O-alkyl macrolide and azalide derivatives and regioselective process for their preparation
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United States of America Patent
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Oct 14, 2008
Grant Date -
Jul 28, 2005
app pub date -
May 21, 2004
filing date -
May 30, 2003
priority date (Note) -
Expired
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Abstract
The present disclosure relates to new 11-O-alkyl macrolides and azalides and pharmaceutically acceptable salts and solvates thereof, and to pharmaceutical compositions thereof. The disclosure also relates to a process for the preparation of 11-O-alkyl macrolides and azalides by regioselective 11-O-alkylation of macrolides and azalides having a vicinal diol system, using diazoalkanes in the presence of transition-metal halides or boric acid as catalysts. In another aspect, the disclosure relates to uses of the 11-O-alkyl macrolides and azalides as antibacterial agents or intermediates for the synthesis of other antibacterial agents.
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