O-alkyl macrolide and azalide derivatives and regioselective process for their preparation
US7435805B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | May 21, 2004 |
| Grant date | Oct 14, 2008 |
| Priority date | — |
| Expiry date | Jan 23, 2025 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07H17/08
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.