Munir Essiz

Fluoronaphthyridines and quinolones as antibacterial agents. 2. Synthesis and structure-activity relationships of new 1-tert-butyl 7-substituted derivatives.

A number of 7-substituted-1-tert-butyl-6-fluoroquinolone-3-carboxylic acids and 7-substituted-1-tert-butyl-6-fluoro-1,8-naphthyridine-3-carboxylic acids have been prepared and tested for antibacterial activities. Among those the 7-aminopyrrolidinyl 20b and the 7-diazabicyclo naphthyridine 18b are the most potent compounds in vitro and in vivo. Physicochemical data and acute toxicity are also discussed. Compound 18b, BMY 40062, exhibits the most favorable overall properties, considering in vitro and in vivo microbiological activity, its low toxicity, and pharmacokinetic profile, and was selected for clinical evaluation.

Stereoselective addition reactions to chiral N-benzylidene-p-toluenesulfinamides. Application to the synthesis of optically active 1,2-diphenylethylamines

Abstract An efficient and enantiospecific synthesis of substituted 1,2-diphenylethylamines 5 from benzaldehydes is described using a recyclable chiral auxiliary.

Studies Toward the Stereocontrolled Synthesis of a Key Azetidinone-Acid Intermediate in the Preparation of a New Carbapenem

Abstract An efficient and stereocontrolled preparation of the key a/etidinone-acid 5a is described.

Utilisation du fluorure de tetrabutylammonium comme de cyclisation dans la synthese d'antibacterines derives d'acide pyridone-4-carboxylique-3

Resume It has been found that the Bu4NF/THF base/solvent couple is very efficient in the key cyclisation step of ( 2 ) to ( 5 ) in the synthesis of antibacterial pyridonecarboxylic acid derivatives. In particular chiral intermediate ( 2d ) is directly converted in one step to ( 4d ), a key intermediate in the synthesis of (S)-Ofloxacin.