C - Chemistry – Metallurgy – 07 – H
Patent
C - Chemistry, Metallurgy
07
H
C07H 17/00 (2006.01) C07H 17/08 (2006.01)
Patent
CA 2526732
The present disclooure 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 -0- alkyl macrolides and azalides as antibacterial agents or intermediates for the synthesis of other antibacterial agents.
L'invention concerne des macrolides et des azalides nouveaux de 11-<I>O</I>-alkyle, ainsi que leurs sels et solvates pharmaceutiquement acceptables et des compositions pharmaceutiques qui les contiennent. L'invention concerne également un procédé de préparation de macrolides et d'azalides de 11-<I>O</I>-alkyle par 11-<I>O</I>-alkylation stéréosélective de macrolides et d'azalides ayant un système diol vicinal, en utilisant des diazoalcanes en présence d'halogénures de métaux de transition ou d'acide borique comme catalyseurs. Un autre aspect de l'invention concerne les utilisations des macrolides et des azalides de 11-<I>O</I>-alkyle comme agents anti-bactériens ou comme produits intermédiaires pour la synthèse d'autres agents anti-bactériens.
Derek Marko
Kidemet Davor
Lazarevski Gorjana
Leljak Marija
Glaxosmithkline Istrazivacki Centar Zagreb D.o.o.
Gowling Lafleur Henderson Llp
Pliva-Istrazivacki Institut D.o.o.
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