PDF herunterladen
Synfacts 2012; 8(8): 0815
DOI: 10.1055/s-0032-1316597
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart · New York

Synthesis of a Telithromycin Analogue

Rezensent(en):
Philip Kocienski
Li B et al. * Pfizer Global Research and Development, Groton, USA; Shanghai ChemPartner Co. Ltd., Shanghai and Asymchem Life Science Co. Ltd., Tianjin, P. R. of China
Process Development of a Novel Ketolide Antibiotic.

Org. Process Res. Dev. 2012;
16: 788-797
CrossrefSuche in Google Scholar
Weitere Informationen

Publikationsverlauf

Publikationsdatum:
19. Juli 2012 (online)

 
 als PDF herunterladen Lizenzen und Reprints

Key words

telithromycin analogues - clarithromycin - ketolide antibiotics - Corey–Kim oxidation - reductive amination

Significance

The target telithromycin analogue was under development as an oral antibiotic for the treatment of respiratory infections. The route depicted delivered kilogram quantities of API starting with clarithromycin (A).


#

Comment

Note the use of a large-scale Corey–Kim oxidation for the synthesis of the ketolide E. An efficient large-scale synthesis of 3-hydroxy-1,5-naphthyridine-4-carbaldehyde (G) was developed using a Skraup reaction.


#
#


   Lizenzen und Reprints