Title:
METHODS UTILIZING ARYL THIOIMINES IN SYNTHESIS OF ERYTHROMYCIN DERIVATIVES
Document Type and Number:
WIPO Patent Application WO2002050093
Kind Code:
A3
Abstract:
An efficient deoximation technique for use in synthesis of erythromycin derivatives, involving aryl thioimine intermediates is disclosed. The aryl thioimine intermediates can be utilized in a method for protecting a ketone of a ketone-containing erythromycin derivative as a thioimine; a method for deoximating an oxime-containing erythromycin derivative, or a method for preparing a 6-O-alkyl erythromycin derivative. Presently preferred erythromycin derivatives have a C-9 oxime or a C-9 ketone.
Inventors:
LUKIN KIRILL A
Application Number:
PCT/US2001/051124
Publication Date:
March 06, 2003
Filing Date:
December 19, 2001
Export Citation:
Assignee:
ABBOTT LAB (US)
International Classes:
A61K31/7048; A61P31/04; C07B61/00; C07H17/08; (IPC1-7): C07H17/08; A61K31/7048; A61P31/04
Foreign References:
| US5852180A | 1998-12-22 |
Other References:
D.H.R. BARTON ET AL.: "Reduction of oximes and aliphatic nitro compounds to imines for further in situ reactions: A novel synthesis of pyrroles and pyrrolin-2-ones", J. CHEM. SOC. PERKIN TRANS. 1, 1986, pages 2243 - 2252, XP002211871
Download PDF: