanions derived from acids with pKa ca. 19-23 similarly displaced the halogen of 2-halobenzonitriles.
- Bech Sommer, Michael,Begtrup, Mikael,Boegesoe, Klaus Peter
-
p. 4817 - 4821
(2007/10/02)
-
- The Synthesis and Transition Temperatures of Some Fluoro-Substituted 4-Cyanophenyl and 4-Cyanobiphenyl-4'-yl 4-Pentyl- and 4-Butoxy-Benzoates
-
A series of 4-cyanophenyl 4-X-benzoates and a series of 4-cyanobiphenyl-4'-yl 4-X-benzoates (X= pentyl, butoxy) have been prepared without fluoro-substitution and with mono-fluoro to tetra-fluoro-substitution; all possible combinations of substitution patterns at the positions ortho- to the cyano group and ortho- to the carboxylate group have been obtained in an attempt to determine the structural features which are responsible for some members of these series showing very large positive values of dielectric anisotropy.The synthesis of novel precursors required for the preparation of these esters is described and the melting points and transition temperatures of the esters are discussed and an explanation is provided for the variation of Tn-1 values with position and extent of fluoro-substitution. - Keywords: Fluoro-substitution, phenyl and biphenyl benzoates, terminal cyano namatogens.
- Gray, G. W.,Hird, M.,Lacey, D.,Toyne, K. J.
-
p. 165 - 190
(2007/10/02)
-