Synthesis and antibacterial activity of C12 des-methyl ketolides.
Lin X, Rico AC, Chu DT, Carroll GL, Barker L, Shawar R, Desai MC, Plattner JJ.
Synthesis of C(12) des-methyl ketolide is developed featuring an intramolecular epoxide formation/elimination process to establish the C(12) stereocenter. These ketolides are potent against several key respiratory pathogens, including erythromycin resistant erm- and mef-containing strains of Streptococcus pneumoniae.