The invention relates to novel compounds from the class of macrolide antibiotics. Particularly, the invention relates to novel 3,6-heiketals from the class of 9a-azalides, to their pharmaceutically acceptable addition salts with inorganic or organic acids, to a process for their preparation and to the use thereof as antibiotics or as intermediates for the synthesis of other macrolide antibiotics.
Compounds are of the formula: ##STR1## and to pharmaceutically acceptable salts thereof. The compounds of formula 1 are potent antibacterial agents that can be used to treat various bacterial infections and disorders related to such infections. The invention also relates to pharmaceutical compositions including the compounds of formula 1 and to methods of treating bacterial infections by administering the compounds of formula 1. The invention also relates to methods of preparing the compounds of formula 1 and to intermediates useful in such preparation.
This invention relates to a method for preparing azithromycin dihydrate from crude azithromycin by the gradual crystallization of azithromycin from acetone by the addition of a minimal amount of water to effect crystal formation is disclosed. This invention also relates to a method of making azithromycin from desmethyl-azithromycin by dissolving desmethyl-azithromycin in acetone, adding activated carbon, adding formaldehyde, adding formic acid; refluxing the desmethyl-azithromycin acetone solution, adding sodium hydroxide to induce precipitation of azithromycin, and isolating azithromycin.
8a-Azalides are useful in the treatment and prevention of bacterial respiratory and enteric infections in livestock animals, particularly in cattle and swine.
